Pharmacodynamics Bormocriptine in a dopamine receptor bound conformation<unk>  is a partial agonist of the dopamine D2 receptor. It also interacts with other dopamine receptors and with various serotonin and adrenergic receptors.<unk>  has additionally been found to inhibit the release of glutamate by reversing the GLT1 glutamate transporter. As an antagonist of the serotonin 5-HT2B receptor,<unk>  has not been associated with cardiac valvulopathy. This is in contrast to other ergolines acting instead as 5-HT2B receptor agonists such as cabergoline and pergolide but is similar to lisuride which likewise acts as a 5-HT2B receptor antagonist. + Site Affinity (Ki nM) Efficacy (Emax %) Action D1 692 ? ? D2S 5.0 41 Partial agonist D2L 15 28 Partial agonist D3 6.8 68 Partial agonist D4 372 0 Silent antagonist D5 537 ? ? 5-HT1A 13 72 Partial agonist 5-HT1B 355 66 Partial agonist 5-HT1D 11 86 Partial agonist 5-HT2A 107 69 Partial agonist 5-HT2B 56 0 Silent antagonist 5-HT2C 741 79 Partial agonist 5-HT6 33 ? ? 5-HT7 11–126 ? ? α1A 4.2 0 Silent antagonist α1B 1.4 ? ? α1D 1.1 ? ? α2A 11 0 Silent antagonist α2B 35 0 Silent antagonist α2C 28 0 Silent antagonist α2D 68 ? ? β1 589 ? ? β2 741 ? ? H1 >10,000 – – M1 >10,000 – – Notes: All receptors are human except α2D-adrenergic, which is rat (no human counterpart), and 5-HT7, which is rat/mouse.
Bromocriptine
Tropisetron
Sertindole
Granisetron
Iobitridol
Agomelatine
Carbidopa/levodopa
Cilansetron