扎考必利

扎考必利（英语：Zacopride），或译为查可必利，是5-HT3受体的有效拮抗剂[1]和5-HT4受体的激动剂。[2]它在动物模型中具有抗焦虑[3]和促智作用，[4]其中(R)-(+)-对映体是更活跃的形式。[5]它还具有止吐[6]和促呼吸作用，在动物研究中既能减少睡眠呼吸暂停，[7]又能逆转阿片类药物引起的呼吸抑制。[8]早期的动物试验还表明，给予扎考必利可以减少对乙醇的偏好和消耗。[9]

扎考必利
臨床資料
ATC碼
  • 未分配
识别
  • 4-amino-5-chloro-2-methoxy-N-(quinuclidin-3-yl)benzamide
CAS号90182-92-6  checkY
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
化学
化学式C15H20ClN3O2
摩尔质量309.79 g·mol−1
3D模型（JSmol）
  • COC1=CC(=C(C=C1C(=O)NC2CN3CCC2CC3)Cl)N
  • InChI=1S/C15H20ClN3O2/c1-21-14-7-12(17)11(16)6-10(14)15(20)18-13-8-19-4-2-9(13)3-5-19/h6-7,9,13H,2-5,8,17H2,1H3,(H,18,20) ☒N
  • Key:FEROPKNOYKURCJ-UHFFFAOYSA-N ☒N

发现扎考必利在400微克的剂量下显着增加人类受试者的醛固酮水平达180分钟。人们认为这是通过刺激肾上腺上的5-HT4受体来实现的。扎考必利在体外应用于人肾上腺时也能刺激醛固酮分泌。肾素、促肾上腺皮质激素或皮质醇水平未观察到显着变化。[2]

扎考必利已在治疗精神分裂症的临床试验中进行了测试，但未获成功。[10]

参考资料
  1. Smith WW, Sancilio LF, Owera-Atepo JB, Naylor RJ, Lambert L. . The Journal of Pharmacy and Pharmacology. April 1988, 40 (4): 301–2. PMID 2900319. S2CID 32862252. doi:10.1111/j.2042-7158.1988.tb05253.x.
  2. Lefebvre H, Contesse V, Delarue C, Soubrane C, Legrand A, Kuhn JM, et al. . The Journal of Clinical Endocrinology and Metabolism. December 1993, 77 (6): 1662–6. PMID 8263156. doi:10.1210/jcem.77.6.8263156.
  3. Costall B, Domeney AM, Gerrard PA, Kelly ME, Naylor RJ. . The Journal of Pharmacy and Pharmacology. April 1988, 40 (4): 302–5. PMID 2900320. S2CID 1083706. doi:10.1111/j.2042-7158.1988.tb05254.x.
  4. Fontana DJ, Daniels SE, Eglen RM, Wong EH. . Neuropharmacology. March 1996, 35 (3): 321–7. PMID 8783207. S2CID 12818436. doi:10.1016/0028-3908(96)00191-8.
  5. Young R, Johnson DN. . European Journal of Pharmacology. August 1991, 201 (2–3): 151–5. PMID 1686755. doi:10.1016/0014-2999(91)90338-Q.
  6. Yamakuni H, Nakayama H, Matsui S, Imazumi K, Matsuo M, Mutoh S. . Journal of Pharmacological Sciences. May 2006, 101 (1): 99–102. PMID 16651699. doi:10.1254/jphs.SCJ05007X 可免费查阅.
  7. Carley DW, Depoortere H, Radulovacki M. . Pharmacology, Biochemistry, and Behavior. 2001, 69 (1–2): 283–9. PMID 11420096. S2CID 11848748. doi:10.1016/S0091-3057(01)00535-4.
  8. Meyer LC, Fuller A, Mitchell D. . American Journal of Physiology. Regulatory, Integrative and Comparative Physiology. February 2006, 290 (2): R405–13. PMID 16166206. S2CID 224414. doi:10.1152/ajpregu.00440.2005.
  9. Knapp DJ, Pohorecky LA. . Pharmacology, Biochemistry, and Behavior. April 1992, 41 (4): 847–50. PMID 1594653. S2CID 45436887. doi:10.1016/0091-3057(92)90237-A.
  10. Newcomer JW, Faustman WO, Zipursky RB, Csernansky JG. . Archives of General Psychiatry. September 1992, 49 (9): 751–2. PMID 1514881. doi:10.1001/archpsyc.1992.01820090079013.
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