SB-334867

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

第一个选择性 Orexin-1 受体拮抗剂，pKb 为 7.4。

The first selective Orexin-1 receptor antagonist with pKb of 7.4; displays 50-fold selectivity over OX2 (pKb 5.7), >100-fold or selectivity over 5-HT2B, 5-HT2C and approximately 50 other molecular targets, in particular GPCRs and ion channels; possesses CNS penetration, in vivo activity following ip dosing.Obesity Preclinical.

SB-334867 (100?pM–?10?μM) inhibits the orexin-A (10?nM) and orexin-B (100?nM)-induced calcium responses in a concentration-dependent manner, with apparent pKb values of 7.27±0.04 and 7.23±0.03, but has no effect on the calcium response elicited by UTP (3?μM), which activates an endogenous purinergic receptor in CHO-OX1 and CHO-OX2 cells.

SB-334867 (intraperitoneal injection; 20?mg/kg; 20 days) administers 15?min before morphine injection can significantly decrease the effect of the morphine challenge dose in mice in comparison with the sporadically morphine-treated group.SB334867 (intraperitoneal injection; 3, 10 and 30 mg/kg) significantly reduces ethanol intake relative to vehicle and does not effect water consumption in female P rats.SB334867 (intraperitoneal injection; 3, 10 and 30 mg/kg) reduces ethanol consumption at the 30 mg/kg dose, high dose suppresses sucrose intake relative to vehicle, and it results in lowerblood ethanol concentrations (BECs) relative to both the 10 and 30 mg/kg doses. Animal Model:Male Swiss mice Dosage:20?mg/kg Administration:Intraperitoneal injection Result:Inhibited the acquisition of morphine-induced sensitization to locomotor activity of mice.Animal Model:C57BL/6J Mice Dosage:3, 10 and 30 mg/kg Administration:Intraperitoneal injection Result:Reduced ethanol consumption, BECs and suppressed sucrose intake in mice.

SB 334867A | SB334867 | SB 334867

GPCR/G Protein

Orexin Receptor

Orexin Receptor

Metabolic Disease

Obesity

249889-64-3

355.7784

C17H14ClN5O2

>98% (HPLC)

10 mM in DMSO

O=C(NC1=CC(OC(C)=N2)=C2C=C1)NC3=CC=NC4=CC=CN=C43.Cl

Urea, N-(2-methyl-6-benzoxazolyl)-N'-1,5-naphthyridin-4-yl-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years