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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).