8-OH-DPAT

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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-HT_1A受体功能，是最早被发现的5-HT_1A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  Y
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：
生物半衰期	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-HT_1A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

• 5-OH-DPAT
• 7-OH-DPAT
• Bay R 1531
• MDAT
• UH-301

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. 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

• Yves Aubert, Thesis, Leiden University. (Dec 11, 2012)Yves Aubert, Thesis, Leiden University. (Dec 11, 2012)