维基百科中的医学内容
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医学声明。
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。
Quick Facts 8-OH-DPAT, 识别 ...
8-OH-DPAT
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系统名 7-(Dipropylamino)-5,6,7,8-tetrahydronaphthalen-1-ol[1]
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识别
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缩写
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8-OH-DPAT
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CAS号
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78950-78-4 Y
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PubChem
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1220 6603866((R)) 10125797((S))
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ChemSpider
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1183, 5036174 (R), 8301316 (S)
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SMILES
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- CCCN(CCC)C1CCc2cccc(O)c2C1
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InChI
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- 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
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InChIKey
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ASXGJMSKWNBENU-UHFFFAOYAY
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ChEBI
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73364
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MeSH
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8-Hydroxy-2-(di-n-propylamino)tetralin
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IUPHAR配体
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7
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性质
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化学式
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C16H25NO
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摩尔质量
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247.38 g·mol−1
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log P
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3.711
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pKa
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10.539
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pKb
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3.458
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药理学
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药代动力学:
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1.5 小时
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若非注明,所有数据均出自标准状态(25 ℃,100 kPa)下。
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Close
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]
- 5-OH-DPAT
- 7-OH-DPAT
- Bay R 1531
- MDAT
- UH-301
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.
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.
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.
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.
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.
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.
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.