5-ht2c

5-HT2A/5-HT2C inverse agonist 1 serves as a dual and potent inverse agonist for the 5-HT2A and 5-HT2C receptors, with hERG inhibition properties that mitigate cardiovascular risks. Demonstrating significant antipsychotic efficacy in the MK-801-induced mouse model, this compound holds potential for psychosis research.

Compound (−)-19, also known as (-)-5-HT2C agonist-3, is a selective 5-HT2C agonist exhibiting a preference for Gq signaling. It demonstrates efficiency with EC50 values for 5-HT2 receptor subtypes as follows: 5-HT2C at 103 nM, 5-HT2B at 570 nM, and 5-HT2A at 72 nM. This compound is utilized in research on antipsychotics.

Compound 3i, a 5-HT2C agonist-4, acts as an agonist for the 5-HT2C receptor with an EC50 of 5.7 nM. It is capable of reducing locomotor activity in zebrafish larvae.

5-HT2C agonist-5 (Compound 3A) functions as a 5-HT2C receptor agonist with an EC50 of less than 1 nM. It is applicable in the research of neurological disorders.

5-HT2C agonist-9 (Compound 33) is a 5-HT2C receptor agonist with an EC50 of 1.4 nM for h5-HT2C. It is utilized in research related to conditions such as depression, drug addiction, alcohol dependence, PTSD, and neuropathic pain.

5-HT2C agonist-6 (Compound 13) is a tricyclic hallucinogen and a 5-HT2C agonist with an EC50 of 13.8 nM, useful for research in neurological disorders.

5-HT2C agonist-11 (Compound 1) is an orally active, brain-penetrant, and selective 5-HT2C receptor agonist with an EC50 of 15 nM. It activates the Gq protein signaling pathway, promoting intracellular calcium release. This compound shows potential for research in depression, post-traumatic stress disorder (PTSD), and neuropathic pain.

5-HT2C agonist-10 (Compound 21) is a 5-HT2C receptor agonist with an EC50 of less than 10 nM. It is utilized in the study of mental disorders.

5-HT2C agonist-3 ((+)-19), a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM), exhibits antipsychotic-like activity by blocking amphetamine-induced hyperactivity [1].

5-HT2C agonist-3 ((+)-19) free base is a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM) that exhibits antipsychotic drug-like activity and inhibits Amphetamine-induced hyperactivity [1].

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

5-HT2A&5-HT2C agonist-1 (Example 2) is a dual-acting agent targeting 5-HT2A and 5-HT2C receptors with IC50 values of 196 nM and 0.9 nM, respectively. It is applicable in studying central nervous system disorders, including depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headaches, post-traumatic stress disorder (PTSD), and seizure disorders [1].

The compound 5-HT2CR agonist 1 (compound 8), a 7-chloro analogue, is a selective partial agonist for the 5-HT2C receptor, exhibiting an Emax of 71.09% and an EC50 of 121.5 nM, with no activity observed toward 5-HT2A or 5-HT2B receptors. It does not recruit β-arrestin and shows low hERG inhibition at 10 μM [1].

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).

PRX933 hydrochloride (GW876167 hydrochloride) is an agonist of 5-HT2C receptor and can be used in studies about hypertension acute treatment.

(Rac)-WAY-161503 is a selective and high-affinity agonist of the 5-HT2C receptor [Ki: 4 nM; EC50: 12 nM], exhibiting anti-obesity and antidepressant effects.

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.

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.

Viloxazine (Viloxazin) (Viloxazin) is a dual-action compound that functions as a norepinephrine reuptake inhibitor and exhibits potent agonistic activity towards 5-HT 2C receptors while acting as an antagonist for 5-HT 2B receptors, with respective potency values of EC 50 = 32 μM and IC 50 = 27 μM. Its primary mechanism of action involves the modulation of serotonergic and noradrenergic pathways. Viloxazine is commonly employed in depression research [1] [2].

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

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

Dapoxetine (Dapoxetina) is a selective serotonin reuptake inhibitor, for the treatment of premature ejaculation.

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.

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.