SB269970 HCl
SB269970 HCl Basic information
- Product Name:
- SB269970 HCl
- Synonyms:
-
- SB-269970A
- (R)-3-((2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidin-1-yl)sulfonyl)phenol hydrochloride
- (r)-3-[2-[2-(4-methylpiperidin-1-yl)ethyl]pyrrolidine-1-sulfonyl]phenol hydrochloride
- SB 269970A, (R)-3-[2-[2-(4-Methylpiperidin-1-yl)ethyl]pyrrolidine-1-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)
- SB269970 hydrochloride, >=98%
- SB269970 HClSB269970 HCl
- CAS:
- 261901-57-9
- MF:
- C18H28N2O3SHCl
- MW:
- 0
- Product Categories:
-
- Inhibitors
- Mol File:
- 261901-57-9.mol
SB269970 HCl Chemical Properties
- storage temp.
- 2-8°C
- solubility
- H2O: soluble10mg/mL, clear (warmed to 60 °C)
- form
- powder
- color
- White to off-white
SB269970 HCl Usage And Synthesis
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.
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