product name SB-334867 HCl
Description: SB-334867 HCl is a selective orexin-1 (OX1) receptor antagonist. It was the first non-peptide antagonist developed that is selective for the orexin receptor subtype OX1, with around 50x selectivity for OX1 over OX2 receptors. It has been shown to produce sedative and anorectic effects in animals, and has been useful in characterising the orexinergic regulation of brain systems involved with appetite and sleep, as well as other physiological processes.
References: Br J Pharmacol. 2001 Mar;132(6):1179-82; Neuropsychopharmacology. 2007 Apr;32(4):786-92.
319.32
Formula
C17H14NClN5O2
CAS No.
249889-64-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 63 mg/mL (197.3 mM)
Water: <1 mg/mL
Ethanol: 3 mg/mL (9.4 mM)
Solubility (In vivo)
1% CMC Na: 30 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: In CHO-OX1 cells, SB-334867 inhibits the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses with pKB of 7.27 and 7.23 respectively, without effect on the UTP (3 microM)-induced calcium response. Kinase Assay: Cell Assay: Orexin-A and orexin-B are two peptides isolated from rat hypothalamus. They are involved in some physiological functions such as the control of feeding, energy metabolism and regulation of the sleep-wake cycle. SB-334867 can inhibit the orexin-A and orexin-B induced calcium responses in CHO-OX1 cells with pKB values of 7.27 and 7.23, respectively. SB-334867 is more selective for OX1 receptor over OX2 receptor. It causes 32.7% and 22% inhibition of orexin-A and orexin-B induced calcium responses in CHO-OX2 cells, respectively. |
|---|---|
| In Vivo | In both male and female rats, SB-334867 (30 mg/kg, i.p.) significantly reduces natural and orexin-A-induced food intake. SB-334867 (2 mg/kg, i.v.) blocks the effects of antipsychotic drugs on dopamine neuronal activity in rats. SB-334867 also inhibits the development of morphine analgesic tolerance in rats. |
| Animal model | Male and female Sprague–Dawley rats |
| Formulation & Dosage | Dissolved in 10% (w/v) Encapsin in sterile water; 30 mg/kg; i.p. administration |
| References | Br J Pharmacol. 2001 Mar;132(6):1179-82; Regul Pept. 2000 Dec 22;96(1-2):45-51; Neuropsychopharmacology. 2007 Apr;32(4):786-92. |
