维基百科

8-OH-DPAT

化合物
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8-OH-DPAT，是1980年代开发的氨基四氢萘化学类研究化学品，常用于研究5-HT1A受体功能，是最早被发现的5-HT1A受体完全激动剂之一。

8-OH-DPAT
系统名
7-(Dipropylamino)-5,6,7,8-tetrahydronaphthalen-1-ol[1]
识别
缩写 8-OH-DPAT
CAS号 78950-78-4  checkY
PubChem 1220
6603866（(R)）
10125797（(S)）
ChemSpider 1183, 5036174 (R), 8301316 (S)
SMILES
 
  • CCCN(CCC)C1CCc2cccc(O)c2C1
InChI
 
  • 1/C16H25NO/c1-3-10-17(11-4-2)14-9-8-13-6-5-7-16(18)15(13)12-14/h5-7,14,18H,3-4,8-12H2,1-2H3
InChIKey ASXGJMSKWNBENU-UHFFFAOYAY
ChEBI 73364
MeSH 8-Hydroxy-2-(di-n-propylamino)tetralin
IUPHAR配体 7
性质
化学式 C16H25NO
摩尔质量 247.38 g·mol−1
log P 3.711
pKa 10.539
pKb 3.458
药理学
药代动力学：
1.5 小时
若非注明，所有数据均出自标准状态（25 ℃，100 kPa）下。

最初科学家认为该化学品对5-HT1A受体有结合专一性，但后来发现8-OH-DPAT也可作5-HT7受体激动剂及血清素再摄取抑制剂/释放剂。[2][3][4][5][6]

动物研究发现，8-OH-DPAT可抗抑郁、[7]抗焦虑、[8]、降低攻击性[9]、降低食欲、[10]止吐、[11]降低身体温度、[12]降血压、[13]令心跳过缓、[13]令换气过度及[14][15][16]镇痛。[17]

参见

参考文献

  1. ^ 8-hydroxy-2-(di-n-propylamino)tetralin - PubChem Public Chemical Database. The PubChem Project. USA: National Center for Biotechnology Information. [2022-03-22]. （原始内容存档于2012-10-16）. 
  2. ^ Larsson LG; Rényi L; Ross SB; Svensson B; Angeby-Möller K. Different effects on the responses of functional pre- and postsynaptic 5-HT1A receptors by repeated treatment of rats with the 5-HT1A receptor agonist 8-OH-DPAT. Neuropharmacology. February 1990, 29 (2): 85–91. PMID 1691832. doi:10.1016/0028-3908(90)90047-U. 
  3. ^ Sprouse J; Reynolds L; Li X; Braselton J; Schmidt A. 8-OH-DPAT as a 5-HT7 agonist: phase shifts of the circadian biological clock through increases in cAMP production. Neuropharmacology. January 2004, 46 (1): 52–62. PMID 14654097. doi:10.1016/j.neuropharm.2003.08.007. 
  4. ^ IUPHAR DATABASE - 5-Hydroxytryptamine receptors - 5-HT7. [2022-03-22]. （原始内容存档于2016-03-03）. 
  5. ^ Assié MB; Koek W. Possible in vivo 5-HT reuptake blocking properties of 8-OH-DPAT assessed by measuring hippocampal extracellular 5-HT using microdialysis in rats. British Journal of Pharmacology. November 1996, 119 (5): 845–50. PMC 1915946  . PMID 8922730. doi:10.1111/j.1476-5381.1996.tb15749.x. 
  6. ^ Wölfel R; Graefe KH. Evidence for various tryptamines and related compounds acting as substrates of the platelet 5-hydroxytryptamine transporter. Naunyn-Schmiedeberg's Archives of Pharmacology. February 1992, 345 (2): 129–36. PMID 1570019. doi:10.1007/BF00165727. 
  7. ^ Luscombe GP; Martin KF; Hutchins LJ; Gosden J; Heal DJ. Mediation of the antidepressant-like effect of 8-OH-DPAT in mice by postsynaptic 5-HT1A receptors. British Journal of Pharmacology. March 1993, 108 (3): 669–77. PMC 1908013  . PMID 8467355. doi:10.1111/j.1476-5381.1993.tb12859.x. 
  8. ^ Schreiber R; De Vry J. Neuronal circuits involved in the anxiolytic effects of the 5-HT1A receptor agonists 8-OH-DPAT ipsapirone and buspirone in the rat. European Journal of Pharmacology. November 1993, 249 (3): 341–51. PMID 7904566. doi:10.1016/0014-2999(93)90531-L. 
  9. ^ de Boer SF; Koolhaas JM. 5-HT1A and 5-HT1B receptor agonists and aggression: a pharmacological challenge of the serotonin deficiency hypothesis. European Journal of Pharmacology. December 2005, 526 (1–3): 125–39. PMID 16310183. doi:10.1016/j.ejphar.2005.09.065. 
  10. ^ Dourish CT; Hutson PH; Curzon G. Characteristics of feeding induced by the serotonin agonist 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT). Brain Research Bulletin. October 1985, 15 (4): 377–84. PMID 2933126. doi:10.1016/0361-9230(85)90005-X. 
  11. ^ Lucot JB. Antiemetic effects of flesinoxan in cats: comparisons with 8-hydroxy-2-(di-n-propylamino)tetralin. European Journal of Pharmacology. February 1994, 253 (1–2): 53–60. PMID 8013549. doi:10.1016/0014-2999(94)90756-0. 
  12. ^ O'Connell MT; Sarna GS; Curzon G. Evidence for postsynaptic mediation of the hypothermic effect of 5-HT1A receptor activation. British Journal of Pharmacology. July 1992, 106 (3): 603–9. PMC 1907559  . PMID 1387027. doi:10.1111/j.1476-5381.1992.tb14382.x. 
  13. ^ 13.0 13.1 Fozard JR; Mir AK; Middlemiss DN. Cardiovascular response to 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) in the rat: site of action and pharmacological analysis. Journal of Cardiovascular Pharmacology. March 1987, 9 (3): 328–47. PMID 2437400. doi:10.1097/00005344-198703000-00010. 
  14. ^ Sahibzada N; Ferreira M; Wasserman AM; Taveira-DaSilva AM; Gillis RA. Reversal of morphine-induced apnea in the anesthetized rat by drugs that activate 5-hydroxytryptamine(1A) receptors. The Journal of Pharmacology and Experimental Therapeutics. February 2000, 292 (2): 704–13. PMID 10640309. 
  15. ^ Meyer LC; Fuller A; Mitchell D. Zacopride and 8-OH-DPAT reverse opioid-induced respiratory depression and hypoxia but not catatonic immobilization in goats. American Journal of Physiology. Regulatory, Integrative and Comparative Physiology. February 2006, 290 (2): R405–13. PMID 16166206. doi:10.1152/ajpregu.00440.2005. 
  16. ^ Guenther U; Manzke T; Wrigge H; Dutschmann M; Zinserling J; Putensen C; Hoeft A. The counteraction of opioid-induced ventilatory depression by the serotonin 1A-agonist 8-OH-DPAT does not antagonize antinociception in rats in situ and in vivo. Anesthesia and Analgesia. April 2009, 108 (4): 1169–76. PMID 19299781. doi:10.1213/ane.0b013e318198f828. 
  17. ^ Xu W; Qiu XC; Han JS. Serotonin receptor subtypes in spinal antinociception in the rat. The Journal of Pharmacology and Experimental Therapeutics. June 1994, 269 (3): 1182–9 [2022-03-22]. PMID 8014862. （原始内容存档于2020-01-25）. 

外部链接


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