関: 8-hydroxy-2-(di-n-propylamino)tetralin

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the 15th letter of the Roman alphabet (同)o
the blood group whose red cells carry neither the A nor B antigens; "people with type O blood are universal donors" (同)type_O, group O

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《呼び掛けの名前の前につけて》『おお』,あ / (驚き・恐れ・喜び・苦痛などを表して)『おお』,ああ,まあ / 《肯定・否定を強めて》
oxygenの化学記号
ohmオーム / Old
《喜び・驚き・失望などを表して》『おお』,ああ,まあ
Ohio

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/07/11 15:11:03」(JST)

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8-OH-DPAT is a research chemical of the aminotetralin chemical class which was developed in the 1980s and has been widely used to study the function of the 5-HT_1A receptor. It was one of the first major 5-HT_1A receptor full agonists to be discovered.

Originally believed to be selective for the 5-HT_1A receptor, 8-OH-DPAT was later found to act as a 5-HT₇ receptor agonist and serotonin reuptake inhibitor/releasing agent as well.^[2]^[3]^[4]^[5]^[6]

In animal studies, 8-OH-DPAT has been shown to possess antidepressant,^[7] anxiolytic,^[8] serenic,^[9] anorectic,^[10] antiemetic,^[11] hypothermic,^[12] hypotensive,^[13] bradycardic,^[13] hyperventilative,^[14]^[15]^[16] and analgesic effects.^[17]

References

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

External links

Yves Aubert, Thesis, Leiden University. (Dec 11, 2012) Sex, aggression and pair-bond: a study on the serotonergic regulation of female sexual function in the marmoset monkey

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Endogenous ciliary neurotrophic factor (CNTF)(1) regulates neurogenesis of the adult brain in the hippocampal subgranular zone (SGZ)(2) and the subventricular zone (SVZ)(3). We have previously shown that the cAMP-inhibiting D2 dopamine receptor increases neurogenesis by inducing astroglial CNTF expr
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Japanese Journal

Enhanced Behavioral Response to Serotonin-Related Agonists in Postweaning Protein Malnourished Mice

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… Twenty days later, we tested for behavioral effects of the selective serotonin (5-HT)1A receptor agonist 8-hydroxy-N,N-dipropyl-2-aminoteralin (8-OH-DPAT) and the 5-HT releaser d-fenfluramine. … The number of head weaving responses induced by 8-OH-DPAT or d-fenfluramine in the PM mice was significantly increased compared with the control diet group. …
NAID 130001872360

Serotonergic Modulation of Absence-Like Seizures in Groggy Rats : a Novel Rat Model of Absence Epilepsy

OHNO Yukihiro,SOFUE Nobumasa,IMAOKU Takuji,MORISHITA Eri,KUMAFUJI Kenta,SASA Masashi,SERIKAWA Tadao
Journal of pharmacological sciences 114(1), 99-105, 2010-09-20
… agonist (±)-8-hydroxy-2-(di-n-propylamino)-tetralin [(±)8-OH-DPAT] or the 5-HT2 … In addition, the inhibitory effects of (±)8-OH-DPAT and (±)DOI were reversed by WAY-100135 (5-HT1A …
NAID 10029889960

Related Pictures

★リンクテーブル★

リンク元	「セロトニン受容体」「8-ヒドロキシDPAT」「8-hydroxy-2-(di-n-propylamino)tetralin」
関連記事	「DP」「OH」「O」

「セロトニン受容体」

8-OH-DPAT
	Systematic name 7-(Dipropylamino)-5,6,7,8-tetrahydronaphthalen-1-ol
Identifiers
Abbreviations	8-OH-DPAT
CAS number	78950-78-4
PubChem	1220, 6603866 (R), 10125797 (S)
ChemSpider	1183 , 5036174 (R) , 8301316 (S)
MeSH	8-Hydroxy-2-(di-n-propylamino)tetralin
ChEBI	CHEBI:73364
ChEMBL	CHEMBL56
IUPHAR ligand	7
Jmol-3D images	Image 1; Image 2
	SMILES CCCN(CCC)C1CCc2cccc(O)c2C1 CCCN(CCC)C1CCC2=C(C1)C(O)=CC=C2 ;
	InChI InChI=1S/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 ; Key: ASXGJMSKWNBENU-UHFFFAOYSA-N 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; Key: ASXGJMSKWNBENU-UHFFFAOYAY ;
Properties
Molecular formula	C16H25NO
Molar mass	247.38 g mol−1
log P	3.711
Acidity (pKa)	10.539
Basicity (pKb)	3.458
Pharmacology
Elimination; half-life	1.5 hours
	Except where noted otherwise, data are given for materials in their standard state (at 25 °C (77 °F), 100 kPa)
	(verify) (what is: /?)
	Infobox references

　　[★]

英: serotonin receptor
同: 5-HT受容体
関: セロトニン

セロトニン受容体 (GOO.300)

サブタイプ	シグナル	局在	機能	生体反応	選択的作動薬	選択的阻害薬
5-HT_1A	AC↓	縫線核海馬	自己受容体		8-OH-DPAT tandospirone
5-HT_1B	AC↓	鉤状回黒質	自己受容体
5-HT_1C	AC↓	脳血管	血管収縮
5-HT_1D	AC↓	皮質線条体	-		sumatriptan
5-HT_1E	AC↓	脳および末梢	-
5-HT_2A	PLC↑	血小板平滑筋大脳皮質	血小板凝集収縮神経興奮		α-methtl-5-HT, DOI	スピペロン ketanserin
5-HT_2B	PLC↑	胃底	収縮		α-methtl-5-HT, DOI
5-HT_2C	PLC↑	脈絡叢	-		α-methtl-5-HT, DOI
5-HT₃	ion channel	末梢神経	神経興奮		2-methyl-5-HT	ondansetron tropisetron
		腸神経細胞		嘔吐
		最後野		嘔吐
5-HT₄	AC↑	胃腸管	神経興奮		renzapride
5-HT₄	AC↑	海馬	神経興奮	認知	renzapride
5-HT_5A	AC↓
5-HT_5B	?	海馬	？
5-HT₆	AC↑	線条体	？
5-HT₇	AC↑	脳下垂体小腸	？

5-HT₃受容体はリガンドの結合により開閉してNa+, K+の等価に関わる。ニコチン性受容体に似ている。(GOO.299)

セロトニン受容体

5-HT₁受容体

5-HT_1A

リガンドの結合に共役してK+チャネルを開口→過分極→電位依存性カルシウムチャネルを抑制
脳幹の縫線核、に局在

鎮静作用をしめすセロトニン作動性ニューロンが存在

somatodendritic 5-HT_1A autoreceptors descrease raphe cell fireing when activated by 5-HT released from axon collaterals of the same or adjacent neurons. (GOO.301)