5-ht2a antagonist

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

5-HT2A antagonist 3 (Formula (III)) functions as both an antagonist and an inverse agonist of the 5-HT2A receptor, exhibiting a pIC50 value of 8.7 and a pKi value of 9. It is applicable for research in neuroscience.

5-HT2A antagonist 2 is an orally active, selective 5HT2A antagonist with an IC50 of 14 nM. It exhibits good chemical, hepatocyte, and plasma stability, without significant cytotoxicity in cell lines VERO, HFL-1, L929, NIH3T3, CHO-K1 [1].

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).

QF0301B is a potent α1-adrenergic receptor antagonist with inhibitory effects on α2-adrenergic receptors, 5-HT2A and histamine H1 receptors.

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.

dopamine D1 receptor antagonist

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.

LY-2624803 is a 5-HT2A receptor antagonist and histamine receptor inverse agonist that can be used to improve slow wave sleep.

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.

Perphenazine dihydrochloride is an orally active dopamine receptor and histamine-1 receptor antagonist that acts on D2 (Ki: 0.56 nM), D3 (Ki: 0.43 nM), and 5-HT2A (Ki: 0.6 nM) receptors, and also binds Alpha-1A adrenergic receptors. It can induce apoptosis, inhibit cancer cell proliferation, and is used to study psychiatric disorders, cancer, and inflammation.

Promethazine hydrochloride (Promethazine HCl) , the first-generation antihistamine, is a strong antagonist of the H1 receptor and a moderate antagonist of the mACh receptor, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.

Clozapine (HF 1854) is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity.

Aripiprazole (OPC-14597) is an antipsychotic agent that is structurally related to piperazines and quinolones. It is a partial agonist of SEROTONIN RECEPTOR, 5-HT1A and DOPAMINE D2 RECEPTORS, where it also functions as a post-synaptic antagonist, and an antagonist of SEROTONIN RECEPTOR, 5-HT2A.

Tolazoline (Benzalolin), a non-selective competitive α-adrenergic receptor antagonist, is used as a vasodilator to treat spasms of peripheral blood vessels. It has also been used successfully as an antidote to reverse the severe peripheral vasoconstriction as a result of overdose with certain 5-HT2A agonist drugs.

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.

Cyproheptadine hydrochloride is an effective orally active 5-HT2A receptor antagonist with antidepressant, anti-serotonin, and antiplatelet activities. It can be used for research on thromboembolic diseases and for the establishment of diabetes models.

Org GC 94 is a psychoactive small-molecule compound belonging to the tetracyclic antidepressant (TeCA) therapeutic family, extensively characterized as a noradrenergic and specific serotonergic antidepressant (NaSSA) with clinically documented antidepressant, anxiolytic, hypnotic, antiemetic, orexigenic, and antihistamine pharmacological effects. Org GC 94 mechanistically acting as an antagonist or inverse agonist at H1, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT6, 5-HT7, α1-adrenergic, and α2-adrenergic receptors, inhibiting norepinephrine reuptake, exhibiting high-affinity H1 inverse agonism associated with sedation and weight gain, showing negligible affinity for muscarinic acetylcholine receptors and thus lacking anticholinergic effects.

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

MDL 100009, the S-enantiomer of MDL 100151 and the opposite enantiomer of MDL 100907, is a selective antagonist of 5-HT2A.

4F 4PP oxalate is a 5-HT2A antagonist.

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.