リカセトロン

リカセトロン
IUPAC命名法による物質名
	IUPAC名 endo-N-(8-Methyl-8-azabicyclo[3.2.1]oct-3yl)-2,3-dihydro-3,3-dimethyl-indole-1-carboxamide;
識別
CAS番号;	117086-68-7
ATCコード	none
PubChem	CID: 14850173
IUPHAR/BPS	2302
ChemSpider	16736765
UNII	R92JB88O88
ChEMBL	CHEMBL2105377
化学的データ
化学式	C19H27N3O
分子量	313.45 g·mol−1
	SMILES CC1(CN(c2c1cccc2)C(=O)N[C@H]3C[C@H]4CC[C@@H](C3)N4C)C;
	InChI InChI=1S/C19H27N3O/c1-19(2)12-22(17-7-5-4-6-16(17)19)18(23)20-13-10-14-8-9-15(11-13)21(14)3/h4-7,13-15H,8-12H2,1-3H3,(H,20,23)/t13-,14+,15- ; Key:ILXWRFDRNAKTDD-QDMKHBRRSA-N ;

リカセトロン(Ricasetron, BRL-446470)は、セロトニンの5-HT3受容体の選択的アンタゴニストとして作用する薬剤である[1]。他の5-HT3受容体拮抗薬と同様に、制吐薬としての作用を持つ[2]。また、関連の薬剤よりもかなり強い抗不安薬の作用も持ち[3]、ベンゾジアゼピン系の抗不安薬と比べて副作用は少ない[4][5]。しかし、医療用途の開発はなされなかった。

出典

“BRL 46470 potently antagonizes neural responses activated by 5-HT3 receptors”. Neuropharmacology 32 (8): 729-35. (August 1993). doi:10.1016/0028-3908(93)90180-B. PMID 8413836.
“Prolonged anti-emetic activity and 5-HT3-receptor antagonism by BRL 46470 in conscious ferrets”. The Journal of Pharmacy and Pharmacology 46 (6): 520-1. (June 1994). doi:10.1111/j.2042-7158.1994.tb03843.x. PMID 7932054.
“BRL 46470A: a highly potent, selective and long acting 5-HT3 receptor antagonist with anxiolytic-like properties”. Psychopharmacology 110 (3): 257-64. (1993). doi:10.1007/BF02251279. PMID 7831418.
“The effects of BRL 46470A, a novel 5-HT3 receptor antagonist, and lorazepam on psychometric performance and the EEG”. British Journal of Clinical Pharmacology 35 (4): 395-9. (April 1993). doi:10.1111/j.1365-2125.1993.tb04156.x. PMC 1381550. PMID 8485019.
“Absence of amnestic effect of an anxiolytic 5-HT3 antagonist (BRL 46470A) injected into basolateral amygdala, as opposed to diazepam”. Behavioural Brain Research 59 (1-2): 141-5. (December 1993). doi:10.1016/0166-4328(93)90160-R. PMID 8155281.

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[pmid8413836-1] “BRL 46470 potently antagonizes neural responses activated by 5-HT3 receptors”. Neuropharmacology 32 (8): 729-35. (August 1993). doi:10.1016/0028-3908(93)90180-B. PMID 8413836.

[pmid7932054-2] “Prolonged anti-emetic activity and 5-HT3-receptor antagonism by BRL 46470 in conscious ferrets”. The Journal of Pharmacy and Pharmacology 46 (6): 520-1. (June 1994). doi:10.1111/j.2042-7158.1994.tb03843.x. PMID 7932054.

[pmid7831418-3] “BRL 46470A: a highly potent, selective and long acting 5-HT3 receptor antagonist with anxiolytic-like properties”. Psychopharmacology 110 (3): 257-64. (1993). doi:10.1007/BF02251279. PMID 7831418.

[pmid8485019-4] “The effects of BRL 46470A, a novel 5-HT3 receptor antagonist, and lorazepam on psychometric performance and the EEG”. British Journal of Clinical Pharmacology 35 (4): 395-9. (April 1993). doi:10.1111/j.1365-2125.1993.tb04156.x. PMC 1381550. PMID 8485019.

[pmid8155281-5] “Absence of amnestic effect of an anxiolytic 5-HT3 antagonist (BRL 46470A) injected into basolateral amygdala, as opposed to diazepam”. Behavioural Brain Research 59 (1-2): 141-5. (December 1993). doi:10.1016/0166-4328(93)90160-R. PMID 8155281.

リカセトロン

関連項目

出典