ベメセトロン

ベメセトロン
IUPAC命名法による物質名
	IUPAC名 [(1S,5R)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] 3,5-dichlorobenzoate;
データベースID
CAS番号;	40796-97-2
ATCコード	none
PubChem	CID: 671690
ChemSpider	10498629
UNII	O98T3677PA
ChEMBL	CHEMBL2107804
化学的データ
化学式	C15H17Cl2NO2
分子量	314.21 g·mol−1
	SMILES CN3[C@@H]1CC[C@H]3C[C@H](C1)OC(=O)c2cc(Cl)cc(Cl)c2;
	InChI InChI=1S/C15H17Cl2NO2/c1-18-12-2-3-13(18)8-14(7-12)20-15(19)9-4-10(16)6-11(17)5-9/h4-6,12-14H,2-3,7-8H2,1H3/t12-,13+,14+ ; Key:MNJNPLVXBISNSX-WDNDVIMCSA-N ;
	テンプレートを表示

ベメセトロン(Bemesetron, MDL-72222)は、5-HT3受容体のアンタゴニストとして作用する薬剤である^[1]。メトクロプラミドと匹敵する程の制吐薬としての作用を持つ^[2]。しかし、臨床使用されたことはなく、主な用途は、乱用薬物の活性における5-HT3受容体の関わりについての科学的研究における利用である^[3]^[4]^[5]^[6]。

出典

^ “Effect of the selective 5-HT3 receptor antagonists ICS 205-930 and MDL 72222 on 5-HTP-induced head shaking and behavioral symptoms induced by 5-methoxy-N,N,dimethyltryptamine in rats: comparison with some other 5-HT receptor antagonists”. Psychopharmacology 92 (4): 520-3. (1987). doi:10.1007/bf00176488. PMID 3114804.
^ “Randomized comparison of the antiemetic efficacy of a serotonin type 3 receptor antagonist (MDL 72,222) with a high-dose metoclopramide regimen”. Am. J. Clin. Oncol. 16 (2): 175-9. (April 1993). doi:10.1097/00000421-199304000-00020. PMID 8452114.
^ “Effects of MDL 72222, a serotonin3 antagonist, on operant responding for ethanol by alcohol-preferring P rats”. Alcohol. Clin. Exp. Res. 24 (10): 1500-4. (October 2000). doi:10.1111/j.1530-0277.2000.tb04567.x. PMID 11045857.
^ “5-HT3 receptor antagonist MDL 72222 attenuates cocaine- and mazindol-, but not methylphenidate-induced neurochemical and behavioral effects in the rat”. Psychopharmacology 159 (4): 341-50. (February 2002). doi:10.1007/s00213-001-0939-4. PMID 11823886.
^ “Effect of 5-HT3 receptor antagonist MDL 72222 on behaviors induced by ketamine in rats and mice”. Eur Neuropsychopharmacol 16 (4): 297-310. (May 2006). doi:10.1016/j.euroneuro.2005.10.001. PMID 16288851.
^ “Dopamine neurotransmission is involved in the attenuating effects of 5-HT3 receptor antagonist MDL 72222 on acute methamphetamine-induced locomotor hyperactivity in mice”. Synapse 62 (1): 8-13. (January 2008). doi:10.1002/syn.20461. PMID 17948891.

[1] “Effect of the selective 5-HT3 receptor antagonists ICS 205-930 and MDL 72222 on 5-HTP-induced head shaking and behavioral symptoms induced by 5-methoxy-N,N,dimethyltryptamine in rats: comparison with some other 5-HT receptor antagonists”. Psychopharmacology 92 (4): 520-3. (1987). doi:10.1007/bf00176488. PMID 3114804.

[2] “Randomized comparison of the antiemetic efficacy of a serotonin type 3 receptor antagonist (MDL 72,222) with a high-dose metoclopramide regimen”. Am. J. Clin. Oncol. 16 (2): 175-9. (April 1993). doi:10.1097/00000421-199304000-00020. PMID 8452114.

[3] “Effects of MDL 72222, a serotonin3 antagonist, on operant responding for ethanol by alcohol-preferring P rats”. Alcohol. Clin. Exp. Res. 24 (10): 1500-4. (October 2000). doi:10.1111/j.1530-0277.2000.tb04567.x. PMID 11045857.

[4] “5-HT3 receptor antagonist MDL 72222 attenuates cocaine- and mazindol-, but not methylphenidate-induced neurochemical and behavioral effects in the rat”. Psychopharmacology 159 (4): 341-50. (February 2002). doi:10.1007/s00213-001-0939-4. PMID 11823886.

[5] “Effect of 5-HT3 receptor antagonist MDL 72222 on behaviors induced by ketamine in rats and mice”. Eur Neuropsychopharmacol 16 (4): 297-310. (May 2006). doi:10.1016/j.euroneuro.2005.10.001. PMID 16288851.

[6] “Dopamine neurotransmission is involved in the attenuating effects of 5-HT3 receptor antagonist MDL 72222 on acute methamphetamine-induced locomotor hyperactivity in mice”. Synapse 62 (1): 8-13. (January 2008). doi:10.1002/syn.20461. PMID 17948891.

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関連項目

出典