MedChemExpress - Model 8-OH-DPAT -78950-78-4

8-OH-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 weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).

8-OH-DPAT

MCE China：8-OH-DPAT

Brand：MedChemExpress (MCE)

Cat. No.HY-112061

CAS：78950-78-4

Synonyms：8-Hydroxy-DPAT

Purity：99.26%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：8-OH-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 weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).

In Vitro：8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A; weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 [1]. 8-OH-DPAT has high affinity at 5-HT7 with a Ki of 466 nM, and does not bind to 5-HT6 or 5-HT4[2].

In Vivo：8-OH-DPAT (1 mg/kg) normalizes hypolocomotion, significantly increases wakefulness and reduces the duration of REM sleep without effect on the duration of non-REM sleep in the dark period in orexin knockout (KO) mice. 8-OH-DPAT shows no obvious effect on wakefulness or the duration of either REM sleep or non-REM sleep in WT mice. 8-OH-DPAT (1 mg/kg, s.c.) activates 5-HT1A receptor in orexin knockout mice[3].

Animal Administration：Mice[3] The locomotor activity of mice is measured by an infrared sensor placed in individual home cages. To compare the locomotor activity in the light and dark periods, locomotor activity is monitored at 30-min intervals starting at 8:00 a.m. and 8:00 p.m., respectively. To measure the effects of psychostimulants (8-OH-DPAT, 1, 3 mg/kg, s.c; etc.) on locomotor activity in the dark period, all drugs are administered at 8:00 p.m., and locomotor activity is then measured through 3 h[3].

IC50 & Target：5-HT1A Receptor 8.19 (pIC50) 5-HT7 Receptor 466 nM (Ki)

References：

[1]. DEREK N. MIDDLEMISS, et al. 8-HYDROXY-2-(DI-n-PROPYLAMINO)-TETRALIN DISCRIMINATES BETWEEN SUBTYPES OF

[2]. Bard JA, 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. [Content Brief]

[3]. Mori T, et al. Narcolepsy-like sleep disturbance in orexin knockout mice are normalized by the 5-HT1A receptor agonist 8-OH-DPAT. Psychopharmacology (Berl). 2016 Jun;233(12):2343-53. [Content Brief]

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MedChemExpress - Model 8-OH-DPAT -78950-78-4

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8-OH-DPAT