5-ht2 receptor

IrindaloneIrindalone is a potent serotonin (5-HT2) antagonist.

Nexopamil racemate((Rac)-Nexopamil) is a racemate of Nexopamil. The Nexopamil racemate has potential anti-asthmatic and anti-ulcer activity.

Eplivanserin (SR-46349) is an effective and selective antagonist of 5-HT2A receptor with a Kd of 1.14 nM and an IC50 value of 5.8 nM in rat cortical membrane.

Mirtazapine-D3 is a deuterium labeled Mirtazapine. Mirtazapine is an inhibitor of 5-HT receptor .

(S)-Mirtazapine ((S)-Org3770) is the S(+)-enantiomer of Mirtazapine, functioning as a selective 5-HT2 receptor antagonist with pro-nociceptive effects. It is commonly used in combination with the R(-)-enantiomer of Mirtazapine to study depression.

(S)-Mirtazapine-D3 is a deuterium labeled  (S)-Mirtazapine (T12632L). (S)-Mirtazapine is a stereoselective antagonist of 5-HT2 receptor. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2.

Cinanserin hydrochloride (SQ 10643), a high-affinity antagonist of the 5-HT2 receptor (Ki: 41 nM), is also a 3C-like protease inhibitor of severe acute respiratory syndrome coronavirus.

Fananserin is an effective, selective and oral active antagonist of 5-HT2 (Ki = 0.37 nM for the rat 5-HT2A). Fananserin is an antagonist of human D4 receptor (Ki = 2.93 nM).

Ritanserin (R 55667) is a long-acting, highly potent, relatively selective, orally bioavailable 5-HT2 receptor antagonist with an IC50 of 0.9 nM.

Adatanserin (WY 50324) is a mixed 5-HT1A receptor partial agonist and a 5-HT2A and 5-HT2C receptor antagonist with potential neuroprotective activity for the study of coke oven and depression.

Mirtazapine (6-Azamianserin) is a tetracyclic antidepressant with a somewhat unique mechanism of action. Mirtazapine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.

Trimipramine maleate (Surmontil maleate) appears to inhibit serotonin transport and norepinephrine uptake by nerve terminals. This increases available norepinephrine or serotonin and prolongs its action. Trimipramine Maleate is the maleate salt form of trimipramine, a tricyclic secondary amine of the dibenzazepine class, with an antidepressant property.

Iloperidone (HP 873) is an atypical antipsychotic agent that is used for treatment of schizophrenia.

Trimipramine is an antidepressant with an anxiety-reducing sedative component to its action.

AMI-193 (Spiramide) is an effective and selective antagonist of 5-HT2 and D2 receptor with Kis of 2, 3, 50, 2530, and 4300 nM for 5-HT2, D2 Receptor, 5-HT1A, D1 Receptor, and 5-HT1C Receptor. AMI-193 shows antipsychotic activity.

AL 34662 is a selective and potent 5-HT2A receptor agonist with IC50s of 0.77 nM and 1.5 nM for rat and human 5-HT2 receptors, respectively.AL 34662 is also a low affinity α-1D adrenergic agonist, with an EC50 of 0.4 μM.AL 34662 can be used to lower intraocular pressure.

Iloperidone hydrochloride is a D(2)/5-HT(2) receptor antagonist. It is also an atypical antipsychotic for the treatment of schizophrenia symptoms.

CB1 receptor antagonist/inverse agonist

D1-like dopamine receptor antagonist

Spiroxatrine (R 5188) is a selective and potent 5-HT1α and α2-adrenergic dual antagonist with sedative activity, and inhibitory effects on 5-HT1α, 5-HT1β, 5-HT2, and dopamine receptors. Spiroxatrine may be used in the study of disorders related to the cardiovascular system.

Etoperidone hydrochloride is an antidepressant agent.

Volinanserin (MDL100907) (MDL 100907) is a potent and selective antagonist of the serotonin receptor 5-HT2 (Ki: 0.36 nM) and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 adrenergic and sigma receptors.

Risperidone hydrochloride (R 64 766 hydrochloride) is a 5-HT2 receptor blocker, P-glycoprotein inhibitor, and dopamine D2 receptor antagonist, with activity on 5-HT2A (Ki: 4.8 nM) and dopamine D2 (Ki: 5.9 nM) receptors.

Ziprasidone (CP-88059) mesylate is an orally active 5-HT and dopamine receptor antagonist with affinity for D2, 5-HT2A, and 5-HT1A receptors in rats, exhibiting Ki values of 4.8 nM, 0.42 nM, and 3.4 nM, respectively.