Alniditan is a receptors agonist of 5-HT1B 1D in HEK 293 cells (IC50: 1.7 and 1.3 nM). For 5-HT1B 1D receptors, the pKi values are 8.96 and 9.40, respectively.
SB-277011 dihydrochloride is a potent, selective, orally bioavailable and brain penetrate antagonist of dopamine D3 receptor(pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively).
AR-A 2 is a selective 5-HT1Breceptor antagonist, with a high affinity to guinea pig cortex 5HT1B 1D and recombinant guinea pig 5-HT1Breceptors (Ki: 0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki: 5 nM).
SB 243213 dihydrochloride is an orally active, selective and high-affinity antagonist of 5-hydroxytryptamine (5-HT)2C receptor(pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor).
Sarizotan (EMD 128130) is an orally active compound that acts as an agonist for serotonin 5-HT 1A receptors and dopamine receptors. It has shown potent activity with IC 50 values of 6.5 nM for rat 5-HT 1A , 0.1 nM for human 5-HT 1A , 15.1 nM for rat D 2 , 17 nM for human D 2 , 6.8 nM for human D 3 , and 2.4 nM for human D 4.2 .