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Journal articles on the topic 'Histamine receptor antagonism'

Author: Grafiati

Published: 7 June 2025

Last updated: 2 August 2025

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1

Neely, C. F., I. Matot, D. Haile, J. Nguyen, and V. Batra. "Tone-dependent responses of histamine in feline pulmonary vascular bed." American Journal of Physiology-Heart and Circulatory Physiology 268, no. 2 (1995): H653—H661. http://dx.doi.org/10.1152/ajpheart.1995.268.2.h653.

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Under conditions of controlled pulmonary blood flow and constant left atrial pressure, histamine produced tone-dependent responses in the pulmonary vascular (PV) bed of intact-chest, spontaneously breathing cats. At low, baseline PV tone, histamine produced dose-dependent increases in mean lobar arterial pressure that were antagonized by the selective histamine H1-receptor antagonist, diphenhydramine. The cyclooxygenase inhibitor, meclofenamate, and the thromboxane A2 (TxA2) receptor antagonist, SQ-29548, had no effect on these vasoconstrictor responses of histamine. After an increase in PV to

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2

Mocking, Tamara A. M., Maurice C. M. L. Buzink, Rob Leurs, and Henry F. Vischer. "Bioluminescence Resonance Energy Transfer Based G Protein-Activation Assay to Probe Duration of Antagonism at the Histamine H3 Receptor." International Journal of Molecular Sciences 20, no. 15 (2019): 3724. http://dx.doi.org/10.3390/ijms20153724.

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Duration of receptor antagonism, measured as the recovery of agonist responsiveness, is gaining attention as a method to evaluate the ‘effective’ target-residence for antagonists. These functional assays might be a good alternative for kinetic binding assays in competition with radiolabeled or fluorescent ligands, as they are performed on intact cells and better reflect consequences of dynamic cellular processes on duration of receptor antagonism. Here, we used a bioluminescence resonance energy transfer (BRET)-based assay that monitors heterotrimeric G protein activation via scavenging of rel

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Leth, R., B. Elander, U. Haglund, L. Olbe, and E. Fellenius. "Histamine H2-receptor of human and rabbit parietal cells." American Journal of Physiology-Gastrointestinal and Liver Physiology 253, no. 4 (1987): G497—G501. http://dx.doi.org/10.1152/ajpgi.1987.253.4.g497.

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The histamine H2-receptor on the human parietal cell has been characterized by using dose-response curves and the negative logarithm of the molar concentration of an antagonist (pA2) analyses of cimetidine antagonism of betazole, histamine, and impromidine stimulation in isolated human and rabbit gastric glands. To evaluate the in vitro results, betazole-stimulated gastric acid secretion with and without cimetidine was also studied in healthy subjects. In the in vivo model, individual dose-response curves were shifted to the right with increasing cimetidine concentrations, but this was counter

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4

Miller, Thomas R., David G. Witte, Lynne M. Ireland, et al. "Analysis of Apparent Noncompetitive Responses to Competitive H1-Histamine Receptor Antagonists in Fluorescent Imaging Plate Reader-Based Calcium Assays." Journal of Biomolecular Screening 4, no. 5 (1999): 249–58. http://dx.doi.org/10.1177/108705719900400506.

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We have examined the utility of high throughput fluorescent imaging plate reader (FLIPR)-based calcium assays for pharmacological characterization of G-protein coupled receptors (GPCRs) using recombinant and native human H1-histamine receptors (H1-HR), expressed in HEK293 and HeLa S3 cells, respectively, as model systems. For stably transfected HEK293 cell lines, the potency of histamine for elevating intracellular calcium increased (pD2, 7.13 and 7.86) with increased H1-HR density (about 0.8 and 14 pmol/mg protein, respectively), though histamine binding affinities were similar. The classic H

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Pfanzagl, Beatrix, Roswitha Pfragner, and Erika Jensen-Jarolim. "The Transient Receptor Potential Vanilloid 4 Agonist RN-1747 Inhibits the Calcium Response to Histamine." Pharmacology 104, no. 3-4 (2019): 166–72. http://dx.doi.org/10.1159/000501144.

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Background: Sensitization of transient receptor potential (TRP) cation channels probably contributes to intestinal hypersensitivity, a hallmark of gastrointestinal disorders. Histamine acting via histamine 1 receptor (H1R) to open TRP cation channels might also be involved. Method: The enterochromaffin cell line P-STS, responsive to histamine via H1R, was used as model to study possible synergism between histamine and TRP vanilloid 4 (TRPV4) pathways. Results: The TRPV4 antagonist RN-1734, but not HC-067047, inhibited the cytoplasmic calcium response to histamine in P-STS cells. However, also

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Balemans, D., J. Aguilera-Lizarraga, M. V. Florens, et al. "Histamine-mediated potentiation of transient receptor potential (TRP) ankyrin 1 and TRP vanilloid 4 signaling in submucosal neurons in patients with irritable bowel syndrome." American Journal of Physiology-Gastrointestinal and Liver Physiology 316, no. 3 (2019): G338—G349. http://dx.doi.org/10.1152/ajpgi.00116.2018.

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Previously, we showed histamine-mediated sensitization of transient receptor potential (TRP) vanilloid 1 (TRPV1) in patients with irritable bowel syndrome (IBS). Sensitization of TRP ankyrin 1 (TRPA1) and TRP vanilloid 4 (TRPV4) are also involved in aberrant pain perception in preclinical models of somatic pain. Here, we hypothesize that in parallel with TRPV1, histamine sensitizes TRPA1 and TRPV4, contributing to increased visceral pain in patients with IBS. Rectal biopsies were collected from patients with IBS and healthy subjects (HS) to study neuronal sensitivity to TRPA1 and TRPV4 agonist

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Aihara, Takeshi, Yusuke Nakamura, Makoto M. Taketo, Minoru Matsui, and Susumu Okabe. "Cholinergically stimulated gastric acid secretion is mediated by M3 and M5 but not M1 muscarinic acetylcholine receptors in mice." American Journal of Physiology-Gastrointestinal and Liver Physiology 288, no. 6 (2005): G1199—G1207. http://dx.doi.org/10.1152/ajpgi.00514.2004.

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Muscarinic acetylcholine receptors play an important role in the regulation of gastric acid secretion stimulated by acetylcholine; nonetheless, the precise role of each receptor subtype (M1–M5) remains unclear. This study examined the involvement of M1, M3, and M5 receptors in cholinergic regulation of acid secretion using muscarinic receptor knockout (KO) mice. Gastric acid secretion was measured in both mice subjected to acute gastric fistula production under urethane anesthesia and conscious mice that had previously undergone pylorus ligation. M3 KO mice exhibited impaired gastric acid secr

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8

Black, James. "Drugs from emasculated hormones: The principle of syntopic antagonism." Bioscience Reports 9, no. 3 (1989): 253–72. http://dx.doi.org/10.1007/bf01114681.

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9

Black, James. "Drugs from Emasculated Hormones: The Principle of Syntopic Antagonism." Bioscience Reports 24, no. 4-5 (2004): 302–22. http://dx.doi.org/10.1007/s10540-005-2736-5.

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10

DiBaise, J. K. "Nocturnal acid breakthrough and histamine-2 receptor antagonism." American Journal of Gastroenterology 97, no. 7 (2002): 1595. http://dx.doi.org/10.1111/j.1572-0241.2002.05890.x.

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11

Vande Griend, Joseph P., and Sarah L. Anderson. "Histamine-1 receptor antagonism for treatment of insomnia." Journal of the American Pharmacists Association 52, no. 6 (2012): e210-e219. http://dx.doi.org/10.1331/japha.2012.12051.

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12

Toda, N. "Mechanism underlying responses to histamine of isolated monkey and human cerebral arteries." American Journal of Physiology-Heart and Circulatory Physiology 258, no. 2 (1990): H311—H317. http://dx.doi.org/10.1152/ajpheart.1990.258.2.h311.

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Cerebral artery strips obtained from Japanese monkeys partially contracted with prostaglandin F2 alpha responded to histamine with a relaxation that was attenuated by treatment with cimetidine or chlorpheniramine and was abolished by their combined treatment. Endothelium denudation suppressed the relaxation; the remaining relaxation was not influenced by the H1 antagonism but was abolished by the H2 antagonism. Treatment with methylene blue slowed the development of relaxation and, in the presence of cimetidine, depressed the magnitude of relaxation. Indomethacin did not alter the response. In

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13

Ely, Matthew R., Stephen M. Ratchford, D. Taylor La Salle, Joel D. Trinity, D. Walter Wray, and John R. Halliwill. "Effect of histamine-receptor antagonism on leg blood flow during exercise." Journal of Applied Physiology 128, no. 6 (2020): 1626–34. http://dx.doi.org/10.1152/japplphysiol.00689.2019.

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Leg blood flow during exercise was increased by taking antihistamines, which block the receptors for histamine, a molecule often associated with inflammatory and immune responses. The elevated blood flow occurred over exercise intensities ranging from 20 to 80% of peak capacity and during exercise of 60-min duration. These results suggest that exercise-induced elevations in histamine concentrations are involved in novel, poorly understood, and perhaps complex ways in the exercise response.

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Jooste, Edmund, Yi Zhang, and Charles W. Emala. "Rapacuronium Preferentially Antagonizes the Function of M2 versus M3 Muscarinic Receptors in Guinea Pig Airway Smooth Muscle." Anesthesiology 102, no. 1 (2005): 117–24. http://dx.doi.org/10.1097/00000542-200501000-00020.

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Background Rapacuronium, a nondepolarizing muscle relaxant that was proposed as a replacement for succinylcholine for rapid intubation, was withdrawn from clinical use as a result of fatal bronchospasm, but the mechanism of this effect is not known. Preferential antagonism of presynaptic M2 muscarinic receptors versus postsynpatic M3 muscarinic receptors can facilitate bronchoconstriction. The authors questioned whether rapacuronium preferentially antagonized M2 versus M3 muscarinic receptors in intact airway. Methods Guinea pig tracheal rings were suspended in organ baths and muscle relaxants

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15

Mogilski, Szczepan, Monika Kubacka, Artur Świerczek, et al. "Efficacy of the Multi-Target Compound E153 in Relieving Pain and Pruritus of Different Origins." Pharmaceuticals 16, no. 10 (2023): 1481. http://dx.doi.org/10.3390/ph16101481.

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Itch and pain are closely related but distinct sensations that share largely overlapping mediators and receptors. We hypothesized that the novel, multi-target compound E153 has the potential to attenuate pain and pruritus of different origins. After the evaluation of sigma receptor affinity and pharmacokinetic studies, we tested the compound using different procedures and models of pain and pruritus. Additionally, we used pharmacological tools, such as PRE-084, RAMH, JNJ 5207852, and S1RA, to precisely determine the role of histamine H3 and sigma 1 receptors in the analgesic and antipruritic e

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16

Kotlikoff, M. I., R. K. Murray, and E. E. Reynolds. "Histamine-induced calcium release and phorbol antagonism in cultured airway smooth muscle cells." American Journal of Physiology-Cell Physiology 253, no. 4 (1987): C561—C566. http://dx.doi.org/10.1152/ajpcell.1987.253.4.c561.

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Primary cultures of airway smooth muscle cells were exposed to histamine, and intracellular free calcium transients were measured by the calcium-sensitive dye fura-2. Stimulation with 100 microM histamine resulted in a rise in intracellular calcium from an unstimulated level of 178 +/- 25 to 497 +/- 154 nM Ca2+ (SE; n = 14) and a return to base-line free calcium concentration within 1 min of stimulation. Pretreatment of cells with the H1 receptor blocker pyrilamine (2.5 microM) abolished the response; however, the calcium transient was not altered by pretreatment with the H2 blocker cimetidine

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17

Rossbach, K., K. Wahle, G. Bruer, et al. "Histamine 2 Receptor Agonism and Histamine 4 Receptor Antagonism Ameliorate Inflammation in a Model of Psoriasis." Acta Dermato Venereologica 100, no. 19 (2020): adv00342. http://dx.doi.org/10.2340/00015555-3674.

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18

Orsetti, M., P. Ghi, and A. Di Stilo. "1,2,5-Thiadiazole-S-oxide derivatives: histamine H2-receptor antagonism." European Journal of Pharmacology 183, no. 5 (1990): 1734–35. http://dx.doi.org/10.1016/0014-2999(90)92039-l.

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19

WOOD-BAKER, R., L. LAU, and P. H. HOWARTH. "Histamine and the nasal vasculature: the influence of H1and H2-histamine receptor antagonism." Clinical Otolaryngology 21, no. 4 (1996): 348–52. http://dx.doi.org/10.1111/j.1365-2273.1996.tb01085.x.

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20

Canning, Brendan J., Sandra M. Reynolds, and Stuart B. Mazzone. "Multiple mechanisms of reflex bronchospasm in guinea pigs." Journal of Applied Physiology 91, no. 6 (2001): 2642–53. http://dx.doi.org/10.1152/jappl.2001.91.6.2642.

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The mechanisms of histamine- and bradykinin-induced reflex bronchospasm were determined in anesthetized guinea pigs. With intravenous administration, both autacoids evoked dose-dependent increases in tracheal cholinergic tone. Vagotomy or atropine prevented these tracheal reflexes. When delivered as an aerosol, bradykinin readily increased tracheal cholinergic tone, whereas histamine aerosols were much less effective at inducing tracheal reflexes. Also, unlike histamine, bradykinin could evoke profound increases in cholinergic tone without directly or indirectly (e.g., prostanoid dependent) in

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21

Jucaite, Aurelija, Akihiro Takano, Emma Boström, et al. "AZD5213: a novel histamine H3 receptor antagonist permitting high daytime and low nocturnal H3 receptor occupancy, a PET study in human subjects." International Journal of Neuropsychopharmacology 16, no. 6 (2013): 1231–39. http://dx.doi.org/10.1017/s1461145712001411.

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AbstractThe histamine H3 receptor represents an appealing central nervous system drug target due to its important role in the neurobiology of cognition and wake-sleep regulation. The therapeutic benefit of H3 antagonists/inverse agonists may be hampered by disruption of sleep that has been observed in humans with prolonged high H3 receptor occupancy (H3RO), extending into night-time. AZD5213 is a highly selective H3 antagonist (in vitro inverse agonist) developed to achieve a pharmacokinetic profile permitting circadian fluctuations of H3RO. Its efficacy has been demonstrated in rodent behavio

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22

Skefos, Jerry, Melissa Ghulam, Arjun Mahendra, et al. "Histamine and acetylcholine receptor involvement in sensorimotor gating: an autoradiography study." F1000Research 3 (June 26, 2014): 136. http://dx.doi.org/10.12688/f1000research.4287.1.

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Sensory gating is a way by which the brain manages sensory information flow. For optimal allocation of neural resources, it is important to be able to screen out (or “gate”) irrelevant sensory information when another stimulus is being processed. Sensorimotor gating more generally refers to the overall process of modulation of the motor responses to sensory stimuli. Impaired sensorimotor gating is seen in a variety of neurobehavioral disorders including schizophrenia, autism and sensory processing disorder. The degree of sensorimotor gating can be studied behaviorally by indexing prepulse inhi

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23

Nault, Michael A., Brian Milne, and Joel L. Parlow. "Effects of the Selective H1and H2Histamine Receptor Antagonists Loratadine and Ranitidine on Autonomic Control of the Heart." Anesthesiology 96, no. 2 (2002): 336–41. http://dx.doi.org/10.1097/00000542-200202000-00018.

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Background H1 and H2 histamine receptor subtypes are present throughout the heart and may be involved in disturbances of cardiac rhythm that occur during anaphylaxis. Although H1 and H2 receptor antagonists are used in the treatment of anaphylaxis, there have been reports implicating these drugs in the genesis of dysrhythmias. This study was designed to investigate the effects of the selective H1 and H2 receptor antagonists loratadine and ranitidine on physiologic autonomic control of the healthy cardiovascular system. Methods Using a double-blind, crossover design, 14 healthy volunteers compl

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Reynolds, Gavin P. "Receptor mechanisms of antipsychotic drug action in bipolar disorder – focus on asenapine." Therapeutic Advances in Psychopharmacology 1, no. 6 (2011): 197–204. http://dx.doi.org/10.1177/2045125311430112.

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The atypical antipsychotic drugs are considered a first-line treatment for mania in bipolar disorder with many having a proven superiority to the classical mood stabilisers. This review addresses the pharmacological mechanisms underlying this therapeutic efficacy, as well as those mechanisms considered responsible for the adverse effects of antipsychotic drugs, with a particular focus on the recently introduced asenapine. The high efficacy in bipolar mania of haloperidol, a relatively selective dopamine D2-like receptor antagonist, indicates that the one common receptor mechanism underlying an

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Van Hoecke, Helen, Liesbet Vandenbulcke, and Paul Van Cauwenberge. "Histamine and Leukotriene Receptor Antagonism in the Treatment of Allergic Rhinitis." Drugs 67, no. 18 (2007): 2717–26. http://dx.doi.org/10.2165/00003495-200767180-00006.

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HOWARTH, P. H. "Histamine and asthma: an appraisal based on specific H1-receptor antagonism." Clinical Experimental Allergy 20, s2 (1990): 31–41. http://dx.doi.org/10.1111/j.1365-2222.1990.tb02459.x.

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MILLER, NORMAN S., DONALD W. GOODWIN, FOWLER C. JONES, et al. "Histamine Receptor Antagonism of Intolerance to Alcohol in the Oriental Population." Journal of Nervous and Mental Disease 175, no. 11 (1987): 661–67. http://dx.doi.org/10.1097/00005053-198711000-00003.

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Reynolds, Gavin P., and Olga O. McGowan. "Mechanisms underlying metabolic disturbances associated with psychosis and antipsychotic drug treatment." Journal of Psychopharmacology 31, no. 11 (2017): 1430–36. http://dx.doi.org/10.1177/0269881117722987.

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The increase in cardiovascular disease and reduced life expectancy in schizophrenia likely relate to an increased prevalence of metabolic disturbances. Such metabolic risk factors in schizophrenia may result from both symptom-related effects and aetiological factors. However, a major contributory factor is that of treatment with antipsychotic drugs. These drugs differ in effects on body weight; the underlying mechanisms are not fully understood and may vary between drugs, but may include actions at receptors associated with the hypothalamic control of food intake. Evidence supports 5-hydroxytr

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Saheera, Sherin, Ajay G. Potnuri, and Renuka Nair. "Histamine-2 receptor antagonist famotidine modulates cardiac stem cell characteristics in hypertensive heart disease." PeerJ 5 (October 9, 2017): e3882. http://dx.doi.org/10.7717/peerj.3882.

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Background Cardiac stem cells (CSCs) play a vital role in cardiac homeostasis. A decrease in the efficiency of cardiac stem cells is speculated in various cardiac abnormalities. The maintenance of a healthy stem cell population is essential for the prevention of adverse cardiac remodeling leading to cardiac failure. Famotidine, a histamine-2 receptor antagonist, is currently used to treat ulcers of the stomach and intestines. In repurposing the use of the drug, reduction of cardiac hypertrophy and improvement in cardiac function of spontaneously hypertensive rats (SHR) was reported by our grou

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Stahl, Stephen M. "Selective Histamine H1 Antagonism: Novel Hypnotic and Pharmacologic Actions Challenge Classical Notions of Antihistamines." CNS Spectrums 13, no. 12 (2008): 1027–38. http://dx.doi.org/10.1017/s1092852900017089.

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Numerous “antihistamines” as well as various psychotropic medications with antihistamine properties are widely utilized to treat insomnia. Over-the-counter sleep aids usually contain an antihistamine and various antidepressants and antipsychotics with antihistamine properties have sedative-hypnotic actions. Although widely used for the treatment of insomnia, many agents that block the histamine H1 receptor are also widely considered to have therapeutic limitations, including the development of next-day carryover sedation, as well as problems with chronic use, such as the development of toleran

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Saxena, M., S. S. Bhunia, and A. K. Saxena. "Molecular modelling studies on 2-substituted octahydropyrazinopyridoindoles for histamine H2 receptor antagonism." SAR and QSAR in Environmental Research 26, no. 7-9 (2015): 739–55. http://dx.doi.org/10.1080/1062936x.2015.1088572.

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Sieck, Dylan Charles, Joshua E. Mangum, Matthew R. Ely, et al. "Effect of Histamine‐receptor Antagonism on VO 2Peak Improvements to Exercise Training." FASEB Journal 34, S1 (2020): 1. http://dx.doi.org/10.1096/fasebj.2020.34.s1.09568.

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Ghizzardi, Paola, Thomas Gobbetti, Simona Bertoni, et al. "M1627 Histamine H4 Receptor Antagonism and Mesenteric Ischemia/Reperfusion Injury in Mice." Gastroenterology 136, no. 5 (2009): A—397. http://dx.doi.org/10.1016/s0016-5085(09)61826-6.

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Chen, M., and L. A. Brown. "Histamine stimulation of surfactant secretion from rat type II pneumocytes." American Journal of Physiology-Lung Cellular and Molecular Physiology 258, no. 4 (1990): L195—L200. http://dx.doi.org/10.1152/ajplung.1990.258.4.l195.

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The present study examined the effect of histamine on the secretion of phosphatidylcholine, the predominant component of pulmonary surfactant from adult rat alveolar type II pneumocytes in primary culture. Histamine stimulated surfactant secretion in a time- and dose-dependent manner. At a concentration of 10 microM, histamine stimulated surfactant release by 5.2-fold over the basal secretory rate. The concentration producing half the maximal response for histamine-induced secretion was 70 nM. Histamine-induced secretion was blocked by both the selective histamine1 receptor antagonist pyrilami

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Wittbrodt, Eric T., and Sarah A. Spinler. "Prevention of Anaphylactoid Reactions in High-Risk Patients Receiving Radiographic Contrast Media." Annals of Pharmacotherapy 28, no. 2 (1994): 236–41. http://dx.doi.org/10.1177/106002809402800215.

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OBJECTIVE: To review various pretreatment regimens for the prophylaxis of anaphylactoid reactions to radiographic contrast media (RCM) in high-risk patients. The proposed etiologies and risk factors for such reactions are also reviewed. DATA SOURCES: A MEDLINE search of the English-language literature was used to identify pertinent human studies and reviews. STUDY SELECTION: All studies comparing pretreatment regimens for anaphylactoid reactions to RCM were reviewed as well as studies comparing the incidence of anaphylactoid reactions between lower and higher osmolar RCM. DATA SYNTHESIS: The t

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Ghasemzadeh Rahbardar, Mahboobeh, Farzaneh Shakeri, and Mohammad Hossein Boskabady. "Medicinal Plants and Histamine (H1) Receptors: An Updated Review." Pharmaceutical Sciences 31, no. 3 (2025): 216–36. https://doi.org/10.34172/ps.025.42115.

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Background: Histamine (H1) receptors play vital roles in a variety of physiological and pathological processes, including allergic reactions, inflammation, immunological responses, bronchoconstriction, pain, and memory deficit. Traditional medicine recognizes the therapeutic potential of medicinal plants in treating these conditions. This comprehensive review attempts to provide detailed information about the effects of medicinal plants on H1 receptors. Methods: The modulatory effects of several medicinal plants, including Achillea millefolium, Berberis vulgaris, Bunium persicum, Carum copticu

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Łażewska, Dorota, Maria Kaleta, Paula Zaręba, et al. "Multitargeting Histamine H3 Receptor Ligands among Acetyl- and Propionyl-Phenoxyalkyl Derivatives." Molecules 28, no. 5 (2023): 2349. http://dx.doi.org/10.3390/molecules28052349.

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Alzheimer’s disease (AD) is a neurodegenerative disorder, for which there is no effective cure. Current drugs only slow down the course of the disease, and, therefore, there is an urgent need to find effective therapies that not only treat, but also prevent it. Acetylcholinesterase inhibitors (AChEIs), among others, have been used for years to treat AD. Histamine H3 receptors (H3Rs) antagonists/inverse agonists are indicated for CNS diseases. Combining AChEIs with H3R antagonism in one structure could bring a beneficial therapeutic effect. The aim of this study was to find new multitargetting

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Thomas, Shilu Deepa, Petrilla Jayaprakash, Nurfirzana Z. H. J. Marwan, et al. "Alleviation of Autophagic Deficits and Neuroinflammation by Histamine H3 Receptor Antagonist E159 Ameliorates Autism-Related Behaviors in BTBR Mice." Pharmaceuticals 17, no. 10 (2024): 1293. http://dx.doi.org/10.3390/ph17101293.

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Background/Objectives: Autism spectrum disorder (ASD) is a neurodevelopmental condition marked by social interaction difficulties, repetitive behaviors, and immune dysregulation with elevated pro-inflammatory markers. Autophagic deficiency also contributes to social behavior deficits in ASD. Histamine H3 receptor (H3R) antagonism is a potential treatment strategy for brain disorders with features overlapping ASD, such as schizophrenia and Alzheimer’s disease. Methods: This study investigated the effects of sub-chronic systemic treatment with the H3R antagonist E159 on social deficits, repetiti

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Inaba, Niro, Masahiro Shibata, Sadayoshi Onodera, Yuriko Chida, Tetsuaki Yamaura, and Haruo Ohnishi. "Characterization of the H2-receptor antagonism by FRG-8813, a new histamine H2-receptor antagonist in isolated guinea pig parietal cells." Japanese Journal of Pharmacology 58 (1992): 353. http://dx.doi.org/10.1016/s0021-5198(19)49552-8.

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Dove, Stefan, Martin C. Michel, Sebastian Knieps, and Armin Buschauer. "Pharmacology and quantitative structure-activity relationships of imidazolylpropylguanidines with mepyramine-like substructures as non-peptide neuropeptide Y Y1 receptor antagonists." Canadian Journal of Physiology and Pharmacology 78, no. 2 (2000): 108–15. http://dx.doi.org/10.1139/y99-120.

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The design of non-peptide, Y1-selective antagonists of neuropeptide Y (NPY) as pharmacological tools is in progress and is increasingly important as therapeutic applications are expected. Starting from the potent histamine H2 agonist and weak NPY Y1 antagonist arpromidine, 16 imidazolylpropylguanidine derivatives were synthesized and tested for Y1 antagonistic activity (inhibition of NPY-stimulated Ca2+ increase in human erythroleukemic cells), where the pheniramine-like moiety of arpromidine was replaced with 2-pyridylaminoalkyl, benzyl-(2-pyridyl)aminoalkyl, and phenyl-(2-pyridyl)alkylaminoa

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Bezerra Rodrigues Dantas, Lindaiane, Ana Letícia Moreira Silva, Cícero Pedro da Silva Júnior, et al. "Nootkatone Inhibits Acute and Chronic Inflammatory Responses in Mice." Molecules 25, no. 9 (2020): 2181. http://dx.doi.org/10.3390/molecules25092181.

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Nootkatone (NTK) is a sesquiterpenoid found in essential oils of many species of Citrus (Rutaceae). Considering previous reports demonstrating that NTK inhibited inflammatory signaling pathways, this study aimed to investigate the effects of this compound in mice models of acute and chronic inflammation. Murine models of paw edema induced by carrageenan, dextran, histamine, and arachidonic acid, as well as carrageenan-induced peritonitis and pleurisy, were used to evaluate the effects of NTK on acute inflammation. A murine model of granuloma induced by cotton pellets was used to access the imp

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Meskanen, Katarina, Heidi Ekelund, Jarmo Laitinen, et al. "A Randomized Clinical Trial of Histamine 2 Receptor Antagonism in Treatment-Resistant Schizophrenia." Journal of Clinical Psychopharmacology 33, no. 4 (2013): 472–78. http://dx.doi.org/10.1097/jcp.0b013e3182970490.

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Walther, Andreas, Michael Jäger, Andreas Secchi, et al. "Effects of histamine-1 receptor antagonism on leukocyte-independent plasma extravasation during endotoxemia." Journal of Critical Care 16, no. 1 (2001): 24–31. http://dx.doi.org/10.1053/jcrc.2001.21793.

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Kondru, Sundar Kumar, Ajay Godwin Potnuri, Lingesh Allakonda, and Prasad Konduri. "Histamine 2 receptor antagonism elicits protection against doxorubicin-induced cardiotoxicity in rodent model." Molecular and Cellular Biochemistry 441, no. 1-2 (2017): 77–88. http://dx.doi.org/10.1007/s11010-017-3175-x.

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Cowden, Jeffery M., Fuqu Yu, Mamatha Challapalli, et al. "Antagonism of the histamine H4 receptor reduces LPS-induced TNF production in vivo." Inflammation Research 62, no. 6 (2013): 599–607. http://dx.doi.org/10.1007/s00011-013-0612-5.

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Benyon, R. C., M. A. Lowman, and M. K. Church. "Human skin mast cells: their dispersion, purification, and secretory characterization." Journal of Immunology 138, no. 3 (1987): 861–67. http://dx.doi.org/10.4049/jimmunol.138.3.861.

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Abstract Digestion of human foreskin with collagenase and hyaluronidase disperses approximately 3.4 X 10(7) nucleated cells per gram of tissue, of which mast cells constitute 4.7%. These may be purified to 80% by use of density gradient centrifugation. The majority of mast cells (79%) measured between 9 and 13 micron in diameter, and the mean histamine content was 4.6 pg/cell. Viability was demonstrated by trypan blue exclusion by 93% of the cells and the low spontaneous histamine secretion of less than 7% in functional studies. Anti-IgE released up to 17.5% of cell-associated histamine within

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Schane, Claire P., Adam T. Nelczyk, Cheng Chen, et al. "Abstract 1365: Histamine from mast cells protects against breast cancer recurrence." Cancer Research 85, no. 8_Supplement_1 (2025): 1365. https://doi.org/10.1158/1538-7445.am2025-1365.

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Abstract One in eight women will develop breast cancer in their lifetime. 20-30% of these women develop recurrent metastatic disease, for which clinical treatments have limited efficacy. Metastasis is thought to be a stepwise process, terminating with extravasation into distal tissues. After this distal extravasation, cancer cells do not always immediately proliferate, but remain dormant. These dormant cells may awaken through yet-unknown mechanisms. There is therefore an urgent need to better understand dormancy and reawakening to mitigate the risk of metastatic recurrence. Previous work from

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Mangum, Joshua, Karen Needham, Dylan Sieck, Christopher Minson, and John Halliwill. "Effect of Histamine‐Receptor Antagonism on the Acute Inflammatory Response to Aerobic Cycling Exercise." FASEB Journal 34, S1 (2020): 1. http://dx.doi.org/10.1096/fasebj.2020.34.s1.03432.

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Bhowmik, Malay, Neeru Saini, and Divya Vohora. "Histamine H3 receptor antagonism by ABT-239 attenuates kainic acid induced excitotoxicity in mice." Brain Research 1581 (September 2014): 129–40. http://dx.doi.org/10.1016/j.brainres.2014.06.012.

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Tashiro, Takao, Kageyoshi Ono, Tsuyoshi Watanabe, et al. "Histamine H₂ Receptor Antagonism by T-593: Studies on cAMP Generation in Hepa Cells Expressing Histamine H₂ Receptor." Pharmacology 59, no. 1 (1999): 1–10. http://dx.doi.org/10.1159/000028300.

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