Manufacturer |
Selleckchem
|
Category |
|
Type |
Inhibitors |
Specific against |
other |
Amount |
50 mg |
Item no. |
S2849-50 |
CASRN |
261901-57-9 |
eClass 6.1 |
30220300 |
eClass 9.0 |
32160605 |
Available |
|
Administration |
i.p. |
Animal Models |
C57BL6/J mice |
Chemical Name |
Phenol, 3-[[(2R)-2-[2-(4-methyl-1-piperidinyl)ethyl]-1-pyrrolidinyl]sulfonyl]-, hydrochloride (1:1) |
Description |
SB-269970 HCl is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3. |
Dosages |
10 mg/kg, 30 mg/kg |
Features |
SB-269970 HCl is a hydrochloride salt form of SB-269970 which is a potent 5-HT 7 receptor antagonist. |
Formulation |
Dissolved in saline |
IC50 |
8.3 (pKi) [1], 8.3 (pKi) [1], 8.3 (pKi) [1], 8.3 (pKi) [1], 8.3 (pKi) [1], 8.3 (pKi) [1] |
In vitro |
SB-269970 inhibits 5-CT-stimulated adenylyl cyclase activity in guinea-pig hippocampal membranes. SB-269970 (0.03 uM, 0.1 uM, 0.3 uM and 1 uM) produces a concentration-related rightward-shift of the 5-CT concentration-response curve with no significant alteration in the maximal response to 5-CT. [1] SB-269970 (1 uM) has any effect on 5-HT efflux when superfused alone. [2] |
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. [3] 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. [4] 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. [5] SB-269970 at doses of 0.3, 1 and 3 ug exhibits an anticonflict effect which is weaker than that of diazepam (40 ug), whereas SB-269970 at doses of 3 and 10 ug had marked anti-immobility action comparable to that of imipramine (0.1 ug). [6] |
Molecular Weight (MW) |
388, 95 |
Picture ChemicalStructure Description |
SB-269970 HCl Chemical Structure |
Solubility (25C) |
DMSO 11 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL |
Storage |
2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO |
Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.
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