5-ht2 (human)

Cloroperone has anxiolytic activity and may be used in the study of neurologic disorders.

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.

LY266097 hydrochloride (LY 266097 hydrochloride) is an antagonist of 5-HT2 with pKis of 7.7, 9.8, and 7.6 for human 5-HT2A, 5-HT2B, and 5-HT2C and can be used in studies about depression.

L-745870 hydrochloride has excellent brain penetration. L-745870 hydrochloride is a high-affinity, selective and orally active human dopamine D4 receptor antagonist with a Ki of 0.43 nM, and considerably weaker D2 receptor affinity with a Ki of 960 nM and D3 receptor affinity with a Ki of 2300 nM. 

Loxapine succinate (Loxapac), a D2DR and D4DR inhibitor, is utilized in schizophrenia.

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).

AL-34662 (formate) is a 5-HT2 receptor agonist with an IC50 of 0.8-1.5 nM. It stimulates phosphoinositol turnover and Ca2+ release in human ciliary muscle cells (h-CM) with an E50 of 289 nM and in human trabecular meshwork cells (h-TM) with an E50 of 254 nM. It is used in research on reducing intraocular pressure (IOP).

Loxapine is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent,used primarily in the treatment of schizophrenia. The drug is a member of the dibenzoxazepine class and structurally related to clozapine (which belongs to the chemically akin class of dibenzodiazepines).

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.

SUN-C5174 is a sleective 5-HT2 antagonist (pA2=8.98+/-0.06). SUN C5174 showed a marked inhibitory effect on the platelet aggregation induced by serotonin in combination with collagen and adenosine diphosphate (ADP) in canine or human platelet-rich plasma

AL-38022A is a novel synthetic serotonergic (5-HT) ligand that exhibited high affinity for each of the 5-HT2 receptor subtypes (Ki100-fold less) affinity for other 5-HT receptors. In addition, AL-38022A displayed a very low affinity for a broad array of other receptors, neurotransmitter transport sites, ion channels, and second messenger elements, making it a relatively selective agent. AL-38022A potently stimulated functional responses via native and cloned rat (EC50 range: 1.9-22.5 nM) and human (EC50 range: 0.5-2.2 nM) 5-HT2 receptor subtypes including [Ca2+]i mobilization and tissue contractions with apparently similar potencies and intrinsic activities and was a full agonist at all 5-HT2 receptor subtypes.

SB 206553 is a 5-HT2C inverse agonist that can attenuate methamphetamine-seeking behavior in rats. It exhibits activity for 5-HT2 receptor ligands with pKi values of 5.6 nM (5-HT2A), 7.7 nM (5-HT2B), and 7.8 nM (5-HT2C) in HEK-293 or CHO-K1 cells expressing human recombinant 5-HT2 receptors. SB 206553 can be used for research into psychostimulant abuse disorders [1].