8-OH-DPAT (8-Hydroxy-DPAT) (Synonyms: 8-Hydroxy-DPAT) |
| Catalog No.GC30888 |
8-OH-DPAT (8-Hydroxy-DPAT) is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A and a Ki of 466 nM for 5-HT7; 8-OH-DPAT (8-Hydroxy-DPAT) weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).
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Cas No.: 78950-78-4
Sample solution is provided at 25 µL, 10mM.
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8-OH-DPAT, at a pIC50 of 8.19, exhibits robust and specific agonistic activity on 5-HT1A receptors, indicating high selectivity. However, 8-OH-DPAT shows only weak binding affinity towards 5-HT1B receptors (pIC50, 5.42) and minimal binding to 5-HT receptors (pIC50
Pretreatment of 8-OH-DPAT over the concentration range of 1-100µM significantly inhibited the H2O2 -induced neuronal cell death[3].8-OH-DPAT(10 µM;24 h) reduces lipofuscin accumulation in cultured RPE cells[4].
In rats administered with 8-OH-DPAT(0-0.1 mg/kg; s.c.;2h) and provided with wet mash, feeding and activity frequencies were increased, while resting and total grooming behaviors were inhibited in non-deprived conditions[5]. 8-OH-DPAT(0.5 mg/kg；s.c) enhanced QUIN' (an agonist quinpirole) and HAL's(a potent D₂ antagonist haloperidol) disruption of pup retrieval and pup preference, reversed the increase in hovering over pups induced by HAL in mice[6]. 8-OH-DPAT(0.2 and 0.4mg/kg i.p.) reduces competition from contextual but not discrete conditioning cues[7]. Systemically injected 8-OH-DPAT (0.4 mg/kg) decreased extracellular 5-HT levels in the medial preoptic area (MPOA) as measured by in vivo microdialysis[8].
References:
[1]. Middlemiss DN, Fozard JR. 8-Hydroxy-2-(di-n-propylamino)-tetralin discriminates between subtypes of the 5-HT1 recognition site. Eur J Pharmacol. 1983 May 20;90(1):151-3. doi: 10.1016/0014-2999(83)90230-3. PMID: 6223827.
[2]. Bard JA, Zgombick J, et,al. Cloning of a novel human serotonin receptor (5-HT7) positively linked to adenylate cyclase. J Biol Chem. 1993 Nov 5;268(31):23422-6. PMID: 8226867.
[3]. Lee HJ, Ban JY, et,al. Stimulation of 5-HT1A receptor with 8-OH-DPAT inhibits hydrogen peroxide-induced neurotoxicity in cultured rat cortical cells. Pharmacol Res. 2005 Mar;51(3):261-8. doi: 10.1016/j.phrs.2004.09.003. PMID: 15661577.
[4]. Thampi P, Rao HV, et,al. The 5HT1a receptor agonist 8-Oh DPAT induces protection from lipofuscin accumulation and oxidative stress in the retinal pigment epithelium. PLoS One. 2012;7(4):e34468. doi: 10.1371/journal.pone.0034468. Epub 2012 Apr 3. PMID: 22509307; PMCID: PMC3317995.
[5]. Hartley JE, Montgomery AM. 8-OH-DPAT inhibits both prandial and waterspray-induced grooming. J Psychopharmacol. 2008 Sep;22(7):746-52. doi: 10.1177/0269881107082903. Epub 2008 Feb 28. PMID: 18308782.
[6]. Cai Y, Zhang X, et,al. 8-OH-DPAT enhances dopamine D2-induced maternal disruption in rats. J Comp Physiol A Neuroethol Sens Neural Behav Physiol. 2022 Jul;208(4):467-477. doi: 10.1007/s00359-022-01551-4. Epub 2022 Apr 17. PMID: 35434766.
[7]. Cassaday HJ, Thur KE. Intraperitoneal 8-OH-DPAT reduces competition from contextual but not discrete conditioning cues. Pharmacol Biochem Behav. 2019 Dec;187:172797. doi: 10.1016/j.pbb.2019.172797. Epub 2019 Oct 24. PMID: 31669833; PMCID: PMC6899499.
[8]. Lorrain DS, Matuszewich L, et,al. 8-OH-DPAT influences extracellular levels of serotonin and dopamine in the medial preoptic area of male rats. Brain Res. 1998 Apr 20;790(1-2):217-23. doi: 10.1016/s0006-8993(98)00065-1. PMID: 9593901.
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