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Journal articles on the topic 'Piperazines; Pharmacology'

Author: Grafiati

Published: 4 June 2021

Last updated: 13 February 2022

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1

Šilhánková, Alexandra, Karel Šindelář, Karel Dobrovský, Ivan Krejčí, Jarmila Hodková, and Zdeněk Polívka. "Synthesis of New L-Proline Amides with Anticonvulsive Effect." Collection of Czechoslovak Chemical Communications 61, no. 7 (1996): 1085–92. http://dx.doi.org/10.1135/cccc19961085.

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Series of heterocyclic L-proline amides were prepared from BOC-L-proline and heterocyclic amines (mostly substituted piperazines and morpholines) via active ester with hydroxysuccinimide. 4-(4-Fluorobenzoyl)piperidine afforded L-proline 4-(4-(4-(4-fluorobenzoyl)piperidin-1-yl)benzoyl)piperidine (7b) simultaneously with expected L-proline 4-(4-fluorobenzoyl)piperidide (7a). D-Proline N-(3-(4-(3-chlorophenyl)piperazin-1-yl)propyl)amide (2) was prepared starting from D-proline. The amides were tested by methods of biochemical and behavioural pharmacology.

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2

Elliott, Simon. "Current awareness of piperazines: pharmacology and toxicology." Drug Testing and Analysis 3, no. 7-8 (2011): 430–38. http://dx.doi.org/10.1002/dta.307.

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3

Dolan, Sean B., Ritu A. Shetty, Michael J. Forster, and Michael B. Gatch. "Impure but not inactive: Behavioral pharmacology of dibenzylpiperazine, a common by-product of benzylpiperazine synthesis." Journal of Psychopharmacology 32, no. 7 (2018): 802–10. http://dx.doi.org/10.1177/0269881118780613.

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Background: Substituted piperazines comprise a substantial proportion of the novel psychoactive substance market. Among the most widely abused piperazine compounds are meta-chlorophenylpiperazine (mCPP), tri-fluoromethylphenylpiperazine (TFMPP), and, especially, benzylpiperazine (BZP), which are commonly incorporated, either alone or in combination, in illicit “party pills” or “ecstasy” formulations. Illicit synthesis of BZP often results in production of an impure by-product dibenzylpiperazine (DBZP), which frequently appears alongside BZP in these formulations; however, despite its ubiquity,

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4

Veselkina, O. S., I. L. Solovtsova, N. N. Petrishchev, et al. "Influence of N,N′-Substituted Piperazines on Cytolysis." Pharmaceutical Chemistry Journal 49, no. 11 (2016): 743–48. http://dx.doi.org/10.1007/s11094-016-1363-8.

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5

Popugaeva, Elena, Daria Chernyuk, Hua Zhang, et al. "Derivatives of Piperazines as Potential Therapeutic Agents for Alzheimer’s Disease." Molecular Pharmacology 95, no. 4 (2019): 337–48. http://dx.doi.org/10.1124/mol.118.114348.

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6

Klochkova, I. N., N. N. Semenova, A. A. Safonova, and M. V. Noritsina. "Search for potential cholinesterase inhibitors among substituted pyrrolidines and piperazines." Pharmaceutical Chemistry Journal 33, no. 12 (1999): 638–41. http://dx.doi.org/10.1007/bf02974938.

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7

Weigl, Manuela, та Bernhard Wünsch. "Synthesis of bridged piperazines with σ receptor affinity". European Journal of Medicinal Chemistry 42, № 10 (2007): 1247–62. http://dx.doi.org/10.1016/j.ejmech.2007.02.005.

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8

Kersten, Brian P., and Megan E. McLaughlin. "Toxicology and Management of Novel Psychoactive Drugs." Journal of Pharmacy Practice 28, no. 1 (2014): 50–65. http://dx.doi.org/10.1177/0897190014544814.

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Health care providers are seeing an increased number of patients under the influence of several new psychoactive drug classes. Synthetic cannabinoids, cathinones, and piperazines are sought by users for their psychoactive effects, perceived safety profile, minimal legal regulations, and lack of detection on routine urine drug screening. However, these drugs are beginning to be recognized by the medical community for their toxic effects. The neuropsychiatric and cardiovascular toxicities are among the most common reasons for emergency medical treatment, which in some cases, can be severe and ev

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9

Patel, Divyesh, Rahul Patel, Premlata Kumari, and Navin Patel. "In vitro antimicrobial assessment of coumarin-based s-triazinyl piperazines." Medicinal Chemistry Research 21, no. 8 (2011): 1611–24. http://dx.doi.org/10.1007/s00044-011-9676-3.

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10

Yurttaş, Leyla, Zafer Asım Kaplancıklı, and Yusuf Özkay. "Design, synthesis and evaluation of new thiazole-piperazines as acetylcholinesterase inhibitors." Journal of Enzyme Inhibition and Medicinal Chemistry 28, no. 5 (2012): 1040–47. http://dx.doi.org/10.3109/14756366.2012.709242.

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11

van der Zee, P., and W. Hespe. "Interaction between substituted 1-[2-(diphenylmethoxy)ethyl] piperazines and dopamine receptors." Neuropharmacology 24, no. 12 (1985): 1171–74. http://dx.doi.org/10.1016/0028-3908(85)90150-9.

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12

Soboleva, S. G., A. F. Galatin, T. L. Karaseva, A. V. Golturenko, and S. A. Andronati. "Synthesis and Pharmacological Properties of 1-Aryl-4-(3′4′,5′-trimethoxybenzoyl)piperazines." Pharmaceutical Chemistry Journal 39, no. 5 (2005): 236–38. http://dx.doi.org/10.1007/s11094-005-0124-x.

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13

Mokrov, G. V., A. M. Likhosherstov, V. V. Barchukov, et al. "Synthesis and Cardiotropic Activity of 1-(Methoxybenzyl)-4-{2-[(Methoxybenzyl)-Amino]Ethyl}Piperazines." Pharmaceutical Chemistry Journal 53, no. 9 (2019): 786–91. http://dx.doi.org/10.1007/s11094-019-02080-2.

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14

Caccia, S., I. Conti, A. Notarnicola, and R. Urso. "Lipophilicity and disposition of 1-aryl-piperazines in the rat." Xenobiotica 17, no. 5 (1987): 605–16. http://dx.doi.org/10.3109/00498258709043967.

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15

Slater, Lewis M., Gabriel F. Eilon, Jirong Gu, John W. Jacobs, and Kaoru Hara. "Tumor apoptosis induced by epoxide-containing piperazines, a new class of anti-cancer agents." Cancer Chemotherapy and Pharmacology 45, no. 3 (2000): 183–91. http://dx.doi.org/10.1007/s002800050028.

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16

Silvio Caccia. "N-Dealkylation of Arylpiperazine Derivatives: Disposition and Metabolism of the 1-Aryl-Piperazines Formed." Current Drug Metabolism 8, no. 6 (2007): 612–22. http://dx.doi.org/10.2174/138920007781368908.

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17

YAROSH, H., E. KATZ, A. COOP, and W. FANTEGROSSI. "MDMA-like behavioral effects of N-substituted piperazines in the mouse." Pharmacology Biochemistry and Behavior 88, no. 1 (2007): 18–27. http://dx.doi.org/10.1016/j.pbb.2007.06.007.

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18

Valluri, Kishore K., Tejeswara R. Allaka, IV Kasi Viswanath, and Nagaraju PVVS. "Synthesis and Antibacterial / Anticancer Activities of Compounds Containing Pyrazole Ring Linked to Piperazines." Current Bioactive Compounds 16, no. 4 (2020): 419–31. http://dx.doi.org/10.2174/1573407215666190111124513.

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Background: Many pyrazole piperazine derivatives are known to exhibit a wide range, thus being attractive for the drug design and synthesis of interesting class of widely studied heterocyclic compounds. It is therefore necessary to devote continuing effort for the identification and development of New Chemical Entities (NCEs) as potential antibacterial and anticancer agents to address serious health problems. Methods: A series of new compounds containing pyrazole ring linked to a piperazine hydrochloride moiety were synthesized and screened for their antibacterial activity, cytotoxicity of nov

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19

Angeli, Andrea, Niccolò Chiaramonte, Dina Manetti, Maria Novella Romanelli, and Claudiu T. Supuran. "Investigation of piperazines as human carbonic anhydrase I, II, IV and VII activators." Journal of Enzyme Inhibition and Medicinal Chemistry 33, no. 1 (2017): 303–8. http://dx.doi.org/10.1080/14756366.2017.1417277.

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20

Huang, Rong, Yao Sheng, Ding Wei, Jianghui Yu, Hongli Chen, and Biao Jiang. "Bis(vinylsulfonyl)piperazines as efficient linkers for highly homogeneous antibody-drug conjugates." European Journal of Medicinal Chemistry 190 (March 2020): 112080. http://dx.doi.org/10.1016/j.ejmech.2020.112080.

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21

Gupta, Sonal, Deepti Pandey, Dhanaraju Mandalapu, et al. "Novel aryl piperazines for alleviation of ‘andropause’ associated prostatic disorders and depression." European Journal of Medicinal Chemistry 132 (May 2017): 204–18. http://dx.doi.org/10.1016/j.ejmech.2017.03.036.

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22

Nguyen, William, Madeline G. Dans, Anna Ngo, et al. "Structure activity refinement of phenylsulfonyl piperazines as antimalarials that block erythrocytic invasion." European Journal of Medicinal Chemistry 214 (March 2021): 113253. http://dx.doi.org/10.1016/j.ejmech.2021.113253.

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23

Rudner-Varga, Vanda, Philip K. Ahring, Dinesh Indurthi та ін. "Exploring the structure activity relationships of halogen containing N-(pyridin-3-yl)-piperazines and homopiperazines at α4β2 nAChRs". Biochemical Pharmacology 97, № 4 (2015): 623. http://dx.doi.org/10.1016/j.bcp.2015.08.010.

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24

Schifano, Fabrizio. "Novel psychoactive substances (NPS): clinical and pharmacological issues." Drugs and Alcohol Today 15, no. 1 (2015): 21–27. http://dx.doi.org/10.1108/dat-10-2014-0035.

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Purpose – The purpose of this paper is to provide health professionals with novel psychoactive substances (NPS) clients with up to date information relating to the background, clinical pharmacology and, when possible, clinical management for each of these categories. Design/methodology/approach – The world of NPS is complex and diverse, including a range of different molecules such as: psychedelic phenethylamines; synthetic cannabinoids, cathinone derivatives; novel stimulants; synthetic opiates/opioids; tryptamine derivatives; phencyclidine-like dissociatives; piperazines; GABA-A/GABA-B recep

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25

Genaro-Mattos, Thiago C., Keri A. Tallman, Luke B. Allen, et al. "Dichlorophenyl piperazines, including a recently-approved atypical antipsychotic, are potent inhibitors of DHCR7, the last enzyme in cholesterol biosynthesis." Toxicology and Applied Pharmacology 349 (June 2018): 21–28. http://dx.doi.org/10.1016/j.taap.2018.04.029.

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26

Neganova, Margarita E., Sergey G. Klochkov, Sergey A. Pukhov, et al. "Synthesis and Cytotoxic Activity of Azine Derivatives of 6-Hydroxyxanthanodiene." Current Cancer Drug Targets 20, no. 9 (2020): 666–74. http://dx.doi.org/10.2174/1568009620999200421200338.

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Background: The conjugates of the sesquiterpene lactone of the eremophilane series of 6- hydroxyxanthanodiene with hydrogenated azines (piperidines and piperazines) have been synthesized and identified by NMR spectrometer. Objective: A lactone with an unusual skeleton “6-hydroxyxanthanodiene” was extracted from the plant Elecampane (Inula helenium L) and identified various species with NMR spectrometer. Methods: The cytotoxic, mitochondrial, and antioxidant activities on different tumor lines such as A549, HCT116, RD and Jurkat were investigated and determined possible mechanisms. Results: The

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27

Purohit, Deepika, Vandana Saini, Sanjiv Kumar, Ajit Kumar та Balasubramanian Narasimhan. "Three-dimensional Quantitative Structure-activity Relationship (3DQSAR) and Molecular Docking Study of 2-((pyridin-3-yloxy)methyl) Piperazines as α7 Nicotinic Acetylcholine Receptor Modulators for the Treatment of Inflammatory Disorders". Mini-Reviews in Medicinal Chemistry 20, № 11 (2020): 1031–41. http://dx.doi.org/10.2174/1389557519666190904151227.

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Background & Objective: Comparative molecular field analysis (CoMFA) of 27 analogues of 2-((pyridin-3-yloxy)methyl)piperazine derivatives was carried out using software Tripos SYBYL X. Optimal r2 (0.854) and q2 (0.541) values were obtained for the developed 3D-QSAR model. The contour plots obtained from CoMFA analysis have shown 13.84% steric contribution and 66.14% electrostatic contribution towards an anti-inflammatory activity. Methods: The homology model of the receptor protein, α7 nicotinic acetylcholine, was generated in SWISS MODELLER using auto template mode and was analysed for th

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28

CHEN, JIANHONG, AGRIPINA G. DEACIUC, LINDA P. DWOSKIN, PETER A. CROOKS та DONGLU BAI. "N, N –Disubstituted piperazines and homopiperazines: Synthesis and affinities at α4β2* and α7* neuronal nicotinic acetylcholine receptors". Journal of Enzyme Inhibition and Medicinal Chemistry 21, № 6 (2006): 667–80. http://dx.doi.org/10.1080/14756360600900513.

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29

Kortagere, Sandhya, Peter Gmeiner, Harel Weinstein, and John A. Schetz. "Certain 1,4-Disubstituted Aromatic Piperidines and Piperazines with Extreme Selectivity for the Dopamine D4 Receptor Interact with a Common Receptor Microdomain." Molecular Pharmacology 66, no. 6 (2004): 1491–99. http://dx.doi.org/10.1124/mol.104.001321.

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30

Al-Soud, Yaseen, Najim Al-Masoudi, Hamed Hassan, Erik De Clercq, and Christophe Pannecouque. "Nitroimidazoles. V. Synthesis and anti-HIV evaluation of new 5-substituted piperazinyl-4-nitroimidazole derivatives." Acta Pharmaceutica 57, no. 4 (2007): 379–93. http://dx.doi.org/10.2478/v10007-007-0031-7.

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Nitroimidazoles. V. Synthesis and anti-HIV evaluation of new 5-substituted piperazinyl-4-nitroimidazole derivativesA series of 2-alkylthio-1-[4-(1-benzyl-2-ethyl-4-nitro-1H- -imidazol-5-yl)-piperazin-1-y]lethanones (3-9) and alkyl- [4-(1-benzyl-2-ethyl-4-nitro-1H-imidazol-5-yl)-piperazin- -1-yl)ketones (11-20) as well as the indole analogue22were synthesized from 4-nitro-5-piperazinyl imidazole derivative1, with the aim to develop newly non-nucleoside reverse transcriptase inhibitors (NNRTIs). The newly synthesized compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. Compound2showed i

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31

Gaur, Stuti, Philip Prathipati, Mridula Saxena, and Anil K. Saxena. "CoMFA AND CoMSIA STUDIES ON A SET OF BENZYL PIPERAZINES, PIPERADINES, PYRAZINOPYRIDOINDOLES, PYRAZINOISOQUINOLINES AND SEMI RIGID ANALOGS OF DIPHENHYDRAMINE." Medicinal Chemistry Research 13, no. 8-9 (2004): 746–57. http://dx.doi.org/10.1007/s00044-004-0114-7.

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32

Xu, Hui. "Progress of Bis(heteroaryl)piperazines (BHAPs) as Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs) against Human Immunodeficiency Virus Type 1 (HIV-1)." Mini-Reviews in Medicinal Chemistry 10, no. 1 (2010): 62–72. http://dx.doi.org/10.2174/138955710791112578.

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33

Mizuki, Y., I. Fujiwara, T. Yamaguchi, and Y. Sekine. "Structure-related inhibitory effect of antimicrobial enoxacin and derivatives on theophylline metabolism by rat liver microsomes." Antimicrobial Agents and Chemotherapy 40, no. 8 (1996): 1875–80. http://dx.doi.org/10.1128/aac.40.8.1875.

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Enoxacin, an antimicrobial fluoroquinolone with a 7-piperazinyl-1, 8-naphthyridine skeleton, is a potent inhibitor of cytochrome P-450-mediated theophylline metabolism. The present study was designed to clarify, using seven enoxacin derivatives, the molecular characteristics of the fluoroquinolone responsible for the inhibition. Three derivatives with methyl-substituted 7-piperazine rings inhibited rat liver microsomal theophylline metabolism to 1,3-dimethyluric acid to an extent similar to that of enoxacin (50% inhibitory concentrations [IC50s] = 0.39 to 0.48 mM). 7-Piperazinyl-quinoline deri

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34

Patel, Rahul V., Amit B. Patel, Premlata Kumari, and Kishor H. Chikhalia. "Synthesis of novel 3-(5-sulfanyl-1,3,4-oxadiazol-2-yl)-2H-chromen-2-one condensed s-triazinyl piperazines and piperidines as antimicrobial agents." Medicinal Chemistry Research 21, no. 10 (2011): 3119–32. http://dx.doi.org/10.1007/s00044-011-9842-7.

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35

Mohamed, Osama G., Angela A. Salim, Zeinab G. Khalil, Ahmed H. Elbanna, Paul V. Bernhardt, and Robert J. Capon. "Chrysosporazines F–M: P-Glycoprotein Inhibitory Phenylpropanoid Piperazines from an Australian Marine Fish Derived Fungus, Chrysosporium sp. CMB-F294." Journal of Natural Products 83, no. 2 (2020): 497–504. http://dx.doi.org/10.1021/acs.jnatprod.9b01181.

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36

Elbanna, Ahmed H., Amila Agampodi Dewa, Zeinab G. Khalil, and Robert J. Capon. "Precursor-Directed Biosynthesis Mediated Amplification of Minor Aza Phenylpropanoid Piperazines in an Australian Marine Fish-Gut-Derived Fungus, Chrysosporium sp. CMB-F214." Marine Drugs 19, no. 9 (2021): 478. http://dx.doi.org/10.3390/md19090478.

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Chemical analysis of an M1 agar plate cultivation of a marine fish-gut-derived fungus, Chrysosporium sp. CMB-F214, revealed the known chrysosporazines A–D (11–14) in addition to a suite of very minor aza analogues 1–6. A microbioreactor (MATRIX) cultivation profiling analysis failed to deliver cultivation conditions that significantly improved the yields of 1–6; however, it did reveal that M2 agar cultivation produced the new natural product 15. A precursor-directed biosynthesis strategy adopting supplementation of a CMB-F214 M1 solid agar culture with sodium nicotinate enhanced production of

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37

Devine, R., M. Kelada, S. Leonard, et al. "Design, synthesis, and biological evaluation of aryl piperazines with potential as antidiabetic agents via the stimulation of glucose uptake and inhibition of NADH:ubiquinone oxidoreductase." European Journal of Medicinal Chemistry 202 (September 2020): 112416. http://dx.doi.org/10.1016/j.ejmech.2020.112416.

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38

Jadala, Chetna, Manda Sathish, Pratibha Anchi, et al. "Synthesis of Combretastatin‐A4 Carboxamidest that Mimic Sulfonyl Piperazines by a Molecular Hybridization Approach: in vitro Cytotoxicity Evaluation and Inhibition of Tubulin Polymerization." ChemMedChem 14, no. 24 (2019): 2052–60. http://dx.doi.org/10.1002/cmdc.201900541.

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39

Bindu, B., S. Vijayalakshmi, and A. Manikandan. "Synthesis and discovery of triazolo-pyridazine-6-yl-substituted piperazines as effective anti-diabetic drugs; evaluated over dipeptidyl peptidase-4 inhibition mechanism and insulinotropic activities." European Journal of Medicinal Chemistry 187 (February 2020): 111912. http://dx.doi.org/10.1016/j.ejmech.2019.111912.

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40

Wenceslau, João P. S., Dávila F. de Souza, Maria C. F. de Oliveira, et al. "Novel Lapachol Derivatives and Their Antioxidant Activity." Natural Product Communications 1, no. 8 (2006): 1934578X0600100. http://dx.doi.org/10.1177/1934578x0600100812.

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A convenient synthesis of the new enamine derivatives 2-diethylamino-3-(3-methyl-2-butenyl)-1,4-naphthalenedione (2), 2-ethylamino-3-(3-methyl-2-butenyl)-1,4-naphthalenedione (3), 2-diethanolamino-3-(3-methyl-2-butenyl)-1,4-naphthalenedione (4), and 2-(1-piperazinyl)-3-(3-methyl-2-butenyl)-1,4-naphthalenedione (5) was carried out from natural 2-hydroxy-3-(3-methyl-2-butenyl)-1,4-naphtalenedione (lapachol, 1) and diethylamine, ethylamine, diethanolamine and piperazine, respectively. All products were fully characterized by IR, 1H and 13C NMR spectroscopy. Results revealed no antioxidant behavio

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41

Valenta, Vladimír, Zdeněk Prošek, Jiřina Metyšová, Martin Valchář, Antonín Dlabač, and Miroslav Protiva. "Cataleptic and noncataleptic neuroleptic agents: Synthesis and pharmacology of 4-(2-chloro and 8-chloro substituted 10,11-dihydrodibenzo[b,f]thiepin-10-yl)piperazine-1-ylalkyl ethers and sulfides." Collection of Czechoslovak Chemical Communications 50, no. 5 (1985): 1070–77. http://dx.doi.org/10.1135/cccc19851070.

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The title compounds Iab-Viab were prepared by substitution reactions of 2,11-dichloro- and 2,10-dichloro-10,11-dihydrodibenzo[b,f]thiepin with 1-(2-methoxyethyl)piperazine, 1-(3-methoxypropyl)piperazine, 1-(2-ethoxyethyl)piperazine, 1-(2-phenoxyethyl)piperazine, 1-(2-methylthioethyl)piperazine and 1-(2-phenylthioethyl)piperazine; they were transformed to hydrochlorides, maleates or methanesulfonates. Compounds of series a (8-chloro derivatives) are neuroleptics, with relatively strong cataleptic, antiapomorphine and central depressant activities (Ia, IIa, IIIa,Va) unless the volume and lipophi

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42

Laïos, Ioanna, Anny Cleeren, Guy Leclercq, et al. "Effects of (R,S)/(S,R)-4,5-bis(2-chloro-4-hydroxyphenyl)-2-imidazolines and (R,S)/(S,R)-2,3-bis(2-chloro-4-hydroxyphenyl)piperazines on estrogen receptor alpha level and transcriptional activity in MCF-7 cells." Biochemical Pharmacology 74, no. 7 (2007): 1029–38. http://dx.doi.org/10.1016/j.bcp.2007.06.045.

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43

Ghasi, Samuel, and Obiageli Odurukwe. "The Effects of Sub-chronic Piperazine Treatment on the Liver Status of a Rat Model." Pharmacologia 2, no. 9 (2011): 259–64. http://dx.doi.org/10.5567/pharmacologia.2011.259.264.

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44

Abate, Carmen, Mauro Niso, Marialessandra Contino та ін. "Inside Cover: 1-Cyclohexyl-4-(4-arylcyclohexyl)piperazines: Mixed σ and Human Δ8-Δ7 Sterol Isomerase Ligands with Antiproliferative and P-Glycoprotein Inhibitory Activity (ChemMedChem 1/2011)". ChemMedChem 6, № 1 (2010): 2. http://dx.doi.org/10.1002/cmdc.201090062.

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45

Ghasi, S., O. Odurukwe, and S. Ufelle. "Appraisal of the Kidney Status of the Rat Model to Sub-acute Treatment with Piperazine Citrate." Pharmacologia 3, no. 8 (2012): 306–12. http://dx.doi.org/10.5567/pharmacologia.2012.306.312.

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46

Sharma, Anjali, Sharad Wakode, Faizana Fayaz, Shaik Khasimbi, Faheem H. Pottoo, and Avneet Kaur. "An Overview of Piperazine Scaffold as Promising Nucleus for Different Therapeutic Targets." Current Pharmaceutical Design 26, no. 35 (2020): 4373–85. http://dx.doi.org/10.2174/1381612826666200417154810.

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Piperazine scaffolds are a group of heterocyclic atoms having pharmacological values and showing significant results in pharmaceutical chemistry. Piperazine has a flexible core structure for the design and synthesis of new bioactive compounds. These flexible heterogenous compounds exhibit various biological roles, primarily anticancer, antioxidant, cognition enhancers, antimicrobial, antibacterial, antiviral, antifungal, antiinflammatory, anti-HIV-1 inhibitors, antidiabetic, antimalarial, antidepressant, antianxiety and anticonvulsant activities, etc. In the past few years, researchers focused

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47

Mooney, R. D., M. Y. Shi, and R. W. Rhoades. "Modulation of retinotectal transmission by presynaptic 5-HT1B receptors in the superior colliculus of the adult hamster." Journal of Neurophysiology 72, no. 1 (1994): 3–13. http://dx.doi.org/10.1152/jn.1994.72.1.3.

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1. Radioligand binding with [125I] -cyanopindolol in the presence of isoproterenol was used to define the distribution of 5 -HT1B receptors in the superior colliculus (SC) of adult hamsters. There was a high density of these receptors in the stratum griseum superficiale (SGS), and they were much less dense in other SC laminae. Enucleation of one eye produced a marked reduction in the density of these receptors in the contralateral SGS, suggesting that they are located primarily on retinotectal axon terminals. 2. Intracellular recording techniques were used to evaluate the effects of serotonin

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48

Martin, R. J., M. A. Valkanov, V. M. E. Dale, A. P. Robertson, and I. Murray. "Electrophysiology ofAscarismuscle and anti-nematodal drug action." Parasitology 113, S1 (1996): S137—S156. http://dx.doi.org/10.1017/s0031182000077945.

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SUMMARYThree groups of anthelmintic drugs act directly and selectively on muscle membrane receptors of parasitic nematodes. These groups of anthelmintics are: (1)The Nicotinic Agonists(levamisole, pyrantel, morantel and oxantel) that act on acetylcholine receptors of nematode somatic muscle; (2)The GAB A Agonist, piperazine, that acts on nematode muscle GABA receptors; and (3)The Avermectinsthat open glutamate gated Cl-channels on nematode pharyngeal muscle. The electrophysiology and pharmacology of muscle and neuromuscular transmission the nematode parasite,Ascaris suum, is outlined and effec

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Szczepanska, Katarzyna, Kamil Kuder, and Katarzyna Kiec-Kononowicz. "Histamine H3 Receptor Ligands in the Group of (Homo)piperazine Derivatives." Current Medicinal Chemistry 25, no. 14 (2018): 1609–26. http://dx.doi.org/10.2174/0929867325666171123203550.

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Since its discovery in 1983, followed by gene cloning in 1999, the histamine H3 receptor served as an outstanding target for drug discovery. The wide spectrum of possible therapeutic implications makes H3R's one of the most researched areas in the vast GPCR ligands field - started from imidazole containing ligands, through various successful imidazole replacements, with recent introduction of Wakix® to pharmaceutical market. One such replacement is piperazine moiety, a significant versatile scaffold in rational drug design for most of the GPCR ligands. Therefore, herein, we review ligands buil

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Morris, Julia E., Xiao-Su Pan, and L. Mark Fisher. "Grepafloxacin, a Dimethyl Derivative of Ciprofloxacin, Acts Preferentially through Gyrase in Streptococcus pneumoniae: Role of the C-5 Group in Target Specificity." Antimicrobial Agents and Chemotherapy 46, no. 2 (2002): 582–85. http://dx.doi.org/10.1128/aac.46.2.582-585.2002.

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ABSTRACT Grepafloxacin, a 5-methyl-7-piperazinyl-3"-methyl analogue of ciprofloxacin, was used to obtain stepwise-selected mutants of Streptococcus pneumoniae 7785. Analysis of the quinolone resistance-determining regions of the gyrA, gyrB, parC, and parE genes in these mutants revealed that gyrA mutations preceded those in parC. Given that ciprofloxacin (5-H,7-piperazinyl) and AM-1121 (5-H,7-piperazinyl-3"-methyl) both act through topoisomerase IV, we conclude that the 5-methyl group of grepafloxacin favors gyrase in S. pneumoniae.

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