Title : Interaction of the beta adrenergic receptor antagonist bucindolol with serotonergic receptors.

Pub. Date : 2000 Jan

PMID : 10630730






3 Functional Relationships(s)
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1 Because some beta-adrenergic receptor antagonists such as cyanopindolol are used as 5-HT1A/5-HT1B receptor antagonists, we tested the hypothesis that bucindolol can interact with 5-HT receptors. bucindolol 5-hydroxytryptamine receptor 1A Rattus norvegicus
2 In binding studies, bucindolol displayed high affinity for the 5-HT1A receptor (Ki, 11 nM), modest affinity for the 5-HT2A receptor (Ki, 382 nM), and no measurable affinity for the 5-HT1D receptor; binding affinity for the 5-HT2B receptor was not studied. bucindolol 5-hydroxytryptamine receptor 1A Rattus norvegicus
3 Thus, these data suggest that bucindolol lacks the ability to activate the 5-HT1A, 5-HT1D, 5-HT2A, and 5-HT2B receptor, but can block alpha1-adrenergic receptors and act as a weak 5-HT2A- and 5-HT2B-receptor antagonist. bucindolol 5-hydroxytryptamine receptor 1A Rattus norvegicus