SB 204741 is potent and selective 5-HT2B receptor antagonist (pA2 = 7.95). It displays ≥ 135-fold selectivity over 5-HT2C (pKi = 5.82), 5-HT2A (pKi < 5.2), 5-HT1A, 1D, 1E, 5-HT3 and 5-HT4 receptors.

RU 24969 is a selective agonist of the 5-HT1A and 5-HT1B receptors.

Clozapine N-oxide is a major metabolite of clozapine noted to decrease SR-2A(5-HT2 serotonin receptor) density in vitro.

Asenapine Maleate is a 5-HT and dopamine D2 receptor antagonist used to treat schizophrenia and bipolar mania.

RS 127445 is a potent and selective antagonist at 5-HT2B receptor with pKi value of 9.5.

Geissoschizine methyl ether is a potent serotonin A receptor agonist.

Ritanserin is a serotonin receptor antagonist which was never marketed for clinical use but has been used in scientific research.

Aripiprazole lauroxil is a long-acting injectable atypical antipsychotic. It is an N-acyloxymethyl prodrug of aripiprazole that is administered via intramuscular injection once every four to six weeks for the treatment of schizophrenia.

CP 94253 HCl is a potent, selective 5-HT1B agonist with Ki of 2 nM.

Temanogrel is a highly selective 5-HT2A receptor antagonist with Ki of 4.9 nM.

Tianeptine is a unique tricyclic antidepressant, in contrast to SSRIs, which can increase serotonin uptake in the brain and reduce stress-induced atrophy of neuronal dendrites.

PRX-08066 is a novel 5-HT2B receptor antagonist with IC50 of 3.4 nM.

Pizotifen Malate is a benzocycloheptene-based drug used to reduce the frequency of recurrent migraine headacheswith, with high affinity for 5-HT and dopamine receptors (Kis = 7.94 and 2.4 nM for 5-HT2C and D2, respectively).

VUF10166 is a potent and competitive antagonist for 5-HT3A receptor with Ki of 0.04 nM, its affinity at 5-HT3AB receptor is significantly lower.

RS-127445 is a selective, high affinity and orally bioavailable serotonin 5-HT2B receptor antagonist. RS-127445 is found to have nanomolar affinity for the 5-HT2B receptor (pKi=9.5) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.