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Dissertations / Theses on the topic 'Opioid ligands'

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Published: 4 June 2021

Last updated: 16 February 2022

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1

McFadyen, Iain James. "Structure-activity relationships of opioid ligands." Thesis, Loughborough University, 1999. https://dspace.lboro.ac.uk/2134/33189.

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There are three different types of opioid receptor, namely mu, delta and kappa. Morphine and related clinically useful analgesics exert their actions through the mu opioid receptor. Such compounds represent a huge structural diversity, including both peptides and alkaloids. Nevertheless, there exists a common pharmacophore comprising two critical features, namely an amine nitrogen and an aromatic ring, usually with a hydroxyl substituent; the spatial relationship between them is also vital.

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2

Bergström, Jonas. "Opioid ligands and receptors of the joint /." Stockholm, 2006. http://diss.kib.ki.se/2006/91-7140-751-0/.

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3

Paterson, S. J. "Multiple opioid binding sites and their ligands." Thesis, University of Aberdeen, 1986. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.378093.

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The presence of μ-, δ- and κ-binding sites in homogenates of guinea-pig brain was demonstrated by the use of selective labelling techniques. In saturation experiments, the tritiated ligands [^3H]-[D-Ala^2, MePhe^4, Gly-ol^5]enkephalin, [^3H]-dihydromorphine, [^3H]-morphine and [^3H]-dihydronormorphine labelled only the μ-binding site. The δ-binding site could be labelled selectively with [^3H]-[D-Pen^2, D-Pen^5]enkephalin. However, the less selective δ-ligand, [<sup>3</sup>H]-[D-Ala<sup>2</sup>, D-Leu<sup>5</sup>] enkephalin, could only be used when its μ-binding was blocked with the unlabelle

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4

Jales, Andrew. "Studies of selective ligands for opioid receptors." Thesis, University of Bristol, 2000. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.302154.

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5

DiMattio, Kelly Marie. "Studies on Ligands of the Kappa Opioid Receptor." Diss., Temple University Libraries, 2016. http://cdm16002.contentdm.oclc.org/cdm/ref/collection/p245801coll10/id/334919.

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Pharmacology<br>Ph.D.<br>This thesis is comprised of three parts. In the first part, we investigated zyklophin, a novel selective short-acting kappa opioid receptor (KOPR) antagonist, and its effects on scratching behaviors in Swiss-Webster mice. We investigated whether zyklophin was able to induce scratching in a dose-dependent fashion, and whether this scratching behavior could be blocked by pretreatment with nor-binaltorphimine (norBNI). We also used KOPR -/- mice to further clarify the role of the KOPR in this behavior. In the second part, we examined the role of the divergent amino acid a

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6

Lu, Yu. "Ligands for the sigma receptor and the mu-opioid receptor." Diss., Columbia, Mo. : University of Missouri-Columbia, 2007. http://hdl.handle.net/10355/4961.

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Thesis (M.S.)--University of Missouri-Columbia, 2007.<br>The entire dissertation/thesis text is included in the research.pdf file; the official abstract appears in the short.pdf file (which also appears in the research.pdf); a non-technical general description, or public abstract, appears in the public.pdf file. Title from title screen of research.pdf file (viewed on January 4, 2008) Includes bibliographical references.

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7

Obeng, Samuel. "Design, Synthesis, and Biological Screening of Selective Mu Opioid Receptor Ligands as Potential Treatments for Opioid Addiction." VCU Scholars Compass, 2017. http://scholarscompass.vcu.edu/etd/4771.

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Today, more Americans die each year because of drug overdoses than are killed in motor vehicle accidents. In fact, in 2015, more than 33,000 individuals died due to an overdose of heroin or prescription opioids. Sadly, 40-60 % of patients on current opioid addiction treatment medications relapse. Studies have shown that the addiction/abuse liability of opioids are abolished in mu opioid receptor (MOR) knock-out mice; this indicates that the addiction and abuse liability of opioids are mainly mediated through MOR. Utilizing the “message-address concept”, the our laboratory reported a novel non-

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8

Kulkarni, Vinod V. "Novel Bifunctional Ligands For Neuropathic Pain: Design and Synthesis of Overlapping Pharmacophores of Opioid and Melanocortin Ligands." Diss., The University of Arizona, 2012. http://hdl.handle.net/10150/228191.

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Biologically many disease states lead to changes in expressed proteins. Therefore, "system changes" that occur must be considered in any treatment for the disease. This new approach to drug design and discovery would be particularly applicable to the diseases that involve adaptive changes in the central nervous system, such as neuropathic pain. There is growing evidence that drugs behave differently in pathological states than in normal states, thus preventing their effectiveness in pathological disease states. Therefore, a new paradigm for drug design is needed. In recent years, the melano

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9

Patel, Dinesh. "Structural and pharmacological studies of synthetic and endogenous opioid receptor ligands." Thesis, Loughborough University, 1992. https://dspace.lboro.ac.uk/2134/11073.

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The interaction of a diverse set of opioid alkaloids and peptides with various opioid receptors has been examined using biochemical and pharmacological techniques. Structural information on the compounds was obtained from single crystal X-ray diffraction and nuclear magnetic resonance studies, and modelled by computational methods. The introduction of a dithiocarbazate moiety into the 7a-position of a bridged thebaine was shown to afford a degree of μ selectivity in this class of nonselective compounds. X-ray diffraction analysis of this compound and comparison with the structure of [Met5]enke

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10

Oakley, Sarah M. "The influence of G-protein coupling of the #delta#-opioid receptor on the activity of #delta#-opioid receptor ligands." Thesis, University of Surrey, 2000. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.326816.

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11

Derrick, Ian. "Cinnamoylamino and methoxyfumaroylamino derivatives of epoxymorphinans - potential irreversible ligands for opioid receptors." Thesis, University of Bristol, 1996. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.336849.

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12

Kulkarni, Abhishek S. "Design, Synthesis and Pharmacological Characterization of Potential Mu Opioid Receptor Selective Ligands." VCU Scholars Compass, 2019. https://scholarscompass.vcu.edu/etd/5787.

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Selective Mu Opioid Receptor (MOR) antagonists possess immense potential in the treatment of opioid abuse/addiction. Utilizing the “message-address” concept, our laboratory reported a novel, reversible, non-peptide MOR selective antagonist 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4՛-pyridyl)carboxamido]morphinan (NAP). Molecular modeling studies revealed that the selectivity of NAP for the MOR is because of a π-π stacking interaction of its pyridine ring with the Trp318residue in theMOR. Pharmacological characterization showed that NAP is a P-glycoprotein substrate, thereby limitin

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13

Elbegdorj, Orgil. "DESIGN, SYNTHESES, AND BIOLOGICAL EVALUATION OF 14-N-SUBSTITUTED NALTREXONE DERIVATIVES AS OPIOID RECEPTOR LIGANDS." VCU Scholars Compass, 2013. http://scholarscompass.vcu.edu/etd/455.

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Opium, the dried resin obtained from the unripe seedpods of the poppy flower, has been used for medicinal and euphoric purposes since ancient times. Morphine, the main active ingredient of opium, and other clinically useful opioid analgesics all mediate their effects through activating the mu opioid receptor. Studies involving the mu opioid receptor knockout mice showed that the interaction with the mu opioid receptor is also responsible for many notorious side effects associated with these drugs including dependence and addiction. Therefore, selective antagonists for the mu opioid receptor

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14

Bell, Katrina Margaret. "A biochemical and pharmacological characterisation of some endogenous and exogenous κ opioid ligands". Thesis, Loughborough University, 1994. https://dspace.lboro.ac.uk/2134/12053.

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An investigation of the interaction of stable opioid/ligands and unstable opioid peptides with opioid receptors in guinea pig brain, guinea pig myenteric plexus and mouse vas deferens has been carried out. The initial aim of the study was to further characterise K opioid receptors, using binding assays and isolated tissue bioassays. The second aim was to determine the true affinity and potency of small dynorphin peptides for the K opioid receptor and to determine if metabolism of the peptides to non K opioid receptor-preferring products contributes to their observed in vitro pharmacology.

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15

Crook, Tracy J. "The in vivo and in vitro pharmacology of selective #delta#-opioid receptor ligands." Thesis, University of Surrey, 1993. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.359841.

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16

Black, Shannon Leigh. "The design, synthesis and pharmacological evaluation of ligands targeted at the kappa opioid receptor." Thesis, University of Bath, 2001. https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.392061.

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17

Ramos-Colon, Cyf Nadine, and Cyf Nadine Ramos-Colon. "Design, Synthesis, and Biological Evaluation of Novel Peptide Ligands as Kappa Opioid Receptor Antagonists." Diss., The University of Arizona, 2016. http://hdl.handle.net/10150/621869.

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Millions of people in the US currently suffer from chronic pain but available therapeutics do not provide effective chronic pain treatment. Opiate therapy is still the gold standard for chronic pain management with detrimental side effects, such as tolerance, addiction, constipation, and respiratory depression that limit their therapeutic potential. Opiates exert their positive and negative effects by activating the μ opioid receptor (MOR). Conversely, the κ opioid receptor (KOR) has been shown to modulate the tolerance and addiction produced by MOR agonists and is also involved in mood modula

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18

Hall, Sara M. "Bradykinin Ligands and Receptors Involved in Neuropathic Pain." Diss., The University of Arizona, 2015. http://hdl.handle.net/10150/578606.

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Neuropathic pain is a prevalent disease with no effective, safe treatments and limited knowledge on the mechanisms involved. One target for neuropathic pain treatment may be the blockade of Dynorphin A (Dyn A). Dyn A is a unique endogenous ligand that possesses well-known neuroinhibitory effects via opioid receptors and neuroexcitatory effects that are mediated through the bradykinin 2 receptors (B2Rs). Extensive SAR was carried out to develop a ligand for the blockade of the excitatory actions of Dyn A at the B2R. A lead ligand was able to block Dyn A-induced hyperalgesia in naïve animals and

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19

Reinecke, Bethany A. "Development of Bivalent Ligands Targeting the Putative Mu Opioid Receptor and Chemokine Receptor CXCR4 Heterodimer." VCU Scholars Compass, 2019. https://scholarscompass.vcu.edu/etd/5754.

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Human immunodeficiency virus (HIV) and opioid abuse have been described as synergistic epidemics. Pharmacologically, it has been found that opioids have the capacity to enhance HIV infection and replication. Research has shown that activation of the mu-opioid receptor (MOR) elevates the expression of the HIV-1 entry co-receptor CXCR4 on T-lymphocytes in the peripheral nervous system, thus allowing for enhanced viral entry and invasion. Although the exact mechanism for opioid modulation of CXCR4 expression and subsequent exacerbation of HIV is unknown, several hypotheses exist. One hypothesis i

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20

Cain, James Patrick. "Design, Synthesis, and Evaluation of New Ligands for G Protein-Coupled Receptors and Kinases." Diss., The University of Arizona, 2011. http://hdl.handle.net/10150/204272.

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Peptidergic G Protein-Coupled Receptors (GPCRs) play a role in many of the most important biological functions, and the ability to modulate the activity of these critical proteins has tremendous potential to increase our understanding of biology and allow the development of new therapeutics. In some cases this knowledge will point towards the importance of interconnected proteins of the same or different classes, such as kinases, which interact in a complex and dynamic network in vivo. Understanding these systems will be crucial for addressing unmet therapeutic needs, and new chemical structur

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21

Remesic, Michael Vincent, and Michael Vincent Remesic. "The Design, Synthesis, and Biological Evaluation of Novel Peptidic Ligands for the Treatment of Chronic Neuropathic Pain." Diss., The University of Arizona, 2017. http://hdl.handle.net/10150/625593.

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Chronic neuropathic pain is a disease that impacts the livelihood of millions of people in the United States with no effective pain treatments and limited information pertaining to the underlying mechanisms. Opioid therapy is considered the gold standard for pain therapeutics, but chronic use of these medications brings about serious side effects such as tolerance, addiction, and respiratory depression which limit their overall therapeutic potential. Herein, two approaches are discussed to circumvent these issues: i) a multifunctional approach using N-phenyl-N-piperidin-4-yl-propionamide (Ppp)

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22

Chauvignac, Cédric. "Studies towards the synthesis of new irreversible and selective reversible ligands for the kappa opioid receptor." Thesis, University of Bath, 2005. https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.415765.

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There is considerable interest in the synthesis of K-antagonists as therapeutic agents but also as a means of further understanding the role of the K-opioid receptor. In the search for irreversible and selective reversible K-opioid antagonists, it was decided to modify the structures of the two most well-known K-antagonists, GNTI and norBNI. In particular, two main approaches have been used for the design of novel ligands; these explored the introduction of electrophilic (isothiocyanate) or lipophilic (substituted/unsubstituted benzyl) groups onto the guanidinium moiety of GNTI or at the pyrro

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23

Min, Byoung Joon. "PART I. DESIGN AND SYNTHESIS OF BICYCLIC INTERNAL BETA-TURN MIMETICS AND THEIR INCORPORATION INTO BIOLOGICALLY ACTIVE LIGANDS; PART II. SYNTHESIS OF CYCLIC PEPTIDES BY RING." Diss., The University of Arizona, 2010. http://hdl.handle.net/10150/194081.

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beta-Turns in many biologically active peptides are important secondary structural elements which are critical for their biological activities. Hence, it is not surprising that beta-turn based pharmacophore design including beta-turn mimetics has become a central topic in medicinal chemistry in addition to alpha-helix or helical peptides. One of the advantages of such beta-turn mimetics is that they can better control torsion angles of the backbone of peptides and to some degree dihedral angles chi (X). These beta-turn mimicking scaffolds are designed to have a higher avidity for the acceptor

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24

Kinzeler, Nicole R. "Circuitry and function of mu opioid ligands in the rostral nucleus of the solitary tract and reticular formation." The Ohio State University, 2011. http://rave.ohiolink.edu/etdc/view?acc_num=osu1313104355.

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25

Holmberg, Pär. "Synthesis of Molecular Probes for Exploring the Human Consciousness, 5-HT7 Ligands and Salvinorins." Doctoral thesis, Uppsala universitet, Institutionen för läkemedelskemi, 2005. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-4824.

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In this study, we have addressed the serotonergic and the opioid system within the CNS. Both systems are of outmost importance in the etiology of disease states, especially mental disorders. In our investigation of the serotonergic system, we have synthesized novel enantiomerically pure 6-aryl-3-amino- and 8-aryl-3-aminochromans as ligands for the 5-HT7 receptor. One reason for the lack of understanding of the physiological functionality of the serotonin 5-HT7 receptor, the most recently discovered member of the serotonin receptor family, is the absence of partial agonists and agonists. In th

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26

Holmberg, Pär. "Synthesis of Molecular Probes for Exploring the Human Consciousness, 5-HT₇ Ligands and Salvinorins." Doctoral thesis, Uppsala University, Department of Medicinal Chemistry, 2005. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-4824.

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<p>In this study, we have addressed the serotonergic and the opioid system within the CNS. Both systems are of outmost importance in the etiology of disease states, especially mental disorders. </p><p>In our investigation of the serotonergic system, we have synthesized novel enantiomerically pure 6-aryl-3-amino- and 8-aryl-3-aminochromans as ligands for the 5-HT<sub>7</sub> receptor. One reason for the lack of understanding of the physiological functionality of the serotonin 5-HT<sub>7</sub> receptor, the most recently discovered member of the serotonin receptor family, is the absence of parti

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27

Xiong, Chiyi. "Asymmetric synthesis of conformationally and topographically constrained amino acids as peptidomimetics: An approach to design and synthesis of opioid receptor selective ligands." Diss., The University of Arizona, 2003. http://hdl.handle.net/10150/280393.

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As part of continuing efforts to obtain backbone and side chain conformationally constrained, novel amino acids,¹⁻⁷ we have successfully developed the asymmetric synthesis of β-phenyl-substituted cysteine, tryptophan, and serene derivatives. In this approach, the key intermediate, enantiomerically pure 3-phenylaziridine-2-carboxylic ester, was prepared from an α, β-unsaturated ester by employing the Sharpless asymmetric dihydroxylation. The aziridine was treated with 4-methoxybenzylthiol, indole, and acetic acid to give β-phenyl-substituted cysteine, tryptophan, and serine, respectively, in a

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28

Al-Deeb, Omar A. A. "On the investigation of the synthesis, stereochemistry and structure-activity relationship of opioid ligands related to 4-aryl-1-methylpiperidines and phencyclidine." Thesis, University of Bath, 1989. https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.760592.

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29

Alfaro-Lopez, Lorenzo Josue. "Development of new conformationally and topographically constrained p60(c-src) PTK inhibitors. Solution and solid-phase approaches for the synthesis of delta-opioid receptor peptidomimetic ligands." Diss., The University of Arizona, 1999. http://hdl.handle.net/10150/288981.

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Based on the efficient substrate for p60ᶜ⁻ˢʳᶜ protein tyrosine kinase (PTK) YIYGSFK (1) (K(m) = 55 μM) obtained by combinatorial methods, we have designed and synthesized a series of conformationally and topographically constrained substrate-based peptide inhibitors for this enzyme. The inhibitors showed IC₅₀ values in low micromolar range (0.1-3 μM). A "rotamer scan" was performed by introducing four stereoisomers of β-Me(2')Nal in the postulated interaction site of peptide inhibitor (23) Y-c[D-Pen-(2')Nal-GSFC]KR-NH₂ (IC₅₀ = 1.6 μM). We found that the χ¹ space constraints imposed by the spec

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30

Drieu, la Rochelle Armand. "Etude des interactions fonctionnelles entre récepteurs à peptide RF-amide et caractérisation de ligands bifonctionnels des récepteurs mu opioïde et NPFF." Thesis, Strasbourg, 2018. http://www.theses.fr/2018STRAJ109/document.

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Les opiacés demeurent des molécules incontournables dans le traitement des douleurs moyennes à sévères. Si leur efficacité dans le traitement de la douleur aiguë est incontestable, leur utilisation chronique est responsable de nombreux effets indésirables comprenant une hypersensibilité à la douleur et une tolérance à leurs effets analgésiques. Une partie de ces effets secondaires résulteraient de l’activation de systèmes anti-opioïdes endogènes, comme les neuropeptides RF-amide, dont des études précédentes suggèrent une complémentarité de fonctionnement dans la modulation de la douleur. Le pr

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31

Basti, Vida. "Ligand biased signaling of opioid agonists forphosphorylation and regulation of μ -opioid receptors". Thesis, Uppsala universitet, Farmakologi, 2013. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-192584.

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Abstract Ligand biased signaling of opioid agonists for phosphorylation andregulation of μ -opioid receptors Student: Vida Basti. Supervisor: Prof Macdonald Christie. Departmement of Neuropharmacology, The University of Sydney. Examiner: Prof Ingrid Nylander. Departement of Phamacology, University of Uppsala. Opioid drugs are of great use in the medical practise. The drugs are commonly prescribed formany types of illnesses, mostly in cases of pain management. Although opioids come withmany benefits they are causing a lot of problems as well. The side effects are many andamongst these is tolera

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32

Tang, Xue-jun. "Asymmetric synthesis of stereochemically-defined and conformationally-constrained novel amino acids via direct alkylation of chiral nickel(II)-coordinated Schiff bases of glycine and alanine, and design and synthesis of selective peptide and non-peptide ligands for the delta-opioid receptor." Diss., The University of Arizona, 2002. http://hdl.handle.net/10150/279911.

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A systematic practical method to prepare highly chi (χ)-constrained amino acids has been developed. It was found that increasing the size of R¹ (see figure) from H to Me to Et to n-Pr led to decreased reactivity of the starting complexes. In the case of R¹ as i-Pr, no alkylation was observed. With an increase of the size of R² from H to Me to Et to i-Bu, the reactivities of the alkyl bromides decreased. The starting Schiff bases had more effective stereocontrol at the α-carbon center than at the β-carbon center. The starting Schiff bases showed differential reactivity toward the racemic electr

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33

Qian, Xinhua. "Topographical design of the message domain pharmacophore of the delta opioid agonists using designer amino acids and design of non-peptide ligand for opioid receptors." Diss., The University of Arizona, 1995. http://hdl.handle.net/10150/187062.

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A series of highly constrained tyrosine derivatives, 2',6'-dimethyl- β-methyltyrosines (TMTs), was designed and asymmetrically synthesized. Incorporation of the TMT isomers into peptide agonists of δ opioid receptors provide analogues that are highly potent and selectively for δ opioid receptors and have revealed the stereochemical requirements for recognizing opioid δ receptors. Moreover, the combination of conformational studies and pharmacological studies of the peptide analogues provided for the first time the stereochemical requirements for specifically recognizing opioid δ receptor subty

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34

Wong, Yung Hou. "Molecular basis of the opioid receptor-ligand interactions : the role of guanine nucleotide-binding proteins." Thesis, University of Cambridge, 1988. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.303263.

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35

Richer, Romain. "Coeur, mitochondries, lésions d'ischémie-reperfusion : impact du diabète et du post-conditionnement par les ligands opiacés." Thesis, Normandie, 2018. http://www.theses.fr/2018NORMC408.

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Depuis plus de 30 ans, les progrès thérapeutiques ont permis de réduire la morbi-mortalité liée à l’infarctus du myocarde. La reperfusion est une étape essentielle dans la prise en charge des patients, mais est également à l’origine de lésions tissulaires cardiaques. Plusieurs travaux ont montré que le conditionnement ischémique ou pharmacologique du coeur permet de réduire ces lésions de reperfusion, mais que cet effet bénéfique reste limité dans un contexte de diabète.Dans ce travail, nous avons tout d’abord étudié l’impact du diabète de type 2 sur la fonction mitochondriale. Les études ont

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GALZI, MEJEAN ANNICK. "Synthese de ligands opiaces photoactivables et marquage irreversible des recepteurs mu et kappa des opioides." Université Louis Pasteur (Strasbourg) (1971-2008), 1991. http://www.theses.fr/1991STR13131.

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Le travail presente ici vise a isoler et caracteriser le (les) recepteur(s) des opioides dans le but d'obtenir des informations structurales qui permettront, plus tard, d'aborder leur etude fonctionnelle. Dans l'etat actuel des connaissances, l'objectif majeur evident est d'obtenir la sequence en acides amines de ce ou ces recepteurs. A cet effet, les techniques de marquage irreversible ont deja montre qu'elles sont des outils precieux. Trois types de fonction photoactivable ont ete envisages: les sels d'aryldiazonium, les diazo et les arylazido et une vingtaine d'analogues opiaces comportant

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Dalton, George D. "The Study of the Effect of Drugs of Abuse on Protein Kinase A Activity in Mouse Brain and Spinal Cord." VCU Scholars Compass, 2005. http://scholarscompass.vcu.edu/etd/1527.

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Morphine and Δ9-THC are drugs that produce analgesia and rewarding effects. However, chronic treatment with morphine and Δ9-THC produces problematic side-effects including tolerance and physical dependence. The cellular mechanisms underlying opioid and cannabinoid antinociceptive tolerance have been studied for years. Research has demonstrated that the expression of morphine and Δ9-THC antinociceptive tolerance may be mediated through intracellular signaling pathways, such as the adenylyl cyclase /Protein Kinase A (PKA) cascade. The present study investigated the role of PKA in the expression

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38

Bibian, Mathieu. "Synthèse de 1,2,4-triazoles trisubstitués en position 3, 4 et 5 comme ligands potentiels de RCPGs." Thesis, Montpellier 2, 2010. http://www.theses.fr/2010MON20153.

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L'intérêt croissant de la communauté scientifique pour le noyau 1,2,4-triazole nous a amené à développer une nouvelle synthèse de cet hétérocycle substitué sur les positions 3, 4 et 5 par des acides aminés. L'étape clé de la synthèse est une étape de couplage-cyclisation utilisant du benzoate d'argent. Nous avons prouvé qu'il est possible d'utiliser des α-aminoacides comme produit de départ.L'étude cette réaction a montré qu'elle n'induit pas d'épimérisation sur les atomes de carbones en α des positions 3, 4 et 5 du noyau triazole et que le traitement optimisé permet d'éliminer les sels métall

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CHARPENTIER, STEPHANE. "Bases moleculaires de la reconnaissance selective de ligands peptidiques par les recepteurs opioides mu et delta." Paris 6, 1993. http://www.theses.fr/1993PA066530.

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Les glandes dermiques de rainettes sud-americaines du genre phyllomedusae, secretent en abondance de nombreuses substances biologiquement actives. Parmi celles-ci, les dermorphines, constituent une nouvelle famille de peptides opioides possedant des proprietes biologiques et structurales exceptionnelles. En effet, la dermorphine (tyr-d-ala-phe-gly-tyr-pro-ser-nh#2) est le ligand naturel le plus selectif des recepteurs de type mu. La dermenkephaline (tyr-d-met-phe-his-leu-met-asp-nh#2), la deltorphine i (tyr-d-ala-phe-asp-val-val-gly-nh#2) et la deltorphine ii (tyr-d-ala-phe-glu-val-val-gly-nh#

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Zaidi, Saheem. "Understanding ligand binding, selectivity and functions on the G protein-coupled receptors: A molecular modeling approach." VCU Scholars Compass, 2014. http://scholarscompass.vcu.edu/etd/596.

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The assessment of target protein molecular structure provides a distinct advantage in the rational drug design process. The increasing number of available G protein-coupled receptor crystal structures has enabled utilization of a varied number of computational approaches for understanding the ligand-receptor interactions, ligand selectivity and even receptor response upon ligand binding. The following dissertation examines the results from three different projects with varied objectives – i) structural modeling of human C-C chemokine receptor type 5 (CCR5) and assessment of the ligand binding

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GAIBELET, GERALD. "Mecanisme d'action du recepteur opioide de type : reconnaissance du ligand et couplage aux proteines g de transduction." Toulouse 3, 1998. http://www.theses.fr/1998TOU30039.

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Les substances opioides modulent la liberation de neuromediateurs dans le systeme nerveux central et peripherique par l'intermediaire de recepteurs specifiques : les recepteurs aux opioides. Trois classes de recepteurs (, et ) existent et appartiennent a la famille des recepteurs a 7 domaines transmembranaires couples aux proteines g. Mon travail a porte sur la caracterisation du site de liaison du recepteur qui semble etre le plus implique dans les effets analgesiques et toxicomanogenes des morphiniques, et sur l'analyse du couplage a differentes isoformes de proteines g. Le remplacement des

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Badri, Prajakta. "PREDICTION OF HUMAN SYSTEMIC, BIOLOGICALLY RELEVANT PHARMACOKINETIC (PK) PROPERTIES BASED ON QUANTITATIVE STRUCTURE PHARMACOKINETIC RELATIONSHIPS (QSPKR) AND INTERSPECIES PHARMACOKINETIC ALLOMETRIC SCALING (PK-AS)." VCU Scholars Compass, 2010. http://scholarscompass.vcu.edu/etd/124.

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This research developed validated QSPKR and PK-AS models for predicting human systemic PK properties of three, preselected, pharmacological classes of drugs, namely opioids, β-adrenergic receptor ligands (β-ARL) and β-lactam antibiotics (β-LAs) using pertinent human and animal systemic PK properties (fu,, CLtot, Vdss, fe) and their biologically relevant unbound counterparts from the published literature, followed by an assessment of the effect of different molecular descriptors on these PK properties and on the PK-AS slopes for CLtot and Vdss from two species (rat and dog). Lipophilicity (log

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Liao, Subo 1963. "Design and synthesis of topographically constrained amino acids, and bioactive peptides for studies of ligand-receptor interaction, and for de novo design of delta-opioid selective non-peptide mimetics as potential therapeutics." Diss., The University of Arizona, 1997. http://hdl.handle.net/10150/282418.

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Topographical constraint is the most powerful approach for the design of bioactive peptides to explore the bioactive conformation of crucial side-chain pharmacophores of amino acid residues in peptide-receptor recognition and signal transduction. Novel topographically constrained amino acids β-isopropylphenylalanine and 2',6'-dimethyl-2,3-methanophenylalanine have been designed and synthesized. Incorporation of the four optically pure β-isopropylphenylalanine stereoisomers into deltorphin I produced four peptide analogues of [β-iPrPhe]Deltorphin I with differentiated bioactivities. The most po

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Robichon, Alain. "Photoaffinité des récepteurs opioides U et D et du récepteur au VIP (vasoactive intestinal peptide)." Paris 6, 1987. http://www.theses.fr/1987PA066605.

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Chen, Qing Yuan, and 陳清淵. "New benzeneacetamide amine type compounds as selective ligands for the k opioid receptor." Thesis, 1996. http://ndltd.ncl.edu.tw/handle/11647214962120600512.

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Marková, Vendula. "Studium molekulárních interakcí μ-opioidního receptoru: vliv usměrňovacích ligandů". Master's thesis, 2019. http://www.nusl.cz/ntk/nusl-405221.

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G protein-coupled receptors (GPCRs) are the largest group of membrane-bound receptors. Transmission of signals into the cell interior is mediated through the interactions of these receptors with other signaling molecules. Nowadays, a great attention is devoted to biased ligands which are able to alter the conformation of the receptor in a specific way and thus distinctly affect its function. This diploma thesis was focused on a study of µ-opioid receptor (MOR), which is important in nociception. The aim of this study was to find out, how the activation of MOR by specific biased ligands (morphi

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Audet, Nicolas. "La sélectivité fonctionnelle des ligands du récepteur delta opiacé." Thèse, 2011. http://hdl.handle.net/1866/7057.

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Les récepteurs couplés aux protéines GRCPG sont une des plus grandes familles de récepteur membranaire codifié par le génome humain et certainement la plus grande famille de récepteurs. Localisés au niveau des membranes plasmiques, ils sont responsables d’une grande variété de réponses cellulaires. L’activation de ces derniers par des ligands était traditionnellement associée à un changement de conformation de la protéine, passant d’un état inactif à un état actif. Toutefois, certaines observations entraient en contradiction avec cette théorie et laissaient supposer la présence de plusieurs co

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"The effects of the endogenous mu-opioid ligands, endomorphin 1 and 2, on minute ventilation in the conscious rat." Tulane University, 2002.

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Endogenous ligands for the mu-opioid receptor (MOR) have been implicated in the central control of minute ventilation (VE) (Shook, et al. 1990). While these studies examined the effects of beta-endorphin on V E, beta-endorphin binds to the mu- and to the delta-opioid receptors with equal affinity and therefore cannot be considered a pure mu agonist. In 1997, two tetrapeptides, endomorphin 1 and 2 (EM1; EM2) were isolated from the bovine frontal cortex, shown to exhibit high selectivity and affinity for the MOR (Zadina, et al, 1997), and to produce antinociception (Zadina, et al, 1997), bradyca

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Bagheri, Haniyeh. "L'inhibition de la production d'AMPc est modulée différemment à court et long terme par l'internalisation du récepteur opioïde delta." Thèse, 2014. http://hdl.handle.net/1866/11815.

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Les opioïdes sont les analgésiques les plus puissants mais leur utilisation prolongée peut entraîner le développement d’une tolérance analgésique. La tolérance serait en partie associée à l’inhibition prolongée de l’adénosine monophosphate cyclique (AMPc) entraînant des changements compensatoires dans la voie de l’adénylate cyclase. Pour cette étude, nous avons eu recours à un biosenseur basée sur la technologie de Bioluminescence Resonnance Energy Transfer (BRET) et qui fournit des mesures de l’AMPc en fonction du temps réel. Durant les 15 premières minutes de stimulation, la réponse de l’AMP

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Hadzima, Martin. "Příprava modifikovaných ligandů mju-opioidních receptorů." Master's thesis, 2018. http://www.nusl.cz/ntk/nusl-387048.

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This diploma thesis deals with preparation of modified ligands of mu, delta and kappa opioid receptors, following up on the author's bachelor's thesis.1 The main goal of the submitted thesis is ligand tethering at an appropriate position using oligoethylene glycol linkers, to enable their use in the innovative iBodies concept.2 Ligands chosen for modifications were: naltrexone (μ-opioid receptor), naltrindole (δ-opioid receptor) and nalfurafine (κ-opioid receptor). Naltrexone was modified, according to the bachelor's thesis results, at the C-6 position with linker attachment via ether and amid

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