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
{"title":"GtoPdb v.2023.1中的组胺受体","authors":"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","doi":"10.2218/gtopdb/f33/2023.1","DOIUrl":null,"url":null,"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].","PeriodicalId":14617,"journal":{"name":"IUPHAR/BPS Guide to Pharmacology CITE","volume":"74 1","pages":"0"},"PeriodicalIF":0.0000,"publicationDate":"2023-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Histamine receptors in GtoPdb v.2023.1\",\"authors\":\"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\",\"doi\":\"10.2218/gtopdb/f33/2023.1\",\"DOIUrl\":null,\"url\":null,\"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].\",\"PeriodicalId\":14617,\"journal\":{\"name\":\"IUPHAR/BPS Guide to Pharmacology CITE\",\"volume\":\"74 1\",\"pages\":\"0\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2023-04-26\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"IUPHAR/BPS Guide to Pharmacology CITE\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2218/gtopdb/f33/2023.1\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"IUPHAR/BPS Guide to Pharmacology CITE","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2218/gtopdb/f33/2023.1","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
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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