阿贝卡尔

**阿贝卡尔**
臨床資料
ATC碼	未分配;
藥物動力學數據
生物半衰期	3.4 hours (IV), 7 hours (oral)
识别信息
	IUPAC命名法 propan-2-yl 4-(methoxymethyl)-6-(phenylmethoxy) -9H-pyrido[5,4-b]indole-3-carboxylate; ;
CAS号	111841-85-1
PubChem CID	65914;
ChemSpider	59323 ;
UNII	IZM1PNJ3JL;
KEGG	D02594 ;
ChEMBL	ChEMBL454095 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID40149745 ;
化学信息
化学式	C24H24N2O4
摩尔质量	404.47 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES COCc3c(C(=O)OC(C)C)ncc4[nH]c2ccc(OCc1ccccc1)cc2c34;
	InChI InChI=1S/C24H24N2O4/c1-15(2)30-24(27)23-19(14-28-3)22-18-11-17(29-13-16-7-5-4-6-8-16)9-10-20(18)26-21(22)12-25-23/h4-12,15,26H,13-14H2,1-3H3 ; Key:RLFKILXOLJVUNF-UHFFFAOYSA-N ;

阿贝卡尔（英语：Abecarnil，代号：ZK-112,119）是一种来自β-咔啉家族的抗焦虑药。它是相对较新开发的一类药物之一，称为非苯二氮䓬类药物，与较早的苯二氮䓬类药物具有相似的作用，但化学结构截然不同。它是一种部分激动剂，选择性地作用于GABA_A受体的苯二氮䓬位点。^[1]

阿贝卡尔最初是作为抗焦虑药物开发的，但尚未商业化开发用于人类，目前主要用于研究开发其他新型镇静和抗焦虑药物。对其作用的调查仍在继续，它看起来很可能被开发用于治疗焦虑症，^[2]以及作为一种不太容易上瘾的替代药物来治疗苯二氮䓬类药物^[3]和酒精^[4]成瘾。与非选择性全激动剂苯二氮䓬类药物相比，阿贝卡尼的耐受性和戒断问题也可能更少。^[5]

阿贝卡尔是一种相对亚型选择性的药物，主要产生抗焦虑作用，具有相对较弱的镇静或肌肉松弛作用，^[6]^[7]并且不会显着增强酒精的作用。^[8]

阿贝卡尔的滥用可能性被认为低于苯二氮卓类药物，^[9]突然停止治疗后仅会出现轻微的戒断症状。^[10]

参见[编辑]

参考资料[编辑]

^ Ozawa, M; Nakada, Y; Sugimachi, K; Yabuuchi, F; Akai, T; Mizuta, E; Kuno, S; Yamaguchi, M. Pharmacological characterization of the novel anxiolytic beta-carboline abecarnil in rodents and primates. Japanese Journal of Pharmacology. Mar 1994, 64 (3): 179–87. PMID 7912751. doi:10.1254/jjp.64.179 .
^ Aufdembrinke B. Abecarnil, a new beta-carboline, in the treatment of anxiety disorders. British Journal of Psychiatry. 1998, 34 (34): 55–63. PMID 9829018. S2CID 24311570. doi:10.1192/S0007125000293537.
^ Pinna G, Galici R, Schneider HH, Stephens DN, Turski L. Alprazolam dependence prevented by substituting with the beta-carboline abecarnil. Proceedings of the National Academy of Sciences of the United States of America. Mar 1997, 94 (6): 2719–23. Bibcode:1997PNAS...94.2719P. PMC 20156 . PMID 9122263. doi:10.1073/pnas.94.6.2719 .
^ Jung ME, Wallis CJ, Gatch MB, Lal H. Abecarnil and alprazolam reverse anxiety-like behaviors induced by ethanol withdrawal. Alcohol. Jun 2000, 21 (2): 161–8. PMID 10963939. doi:10.1016/S0741-8329(00)00079-3.
^ Löscher W, Hönack D. Withdrawal precipitation by benzodiazepine receptor antagonists in dogs chronically treated with diazepam or the novel anxiolytic and anticonvulsant beta-carboline abecarnil. Naunyn Schmiedebergs Arch. Pharmacol. April 1992, 345 (4): 452–60. PMID 1352384. S2CID 20486955. doi:10.1007/BF00176624.
^ Krause W, Schutt B, Duka T. Pharmacokinetics and acute toleration of the beta-carboline derivative abecarnil in man. Arzneimittelforschung. May 1990, 40 (5): 529–32. PMID 1974428.
^ Duka T, Schutt B, Krause W, Dorow R, McDonald S, Fichte K. Human studies on abecarnil, a new beta-carboline anxiolytic: safety, tolerability and preliminary pharmacological profile. British Journal of Clinical Pharmacology. Apr 1993, 35 (4): 386–94. PMC 1381549 . PMID 8097921. doi:10.1111/j.1365-2125.1993.tb04155.x.
^ Stephens DN, Schneider HH, Kehr W, Andrews JS, Rettig KJ, Turski L, Schmiechen R, Turner JD, Jensen LH, et al. Abecarnil, a metabolically stable, anxioselective beta-carboline acting at benzodiazepine receptors. Journal of Pharmacology and Experimental Therapeutics. Apr 1990, 253 (1): 334–43. PMID 1970361.
^ Sannerud CA, Ator NA, Griffiths RR. Behavioral pharmacology of abecarnil in baboons: self-injection, drug discrimination and physical dependence. Behavioural Pharmacology. Oct 1992, 3 (5): 507–516. PMID 11224153. S2CID 32081258. doi:10.1097/00008877-199210000-00009.
^ Ballenger JC, McDonald S, Noyes R, Rickels K, Sussman N, Woods S, Patin J, Singer J. The first double-blind, placebo-controlled trial of a partial benzodiazepine agonist abecarnil (ZK 112-119) in generalized anxiety disorder. Psychopharmacology Bulletin. 1991, 27 (2): 171–9. PMID 1681563.

[1] Ozawa, M; Nakada, Y; Sugimachi, K; Yabuuchi, F; Akai, T; Mizuta, E; Kuno, S; Yamaguchi, M. Pharmacological characterization of the novel anxiolytic beta-carboline abecarnil in rodents and primates. Japanese Journal of Pharmacology. Mar 1994, 64 (3): 179–87. PMID 7912751. doi:10.1254/jjp.64.179 .

[2] Aufdembrinke B. Abecarnil, a new beta-carboline, in the treatment of anxiety disorders. British Journal of Psychiatry. 1998, 34 (34): 55–63. PMID 9829018. S2CID 24311570. doi:10.1192/S0007125000293537.

[3] Pinna G, Galici R, Schneider HH, Stephens DN, Turski L. Alprazolam dependence prevented by substituting with the beta-carboline abecarnil. Proceedings of the National Academy of Sciences of the United States of America. Mar 1997, 94 (6): 2719–23. Bibcode:1997PNAS...94.2719P. PMC 20156 . PMID 9122263. doi:10.1073/pnas.94.6.2719 .

[4] Jung ME, Wallis CJ, Gatch MB, Lal H. Abecarnil and alprazolam reverse anxiety-like behaviors induced by ethanol withdrawal. Alcohol. Jun 2000, 21 (2): 161–8. PMID 10963939. doi:10.1016/S0741-8329(00)00079-3.

[5] Löscher W, Hönack D. Withdrawal precipitation by benzodiazepine receptor antagonists in dogs chronically treated with diazepam or the novel anxiolytic and anticonvulsant beta-carboline abecarnil. Naunyn Schmiedebergs Arch. Pharmacol. April 1992, 345 (4): 452–60. PMID 1352384. S2CID 20486955. doi:10.1007/BF00176624.

[6] Krause W, Schutt B, Duka T. Pharmacokinetics and acute toleration of the beta-carboline derivative abecarnil in man. Arzneimittelforschung. May 1990, 40 (5): 529–32. PMID 1974428.

[7] Duka T, Schutt B, Krause W, Dorow R, McDonald S, Fichte K. Human studies on abecarnil, a new beta-carboline anxiolytic: safety, tolerability and preliminary pharmacological profile. British Journal of Clinical Pharmacology. Apr 1993, 35 (4): 386–94. PMC 1381549 . PMID 8097921. doi:10.1111/j.1365-2125.1993.tb04155.x.

[8] Stephens DN, Schneider HH, Kehr W, Andrews JS, Rettig KJ, Turski L, Schmiechen R, Turner JD, Jensen LH, et al. Abecarnil, a metabolically stable, anxioselective beta-carboline acting at benzodiazepine receptors. Journal of Pharmacology and Experimental Therapeutics. Apr 1990, 253 (1): 334–43. PMID 1970361.

[9] Sannerud CA, Ator NA, Griffiths RR. Behavioral pharmacology of abecarnil in baboons: self-injection, drug discrimination and physical dependence. Behavioural Pharmacology. Oct 1992, 3 (5): 507–516. PMID 11224153. S2CID 32081258. doi:10.1097/00008877-199210000-00009.

[10] Ballenger JC, McDonald S, Noyes R, Rickels K, Sussman N, Woods S, Patin J, Singer J. The first double-blind, placebo-controlled trial of a partial benzodiazepine agonist abecarnil (ZK 112-119) in generalized anxiety disorder. Psychopharmacology Bulletin. 1991, 27 (2): 171–9. PMID 1681563.

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