SB269970 HCl Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
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-HT
1, 5-HT
2, 5-HT
4, 5-HT
6, adrenergic α
1, dopamine D
2, and dopamine D
3 receptors. It is also reported to block adrenergic α
2 receptors in guinea pig vas deferens. SB-269970 has been used to target the 5-HT
7 receptor in the study of schizophrenia-like cognitive deficits.
Verwenden
SB 269970A is a selective 5-HT7 receptor antagonist.
Allgemeine Beschreibung
A selective 5-HT
7 receptor antagonist. Extremely potent
in vivo and
in vitro. Chronic or acute (even single dose) administration of SB269970 induces functional desensitization of the 5-HT
7 receptor system, which precedes changes in the receptor density. This mechanism may be responsible for the rapid antidepressant-like effect of the 5-HT
7 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).
SB269970 HCl Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte