Identification | Back Directory | [Name]
SB269970 HCl | [CAS]
261901-57-9 | [Synonyms]
SB-269970A SB269970 HCl USP/EP/BP SB269970 HClSB269970 HCl SB269970 HCl (SB-269970A) SB269970 hydrochloride, >=98% (r)-3-[2-[2-(4-methylpiperidin-1-yl)ethyl]pyrrolidine-1-sulfonyl]phenol hydrochloride (R)-3-((2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)phenol hydrochloride (2R)-1-[(3-Hydroxyphenyl)sulfonyl]-2-[2-(4-methyl-1-piperidinyl)ethyl]pyrrolidine monohydrochloride Phenol, 3-[[(2R)-2-[2-(4-methyl-1-piperidinyl)ethyl]-1-pyrrolidinyl]sulfonyl]-, hydrochloride (1:1) SB 269970A, (R)-3-[2-[2-(4-Methylpiperidin-1-yl)ethyl]pyrrolidine-1-sulfonyl]phenol hydrochloride | [Molecular Formula]
C18H28N2O3SHCl | [MDL Number]
MFCD03788020 | [MOL File]
261901-57-9.mol |
Hazard Information | Back Directory | [Description]
The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated by at least seven major 5-HT receptor subtypes. SB-269970 is a potent 5-HT7A antagonist (pKi = 8.9) that demonstrates >50-fold binding selectivity over 5-HT5A and >250-fold selectivity over 5-HT1, 5-HT2, 5-HT4, 5-HT6, adrenergic α1, dopamine D2, and dopamine D3 receptors. It is also reported to block adrenergic α2 receptors in guinea pig vas deferens. SB-269970 has been used to target the 5-HT7 receptor in the study of schizophrenia-like cognitive deficits. | [Uses]
SB 269970A is a selective 5-HT7 receptor antagonist. | [General Description]
A selective 5-HT7 receptor antagonist. Extremely potent in vivo and in vitro. Chronic or acute (even single dose) administration of SB269970 induces functional desensitization of the 5-HT7 receptor system, which precedes changes in the receptor density. This mechanism may be responsible for the rapid antidepressant-like effect of the 5-HT7 antagonist in animal models. SB-269970 is an analogue of SB-258719 and has been shown to have at least 100 fold selectivity versus all other 5-HT receptor subtypes except the human 5-HT5A receptor (pKi values are 8.9, 7.2 and 6.0 for 5-HT7A, 5-HT5A and 5-HT1B). | [Biochem/physiol Actions]
Primary Target5-HT | [storage]
+4°C | [References]
[1] hagan j j, price g w, jeffrey p, et al. characterization of sb-269970-a, a selective 5-ht7 receptor antagonist. british journal of pharmacology, 2000, 130(3): 539-548. |
|
Company Name: |
Sigma-Aldrich
|
Tel: |
021-61415566 800-8193336 |
Website: |
https://www.sigmaaldrich.cn |
Company Name: |
SPIRO PHARMA
|
Tel: |
|
Website: |
www.spiropharma.com.cn |
|