8-OH-DPAT - CAS 78950-78-4
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
5-HT Receptor
8-OH-DPAT (8-Hydroxy-DPAT) is an agonist that has selectivity for 5-HT1A receptor (pIC50 = 8.19). It was subsequently found to be a serotonin reuptake inhibitor and a 5-HT7 receptor agonist as well. Studies showed that it exhibited antidepressant, anxiolytic and other properties.
Brife Description:
An agonist that has selectivity for 5-HT1A receptor (pIC50 = 8.19)
99.03 %
Solid Powder
8-HYDROXY-2-(DI-n-PROPYLAMINO)TETRALIN; 7-(dipropylamino)-5,6,7,8-tetrahydronaphthalen-1-ol; CHEMBL56; Ro-31-8220 in solution; 8-Hydroxy-DPAT
DMSO Solubility: 49 mg/mL (198.07 mM)
Store in a cool and dry place (or refer to the Certificate of Analysis).
Boiling Point:
372.5±42.0 °C at 760 mmHg
1.0±0.1 g/cm3
Canonical SMILES:
1.Effect of metergoline, fenfluramine, and 8-OHDPAT on catalepsy induced by haloperidol or morphine.
Broekkamp CL;Oosterloo SK;Berendsen HH;van Delft AM Naunyn Schmiedebergs Arch Pharmacol. 1988 Aug;338(2):191-5.
The influences of the indirect serotonin agonist fenfluramine (5; 10 mg/kg s.c.), the serotonin antagonist metergoline (5; 10 mg/kg s.c.) and the 5-HT1A agonist 8-OHDPAT (0.1; 0.2; 0.46 mg/kg s.c.) on haloperidol-induced catalepsy in rats or mice and on morphine-induced catalepsy in rats were studied. Morphine-induced catalepsy was enhanced by fenfluramine and attenuated by metergoline, whereas neither fenfluramine nor metergoline had any effect on haloperidol-induced catalepsy. 8-OHDPAT strongly antagonised catalepsy induced by morphine or haloperidol. We conclude that serotonergic transmission plays a major role in effectuating morphine catalepsy but not in effectuating haloperidol catalepsy. The antagonistic effect of 8-OHDPAT suggests a secondary, modulating role for 5-HT1A receptor mediated events in both types of catalepsy.
2.Cocaine conditioning: reversal by autoreceptor dose levels of 8-OHDPAT.
Carey RJ;Damianopoulos EN;Shanahan AB Pharmacol Biochem Behav. 2009 Jan;91(3):447-52. doi: 10.1016/j.pbb.2008.08.027. Epub 2008 Sep 9.
In order to investigate the contribution of serotonergic effects of cocaine to Pavlovian conditioning of cocaine locomotor stimulant effects, two experiments were conducted in which groups of rats (N=10) received cocaine treatments (10 mg/kg) paired or unpaired to placement in an open-field environment. Initially, a cocaine conditioned locomotion stimulant effect was established. Next, additional Coc-P and Coc-UP pairings were carried out in conjunction with pretreatment injections of the 5-HT1A agonist, 8-OHDPAT (0.01, 0.025 and 0.05 mg/kg) or saline. In experiment 1, the Coc-P group which received the saline pretreatment again exhibited conditioning but in the 8-OHDPAT pretreatment Coc-P group conditioning was eliminated. In the second experiment, the protocol of the first experiment was repeated but expanded in the post-conditioning phase to include an 8-OHDPAT plus the 5-HT1A antagonist pretreatment Coc-P group. As in the first experiment, the 8-OHDPAT pretreatment Coc-P group did not exhibit a cocaine conditioned locomotion stimulant effect; whereas, the saline pretreatment Coc-P and the 8-OHDPAT plus WAY-100635 pretreatment Coc-P groups did exhibit the cocaine conditioned locomotion stimulant effect.
3.Inhibition of 8-OH-DPAT-induced elevation of plasma corticotrophin by the 5-HT1A receptor antagonist WAY100635.
Critchley DJ;Childs KJ;Middlefell VC;Dourish CT Eur J Pharmacol. 1994 Oct 13;264(1):95-7.
Numerous studies have demonstrated the stimulatory effect of 5-HT1A receptor agonists, such as 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), on plasma corticotrophin (ACTH) levels in the rat. However, until recently the lack of a selective 5-HT1A receptor antagonist has hampered mechanistic studies in this area. In this study we examined the effects of the selective 5-HT1A receptor antagonist N-[2-[4-(2-methoxyphenyl)-1- piperazinyl]ethyl]-N-(2-pyridinyl) cyclohexanecarboxamide trihydrochloride (WAY100635) on plasma ACTH levels and on the elevation of ACTH induced by the 5-HT1A receptor agonist 8-OH-DPAT in the conscious rat. The basal plasma ACTH level was 41.0 +/- 1.8 pg/ml. 8-OH-DPAT increased ACTH levels at doses of 100 and 300 micrograms/kg with maximum increases of 551 and 546% respectively occurring 10 min post-injection. WAY100635 had no effects per se on plasma ACTH at doses up to 100 micrograms/kg, indicating it has no 5-HT1A receptor agonist properties. WAY100635 dose-dependently blocked the elevation of ACTH induced by 8-OH-DPAT, the minimum effective dose being 10 micrograms/kg. The present results indicate that 8-OH-DPAT elevates plasma ACTH levels by stimulating 5-HT1A receptors, a conclusion that is consistent with the findings of previous studies using non-selective 5-HT1A receptor antagonists such as pindolol.
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CAS 78950-78-4 8-OH-DPAT

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