Histamine receptors in GtoPdb v.2023.1

IUPHAR/BPS Guide to Pharmacology CITE Pub Date : 2023-04-26 DOI:10.2218/gtopdb/f33/2023.1

Paul Chazot, Marlon Cowart, Hiroyuki Fukui, C. Robin Ganellin, Ralf Gutzmer, Helmut L. Haas, Stephen J. Hill, Rebecca Hills, Rob Leurs, Roberto Levi, Steve Liu, Pertti Panula, Walter Schunack, Jean-Charles Schwartz, Roland Seifert, Nigel P. Shankley, Holger Stark, Robin Thurmond, Henk Timmerman, J. Michael Young

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Abstract

Histamine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Histamine Receptors [80, 174]) are activated by the endogenous ligand histamine. Marked species differences exist between histamine receptor orthologues [80]. The human and rat H3 receptor genes are subject to significant splice variance [12]. The potency order of histamine at histamine receptor subtypes is H3 = H4 > H2 > H1 [174]. Some agonists at the human H3 receptor display significant ligand bias [183]. Antagonists of all 4 histamine receptors have clinical uses: H1 antagonists for allergies (e.g. cetirizine), H2 antagonists for acid-reflux diseases (e.g. ranitidine), H3 antagonists for narcolepsy (e.g. pitolisant/WAKIX; Registered) and H4 antagonists for atopic dermatitis (e.g. adriforant; Phase IIa) [174] and vestibular neuritis (AUV) (SENS-111 (Seliforant, previously UR-63325), entered and completed vestibular neuritis (AUV) Phase IIa efficacy and safety trials, respectively) [217, 8].

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GtoPdb v.2023.1中的组胺受体

组胺受体(由NC-IUPHAR组胺受体小组委员会商定的命名法[80,174])由内源性配体组胺激活。组胺受体同源物之间存在明显的物种差异[80]。人和大鼠的H3受体基因存在显著的剪接变异[12]。组胺在组胺受体亚型上的效价顺序为H3 = H4 >H2祝辞H1[174]。一些人H3受体激动剂表现出明显的配体偏倚[183]。所有4种组胺受体的拮抗剂都有临床用途:H1拮抗剂用于过敏(如西替利嗪)，H2拮抗剂用于酸反流疾病(如雷尼替丁)，H3拮抗剂用于发作性睡病(如pitolisant/WAKIX;已注册)和H4拮抗剂用于特应性皮炎(例如:adriforant;IIa期)[174]和前庭神经炎(AUV) (SENS-111 (Seliforant，原UR-63325)分别进入并完成了前庭神经炎(AUV) IIa期疗效和安全性试验)[217,8]。

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IUPHAR/BPS Guide to Pharmacology CITE

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