product name SB269970 HCl
Description: SB269970 HCl is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors. As a selective antagonist of 5-HT7 receptor, SB269970 shows at least 100-fold selective against 5-HT7 over a variety of receptors and enzymes. SB269970 also inhibits adenylyl cyclase activity stimulated by 5-CT both in 5-HT7(a)/ HEK293 (pA2 of 8.5) membranes and in guinea-pig hippocampus (pKB of 8.3).
References: Br J Pharmacol. 2000 Jun;130(3):539-48; Behav Pharmacol. 2008 Mar;19(2):153-9.
388.95
Formula
C18H28N2O3S.HCl
CAS No.
261901-57-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 11 mg/mL (28.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: SB-269970 inhibits 5-CT-stimulated adenylyl cyclase activity in guinea-pig hippocampal membranes. SB-269970 (0.03 μM, 0.1 μM, 0.3 μM and 1 μM) produces a concentration-related rightward-shift of the 5-CT concentration-response curve with no significant alteration in the maximal response to 5-CT. SB-269970 (1 μM) has any effect on 5-HT efflux when superfused alone. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | SB-269970 (10 mg/kg and 30 mg/kg) significantly reduces the effects of amphetamine by 25 and 27%, respectively, and blocks the effects of ketamine by 38% (10 mg/kg) and 30% (30 mg/kg). SB-269970 significantly reduces amphetamine-induced hyperactivity in wild-type mice and is without effects in 5-HT7 knockout mice. Systemic administration of SB-269970 (30 mg/kg) significantly reverses amphetamine disruption of PPI and did not enhance PPI by itself compared to control. SB-269970 significantly reverses the deficits induced by MK-801, but not by scopolamine. SB-269970 normalizes MK-801-induced glutamate but not dopamine release in the cortex. SB-269970 (in one medium dose of 0.5 or 1 mg/kg) exerts a specific antianxiety-like effect in the Vogel drinking test in rats, in the elevated plus-maze test in rats and in the four-plate test in mice. Moreover, SB-269970 (in one medium dose of 5 or 10 mg/kg) reveals antidepressant-like activity in the forced swimming and the tail suspension tests in mice. SB-269970 at doses of 0.3, 1 and 3 μg exhibits an anticonflict effect which is weaker than that of diazepam (40 μg), whereas SB-269970 at doses of 3 and 10 μg had marked anti-immobility action comparable to that of imipramine (0.1 μg). |
| Animal model | C57BL6/J mice |
| Formulation & Dosage | Dissolved in saline; 10 mg/kg, 30 mg/kg; i.p.injection |
| References | Br J Pharmacol. 2000 Jun;130(3):539-48; Behav Pharmacol. 2008 Mar;19(2):153-9. |
