SB269970 HCl

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-HT_7A antagonist (pK_i = 8.9) that demonstrates >50-fold binding selectivity over 5-HT_5A 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-HT_5A receptor (pKi values are 8.9, 7.2 and 6.0 for 5-HT_7A, 5-HT_5A and 5-HT_1B).

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.