Journal ArticleDOI
HETEROGENEITY OF HISTAMINE Hi‐RECEPTORS: SPECIES VARIATIONS IN [3H]MEPYRAMINE BINDING OF BRAIN MEMBRANES
TLDR
The tricyclic antidepressant doxepin and the neuroleptic clozapine are the most potent of all drugs examined in competing for [3H]mepyramine binding, exceeding in potency any H1 antihistamines examined.Abstract:
[3H]Mepyramine binds with high affinity to membranes from brain of human, rat, guinea-pig, rabbit and mouse with drug specificity indicating an association with histamine H1receptors. Considerable species differences occur in the affinity of [3H]mepyramine, with guinea-pig and human having 34 times greater affinity than rat, mouse or rabbit. The greater affinity of [3H]mepyramine in guinea-pig than in rat is attributable both to faster association and slower dissociation rates in guinea-pig. Species differences in affinity for H1 receptor sites occur for some antihistamines but not for others. Some tricyclic antidepressant and neuroleptic drugs are extremely potent inhibitors of [3H]mepyramine binding, exceeding in potency any H1 antihistamines examined. The tricyclic antidepressant doxepin and the neuroleptic clozapine are the most potent of all drugs examined in competing for [3H]mepyramine binding. The regional distribution of specific [3H]mepyramine binding differs considerably in the various species examined.read more
Citations
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Journal ArticleDOI
Histamine in the Nervous System
TL;DR: Mutual interactions with other transmitter systems form a network that links basic homeostatic and higher brain functions, including sleep-wake regulation, circadian and feeding rhythms, immunity, learning, and memory in health and disease.
Journal ArticleDOI
The physiology of brain histamine.
TL;DR: The central histamine system is involved in many central nervous system functions: arousal; anxiety; activation of the sympathetic nervous system; the stress-related release of hormones from the pituitary and of central aminergic neurotransmitters; antinociception; water retention and suppression of eating.
Journal Article
International Union of Pharmacology. XIII. Classification of Histamine Receptors
Stephen J. Hill,Charon Robin Ganellin,Henk Timmerman,J C Schwartz,Nigel P. Shankley,J. M. Young,Schunack Walter G,Roberto Levi,Helmut L. Haas +8 more
TL;DR: The classification of histamine receptors has to date been based on rigorous classical pharmacological analysis, and as yet, the classification of the three histamines receptors that have been defined by this process have not been added to because of lack of evidence.
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Neurotransmitter Receptor and Transporter Binding Profile of Antidepressants and Their Metabolites
TL;DR: Novel findings, not widely described previously, suggest that many of the individual drugs studied in these experiments possess some structural characteristic that determines affinity for several G protein-coupled, but not muscarinic, receptors.
Journal ArticleDOI
Biochemical and pharmacological characterization of an extremely potent and selective nonpeptide cholecystokinin antagonist
TL;DR: L-364,718 exhibited a very high selectivity for peripheral CCK receptors relative to brain CCK, gastrin, and various other peptide and nonpeptide receptors in both in vitro radioligand and isolated tissue assays.
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Journal Article
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