Abstract：
:[(3)H]Granisetron binding to 5-HT(3) type serotonin receptors was examined in homogenates of rat forebrain and NG 108-15 cells. We have applied an allosteric model to 5-HT(3) receptor binding for the first time. Slope factors of displacement improved the modelling. Serotonin displaced [(3)H]granisetron binding with micromolar potency in forebrain and with nanomolar potency in NG 108-15 cells. Racemic and (+)verapamil, ifenprodil and GYKI-46903 were used as representative allosteric inhibitors of 5-HT(3) receptors. They displaced [(3)H]granisetron binding with great negative cooperativity (alpha>10) and exerted great negative cooperativity with serotonin binding (beta>10). Great negative cooperativity of these agents with serotonin and [(3)H]granisetron binding cannot be distinguished from dual competitive displacement. Trichloroethanol (data from literature) had no cooperativity with [(3)H]granisetron binding (alpha~1) and exhibit positive cooperativity with serotonin (beta<1) in displacement. The allosteric model can lead to a more quantitative method in vitro to develop allosteric agents for 5-HT(3) receptors.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Maksay G,Bíró T,Bugovics Gdoi
10.1016/j.ejphar.2005.03.019keywords:
subject
Has Abstractpub_date
2005-05-02 00:00:00pages
17-24issue
1eissn
0014-2999issn
1879-0712pii
S0014-2999(05)00317-1journal_volume
514pub_type
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