関: 8-OH-DPAT

WordNet

go `ding dong, like a bell (同)dong, dingdong
a ringing sound
the 14th letter of the Roman alphabet (同)n
being or containing a hydroxyl group

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〈鐘など〉‘を'ガンガン鳴らす / 〈鐘などが〉ガンガン鳴る / (鐘の)ガンガン鳴る音
nitrogenの化学記号
(おもに人称代名詞・固有名詞(人名),thereの後で)had, wouldの短縮形 / (疑問文でwhere,what,whenの後で)didの短縮形;Where'd he go?=Where did he go?
Department of the Interior 内務省 / drill instructor 教練係下士官 / discomfort index

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/10/27 10:40:16」(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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English Journal

Serotonin in the dorsal periaqueductal gray inhibits panic-like defensive behaviors in rats exposed to acute hypoxia.

Spiacci A Junior1, de Oliveira Sergio T1, da Silva GS2, Glass ML2, Schenberg LC3, Garcia-Cairasco N2, Zangrossi H Junior4.
Neuroscience.Neuroscience.2015 Aug 28. pii: S0306-4522(15)00777-0. doi: 10.1016/j.neuroscience.2015.08.045. [Epub ahead of print]
It has been proposed that spontaneous panic attacks are the outcome of the misfiring of an evolved suffocation alarm system. Evidence gathered in the last year is suggestive that the dorsal periaqueductal gray (dPAG) in the midbrain harbors a hypoxia-sensitive suffocation alarm system. We here inves
PMID 26319117

Systemic treatment with a 5HT1a agonist induces anti-oxidant protection and preserves the retina from mitochondrial oxidative stress.

Biswal MR1, Ahmed CM1, Ildefonso CJ1, Han P1, Li H1, Jivanji H1, Mao H1, Lewin AS2.
Experimental eye research.Exp Eye Res.2015 Aug 25;140:94-105. doi: 10.1016/j.exer.2015.07.022. [Epub ahead of print]
Chronic oxidative stress contributes to age related diseases including age related macular degeneration (AMD). Earlier work showed that the 5-hydroxy-tryptamine 1a (5HT1a) receptor agonist 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT) protects retinal pigment epithelium (RPE) cells from hydrog
PMID 26315784

Interaction between anti-Alzheimer and antipsychotic drugs in modulating extrapyramidal motor disorders in mice.

Shimizu S1, Mizuguchi Y1, Sobue A1, Fujiwara M1, Morimoto T1, Ohno Y2.
Journal of pharmacological sciences.J Pharmacol Sci.2015 Apr;127(4):439-45. doi: 10.1016/j.jphs.2015.03.004. Epub 2015 Mar 20.
Antipsychotics are often used in conjunction with anti-Alzheimer drugs to treat the behavioral and psychological symptoms of dementia (BPSD). Here, we examined the effects of cholinesterase inhibitors (ChEIs), donepezil and galantamine, on antipsychotic-induced extrapyramidal side effects (EPS) in m
PMID 25850380

Japanese Journal

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
… To explore the role of the serotonergic system in modulating absence seizures, we examined the effects of 5-HT1A and 5-HT2 agonists on the incidence of spike-and-wave discharges (SWD) in Groogy (GRY) rats, a novel rat model of absence-like epilepsy. …
NAID 10029889960

Early postnatal stress affects 5-HT1A receptor function in the medial prefrontal cortex in adult rats

Matsuzaki Hirokazu,Izumi Takeshi,Matsumoto Machiko,Togashi Hiroko,Yamaguchi Taku,Yoshida Takayuki,Watanabe Masahiko,Yoshioka Mitsuhiro
European Journal of Pharmacology 615(1-3), 76-82, 2009-08-01
… During the postadolescent period (10-14 weeks postnatal), immunohistochemical experiments were carried out to investigate c-Fos expression following the administration of R-(+)-8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT), a 5-HT1A receptor agonist. …
NAID 120001452160

「n」

8-OH-DPAT
Names
	Systematic IUPAC name 7-(Dipropylamino)-5,6,7,8-tetrahydronaphthalen-1-ol
Identifiers
CAS Registry Number	78950-78-4
Abbreviations	8-OH-DPAT
ChEBI	CHEBI:73364
ChEMBL	ChEMBL56
ChemSpider	1183 ; 5036174 (R) ; 8301316 (S)
	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 ;
IUPHAR/BPS	7
Jmol-3D images	Image; Image
MeSH	8-Hydroxy-2-(di-n-propylamino)tetralin
PubChem	1220; 6603866 (R); 10125797 (S)
	SMILES CCCN(CCC)C1CCc2cccc(O)c2C1 ; CCCN(CCC)C1CCC2=C(C1)C(O)=CC=C2 ;
Properties
Chemical formula	C16H25NO
Molar mass	247.38 g·mol−1
log P	3.711
Acidity (pKa)	10.539
Basicity (pKb)	3.458
Pharmacology
	Pharmacokinetics:
Biological half-life	1.5 hours
	Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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	Infobox references