5-ht2a antagonist 1

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

dopamine D1 receptor antagonist

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.

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.

Flibanserin, a compound identified as BIMT-17, acts as a complete agonist at the serotonin 5-HT1A receptor, with a binding affinity (Ki) of 1 nM, while functioning as an antagonist at the 5-HT2A receptor with a 49 nM affinity. Flibanserin D4 represents a deuterium-labeled version of Flibanserin.

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.

D3/5-HT receptor modulator-1 (compound 5i) is a selective antagonist of the dopamine D3 and 5-HT2A receptors, and a partial agonist at the 5-HT1A receptor. It exhibits Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for the dopamine D3, 5-HT2A, and 5-HT1A receptors respectively. The compound shows lower affinity for the dopamine D2 receptor, 5-HT2C receptor, and hERG channel. D3/5-HT receptor modulator-1 possesses atypical antipsychotic properties.

BGC20-761 is a selective 5-HT6 and dopamine receptor antagonist (human receptor K i values: 5-HT6 (20 nM), 5-HT2A (69 nM), D2 (140 nM)), and a tryptamine analog with a high affinity for 5-HT(6) receptors, that can enhance long-term memory, with potential utility as an antipsychotic agent [1].

Pruvanserin hydrochloride (EMD 281014 HCl) is an inverse and selective 5-HT2A receptor antagonist with IC₅₀ values of 0.35 nM and 1 nM for human and rat 5-HT2A receptors, respectively. Pruvanserin hydrochloride inhibits GTP-gamma-S accumulation and alleviates tactile allodynia in diabetic rats, making it suitable for studies on Parkinson's disease, insomnia, and schizophrenia.

SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.IC50 value: 9.0(pKi) [1]Target: 5-HT2C antagonistin vitro: SB 242084 had over 100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors. In studies of 5-HT-stimulated phosphatidylinositol hydrolysis using SH-SY5Y cells stably expressing the cloned human 5-HT2C receptor, SB 242084 acted as an antagonist with a pKb of 9.3, which closely resembled its corresponding receptor binding affinity [1].in vivo: SB 242084 potently inhibited m-chlorophenylpiperazine (mCPP, 7 mgkg i.p. 20 min pre-test)-induced hypolocomotion in rats, a model of in vivo central 5-HT2C receptor function, with an ID50 of 0.11 mg/kg i.p., and 2.0 mg/kg p.o. SB 242084 (0.1-1 mg/kg i.p.) exhibited an anxiolytic-like profile in the rat social interaction test, increasing time spent in social interaction, but having no effect on locomotion. SB 242084 (0.1-1 mg/kg i.p.) also markedly increased punished responding in a rat Geller-Seifter conflict test of anxiety, but had no consistent effect on unpunished responding [1].

Cyproheptadine is an orally active serotonin 5-HT2A receptor antagonist with multiple pharmacological properties including antidepressant, anti-serotonin, antiplatelet, and antithrombotic effects. Cyproheptadine is used as a research compound for investigating thromboembolic diseases, serotonergic signaling, and potential links between serotonin modulation and metabolic disorders such as diabetes.

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-HT6/5-HT2AR antagonist-1 is a potent dual antagonist for the 5-HT6 and 5-HT2A receptors, demonstrating high efficacy with K_i values of 11 nM and 39 nM, respectively [1].

Flibanserin (BIMT-17; BIMT-17BS) hydrochloride is an orally active compound that functions as a 5-HT1A receptor agonist (Ki: 1 nM) and a 5-HT2A receptor antagonist (Ki: 49 nM) of 5-hydroxytryptamine. It possesses antidepressant and anxiolytic effects and is used in studies of hypoactive sexual desire (HSDD).

Zicronapine (Lu 31-130) fumarate, an antipsychotic medication, exhibits potent pro-cognitive effects in animal models and holds promise for treating various neurological and psychiatric conditions. It acts as a strong antagonist at dopamine D1/D2 and serotonin 5-HT2A receptors, highlighting its potential therapeutic efficacy [1] [2].

R-96544 is an orally active antagonist of the 5-HT2A receptor that has demonstrated the ability to inhibit platelet aggregation in vitro [1].

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].

Flibanserin-d4-1 is the deuterated form of Flibanserin. Flibanserin (BIMT-17) functions as a full agonist at the 5-hydroxytryptamine (5-HT1A) receptor with a Ki of 1 nM, and as an antagonist at the 5-HT2A receptor with a Ki of 49 nM. It binds to dopamine D4 receptors with an affinity ranging from 4 to 24 nM, while showing negligible affinity for various other neurotransmitter receptors and ion channels. Flibanserin is being investigated for its potential in treating hypoactive sexual desire disorder (HSDD).

Sarpogrelate-d3 HCl is a deuterated compound of Sarpogrelate HCl. Sarpogrelate HCl has a CAS number of 135159-51-2. Sarpogrelate(MCI-9042) hydrochloride, 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 was shown to have the same affinity as ritanserin for 5-HT2A receptors, with a Ki value of 8.39 nM. Sarpogrelate 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-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.