5-ht2a receptor

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).

cis-Urocanic acid ((E)-Urocanic acid) is a 5-HT2A receptor agonist (Kd: 4.6 nM). It is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.

Deramciclane has high affinity for 5-HT2A and 5-HT2C receptors. It acts as an antagonist in both receptor subtypes and has inverse agonist properties for 5-HT2C receptors, but no direct stimulant agonists.

Tedatioxetine hydrobromide (Lu AA 24530 hydrobromide) is a serotonin-norepinephrine-dopamine reuptake inhibitor and an antagonist of 5-HT2A, 5-HT2C, 5-HT3, and α1A-adrenergic receptors, which can be used to treat depression and anxiety.

Abaperidone is a potent 5-HT2A receptor and dopamine D2 receptor antagonist with an IC50 of 6.2 for 5-HT2A receptors and 17 nM for dopamine D2 receptors.Abaperidone is a potentially atypical anti-psychotropic compound that reduces basal hsp70 mRNA expression in rat striatum and prefrontal cortex. expression in the striatum and prefrontal cortex of rats.

Temanogrel (APD791) is a highly selective antagonist of the 5-HT2A receptor (Ki: 4.9 nM).

Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand [125I-ICYP] to [5HT1B-serotonergic] receptor sites. It is an antihypertensive agent.

Eplivanserin mixture is a selective serotonin reuptake inhibitor and a 5-HT2A receptor antagonist,

NRA-0160 is a selective antagonist of dopamine D4 receptor(Ki of 0.48 nM)

Pipamperone (McN-JR 3345) binds 5-HT2A closely as receptor.

Pimethixene (Calmixen) is a highly potent 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors antagonist(pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively).

Pimethixene maleate (Pimetixene maleate) is a potent 5-HT2B receptor antagonist with sedative and antitussive activity.Pimethixene maleate inhibits 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2, and can be used in studies of dry and irritant cough in children. irritant cough in children.

SEP-363856 is an agent of orally active and CNS active psychotropic with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects, has the potential to treatment of schizophrenia.

SEP-363856 hydrochloride (SEP-856 hydrochloride) is an orally active, CNS-active psychotropic agent with a unique non-D2/5-HT2A mechanism of action, demonstrating antipsychotic-like effects and potential for schizophrenia treatment.

Brilaroxazine (RP5063) is a potent multimodal dopamine/5-HT modulator. Brilaroxazine is a partial agonist of dopamine D2, D3, and D4 receptors, 5-HT1A (Ki =1.5 nM) and 5-HT2A (Ki = 2.5 nM), and has antagonist activity 5-HT2B, and 5-HT7 receptors with Kis of 0.19 nM and 2.7 nM, respectively. Brilaroxazine can be used for research about cognitive impairments in neuropsychiatric and neurological diseases.

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.

GR 113808 is a selective 5-HT4 receptor antagonist that inhibits 5-HT1B, 5-HT2A, 5-HT2C, and 5-HT3 receptors, and attenuates dopamine release.

Iferanserin (S-MPEC) is a selective antagonist of the serotonin (5-HT) receptor with a specific affinity for 5-HT2A receptors, showing potential for the treatment of internal hemorrhoid disease.

Lidanserin is an antagonist of the 5-HT2A and α1-adrenergic receptor.

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).

SB228357 is a potent and selective antagonist of the 5-HT receptor with pKis of 6.9, 8.0, and 9.0 for 5-HT2A, 5-HT2B, and 5-HT2C, respectively.

YM348 is an effective and orally active 5-HT2C receptor agonist. YM348 also shows a high affinity for the cloned human 5-HT2C receptor (Ki: 0.89 nM).

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].