5-ht2a

5-HT1A modulator 1 exhibits high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM).

PNU-96391 (OSU-6162) is an antagonist of dopamine D2 and a partial agonist of 5-HT2A. PNU-96391 can be used in research on the treatment of chronic diseases.

Ketanserin (Ketanserinum) is a quinazoline derivative and serotonin (5-hydroxytryptamine, 5HT) receptor subtype 2 (5-HTR2) antagonist with potential antihypertensive and antiplatelet activities. Following administration, ketanserin binds to and inhibits the signaling mediated by 5-HTR2, which inhibits serotonin-dependent vasoconstriction and platelet activation.

Asenapine Maleate (Org 5222 maleate) is a second generation (atypical) antipsychotic agent that is taken sublingually and used in the treatment of schizophrenia and manic or mixed episodes associated with bipolar 1 disorder. Asenapine is associated with a low rate of transient and mild serum aminotransferase elevations during therapy but has not been linked to instances of clinically apparent acute liver injury.

Ziprasidone hydrochloride (CP-88059 hydrochloride) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity.

Risperidone (R 64 766) is a selective blocker of dopamine D2 receptors and serotonin 5-HT2 receptors that act as an atypical antipsychotic agent.

Elemicin (Elemicine) is a constituent of several plant species' essential oils with anticholinergic effects in human.

Sarpogrelate hydrochloride (MCI-9042) , a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. Target: 5-HT2 Recepter Sarpogrelate is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. Sarpogrelate hydrochloride was shown to have the same affinity as ritanserin for 5-HT2A receptors, with a Ki value of 8.39 nM. Sarpogrelate hydrochloride lacked prominent 5-HT1-like, 5-HT3, beta, H1, H2 and M3 antagonist activity and weakly blocked alpha 1-adrenoceptors (pKB = 6.30). (S)-M-1 showed weak affinity for 5-HT1-like receptors (pKB = 6.30), alpha 1- (pKB = 6.80) and beta- (pKB = 6.54) adrenoceptors, while (R)-M-1 was a weak antagonist at histamine H1 receptors (pKB = 6.49). After 12 weeks of sarpogrelate administration, FBF and LBF responses during RH showed significant increases from 13.2 + - 1.7 to 18.1 + - 2.2 mL min per 100 mL tissue (P < 0.01) and from 8.2 + - 0.9 to 14.2 + - 2.1 mL min per 100 mL tissue (P < 0.05), respectively. Sarpogrelate hydrochloride -induced augmentation of FBF and LBF responses to RH was maintained at 24 weeks. Long-term oral administration of sarpogrelate improves vascular function in patients with PAD.

Quetiapine hemifumarate (ICI-204636), an atypical antipsychotic, is used in the treatment of bipolar I mania, schizophrenia, bipolar II depression, bipolar I depression.

Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

Perospirone (Lullan) is an antagonist of serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist.

Quetiapine (ICI204636) is used for the therapy of schizophrenia, and for the treatment of acute manic episodes associated with bipolar I disorder. The mechanism of quetiapine' action is thought by mediated through antagonist activity at serotonin and dopamine receptors. Specifically, the D1 and D2 dopamine, the α1 adrenoreceptor and α2 adrenoreceptor, and 5-HT1A and 5-HT2 serotonin receptor subtypes are antagonized. Quetiapine also can inhibit the histamine H1 receptor.

Spiperone (Spiropitan) is a spiro butyrophenone analog similar to HALOPERIDOL and other related compounds. It has been recommended in the treatment of SCHIZOPHRENIA.

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.

Cyamemazine is an antipsychotic compound with sedative and anxiolytic activity. Cyamemazine is a 5-HT3, 5-HT2A, and 5-HT2C receptor antagonist with Ki values of 12 nM, 1.5 nM, and 75 nM, respectively.

Org-12962 is an effective and selective 5-HT2C receptor agonist pEC50: 7.01). Org-12962 shows antiaversive effects in a rat model of panic-like anxiety. Org-12962 also shows high effacy for the 5-HT2A and 5-HT2B receptors (pEC50s: 6.38 and 6.28, respectively).

Lumateperone (ITI 722) is a 5HT2A receptor antagonist and a dopamine receptor phosphoprotein modulator (DPPM).

lumateperone Tosylate (ITI-007) is a 5-HT2A receptor antagonist (Ki: 0.54 nM), a SERT blocker (Ki: 61 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki: 32 nM).

Tabernanthalog (TBG) is a 5-HT2A agonist. In rodents,Tabernanthalog has been found to promote structural neuroplasticity, reduce alcohol-seeking and heroin-seeking behavior, and produce antidepressant effects.

Nuciferine ((-)-Nuciferine) is an alkaloid found within the plants Nymphaea caerulea and Nelumbo nucifera. It has a profile of action associated with dopamine receptor blockade.

5-HT2A antagonist 1 is a 5-HT2A receptor blocker that may be useful in treating gastrointestinal and circulatory disorders.

5-HT6 5-HT2A receptor ligand-1 (compound 33) is a dual antagonist for the 5-HT6 and 5-HT2A receptors, exhibiting K i values of 2 nM and 11 nM for the respective receptors, holding promise for research in neurological and psychiatric disorders [1].

Compound 42, a 5-HT6 5-HT2A receptor ligand-2, serves as a dual antagonist for the 5-HT6 and 5-HT2A receptors with Ki values of 25 nM and 32 nM, respectively. This brain-penetrant compound exhibits pro-cognitive properties [1].

5-HT2A receptor agonist-2 is a potent compound that acts as an agonist on the serotonin 5-HT2 receptor, specifically stimulating the 5-HT 2A, 5-HT 2B, and 5-HT 2C receptors with EC50 values of 1.7 nM, 0.58 nM, and 0.50 nM, respectively [1].