SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.

Product information

CAS Number: 249889-64-3

Molecular Weight: 355.78

Formula: C17H14ClN5O2

Chemical Name: 3-(2-methyl-1,3-benzoxazol-6-yl)-1-(1,5-naphthyridin-4-yl)urea hydrochloride

Smiles: Cl.CC1=NC2C=CC(=CC=2O1)NC(=O)NC1=CC=NC2=CC=CN=C12

InChiKey: BKZHSJNLPPAJKB-UHFFFAOYSA-N

InChi: InChI=1S/C17H13N5O2.ClH/c1-10-20-12-5-4-11(9-15(12)24-10)21-17(23)22-14-6-8-18-13-3-2-7-19-16(13)14;/h2-9H,1H3,(H2,18,21,22,23);1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 31.9 mg/mL (100 mM)), with gentle warming Ethanol: 3.2 mg/mL (10 mM)), with gentle warming

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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.

In Vivo:

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 lower blood ethanol concentrations (BECs) relative to both the 10 and 30 mg/kg doses.

References:

1. Smart D, et al. Br J Pharmacol. 2001, 132(6), 1179-1182.
2. Haynes AC, et al. Regul Pept. 2000, 96(1-2), 45-51.
3. Rasmussen K, et al. Neuropsychopharmacology. 2007, 32(4), 786-792.

Products are for research use only. Not for human use.