5-ht2c (human)

Agomelatine (L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors (Kis: 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2), and Agomelatine (S-20098). L(+)-Tartaric acid also functions as a selective 5-HT2C receptor antagonist (pKis: 6.4 and 6.2 at native porcine and cloned human 5-HT2C receptors), actively supporting research into melatonergic signaling pathways, receptor-mediated regulation, and novel psychiatric therapeutics by enabling precise modulation of circadian and serotonergic systems in cellular models to improve neuropharmacological understanding and experimental reproducibility across neuroscientific and clinical translational studies.

SB 243213 is an orally available and selective 5-HT2C receptor antagonist.SB 243213 has anxiolytic and antidepressant activity and is used in schizophrenia and movement disorders.

LY 344864 hydrochloride is a selective receptor agonist with an affinity of 6 nM (Ki) at the 5-HT1F receptor.

Agomelatine hydrochloride (S-20098 hydrochloride) is a specific MT1 and MT2 receptor agonist with Ki values of 0.1 nM for CHO-hMT1, 0.06 nM for HEK-hMT1, 0.12 nM for CHO-hMT2, and 0.27 nM for HEK-hMT2, respectively [1]. Additionally, Agomelatine hydrochloride is a selective antagonist of the 5-HT2C receptor with pKi values of 6.4 and 6.2 for native (porcine) and cloned human 5-HT2C receptors, respectively [2].

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.

Agomelatine (Valdoxan) is structurally closely related to melatonin. Agomelatine is a potent agonist at melatonin receptors and an antagonist at serotonin-2C (5-HT2C) receptors, tested in an animal model of depression.

Iloperidone (HP 873) is an atypical antipsychotic agent that is used for treatment of schizophrenia.

CP-809101 hydrochloride is a potent and selective 5-HT2C receptor agonist with pEC50 values of 9.96 for human 5-HT2C, 7.19 for 5-HT2B, and 6.81 for 5-HT2A receptors.

DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (EC50=1.7 nM).

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.

SB 243213 hydrochloride is an orally active, selective, high-affinity antagonist of the 5-hydroxytryptamine (5-HT)2C receptor (pKi of 9.37 and pKb of 9.8), with an improved anxiolytic profile and potential for treating schizophrenia and motor disorders.

SB 243213 dihydrochloride is an orally active, selective, and high-affinity antagonist of the 5-hydroxytryptamine (5-HT)2C receptor, with a pKi of 9.37 and a pKb of 9.8 for the human 5-HT2C receptor.

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).

ASP-2205, a 5-HT2C receptor agonist (human 5-HT2C receptor, EC50=0.85 nM; rat 5-HT2C receptor, EC50=2.5 nM), enhances the urethral closure reflex mediated by the genital nerve, thereby preventing urinary incontinence.

25B-NBF hydrochloride is a potent agonist of the 5-HT2C receptor, showing binding affinity to the human 5-HT2A receptor and the rat 5-HT2C receptor, with pKi values of 8.57 and 7.73, respectively.

Norquetiapine (N-Desalkylquetiapine) is a metabolite of Quetiapine and acts as a selective HCN1 channel inhibitor with an IC50 of 13.9 μM. It selectively inhibits norepinephrine reuptake and serves as a partial agonist at the 5-HT1A receptor (Ki = 45 nM). Norquetiapine also functions as an antagonist at presynaptic α2 (Ki = 237 nM), 5-HT2C (Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Additionally, it blocks human cardiac sodium channels Nav1.5 in a state-dependent manner. In LPS-injected C57BL/6 mice, Norquetiapine displays partial anti-inflammatory effects. This compound is utilized in research related to depression and inflammation.

Iloperidone hydrochloride is a D(2)/5-HT(2) receptor antagonist. It is also an atypical antipsychotic for the treatment of schizophrenia symptoms.

RS 64459-193 has a high affinity for the 5-HT1A binding site.

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].

Metergoline (Methergoline) is a dopamine agonist and serotonin antagonist. It has been used similarly to BROMOCRIPTINE as a dopamine agonist and also for migraine disorder therapy.

Sarizotan (EMD 128130) is an orally active compound that acts as an agonist for serotonin 5-HT 1A receptors and dopamine receptors, with IC50 values of 6.5 nM for rat 5-HT 1A, 0.1 nM for human 5-HT 1A, 15.1 nM for rat D 2, 17 nM for human D 2, 6.8 nM for human D 3, and 2.4 nM for human D 4.2.

SB 271046 hydrochloride (SB 271046A) is selective, orally active 5-HT6 antagonist (pKi values are 9.02-8.92, 6.35, 6.55, 6.27 at 5-HT6, 5-HT1A, 5-HT1D and D3, and 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively) and is > 200-fold selective over 55 other receptors, enzymes and ion channels. It increases extracellular aspartate and glutamate in the frontal cortex and exhibits anticonvulsant activity (EC50: 0.16 μM).

RO1138452 (CAY10441) is a selective and orally bioavailable antagonist of prostacyclin receptor (pKi: 8.3). It antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cyclic AMP accumulation in a dose-dependent manner. Likewise, it inhibits the binding of tritiated iloprost to rodent neuroblastoma cells with a Ki of about 1.5 nM. At levels between 2-20 mg/kg in rats, CAY10441 shows significant analgesic activity in standard antinociceptive assays [1].

5-HT2A receptor agonist-3 represents the highest selectivity for the human 5-HT2A receptor currently identified, exhibiting a K i of 2.5 nM. It also demonstrates a remarkable 124-fold selectivity over its structurally analogous 5-HT2C receptor [1].