Fluoxetine acts as a direct 5-HT 2C antagonist in addition to inhibiting serotonin reuptake, however, the clinical significance of this action is variable. [15] . Several tetracyclic antidepressants, including mirtazapine, are potent 5-HT 2C antagonists; this action may contribute to their efficacy. [16][17][18]

5-HT2C antagonists are compounds that block the 5-HT2C receptors, influencing the release of dopamine and noradrenaline in the brain. They have shown potential in treating conditions like anxiety, depression, and eating disorders by modulating brain functions related to these disorders.

Jun 21, 2024 · By modulating serotonin’s effect on dopamine, 5-HT2C receptor antagonists can potentially improve cognitive function and alleviate negative symptoms, offering a complementary approach to traditional antipsychotic medications.

An ergot-derivative that acts as an antagonist at certain 5-HT receptor subtypes and as an agonist at dopamine receptors. It is often used in situations where inhibition of prolactin is desirable. Methotrimeprazine

Importantly, the X-ray crystal structure of the 5-HT 2C R has recently been solved with non-selective 5-HT agonist ergotamine (“active-like” state) or the 5-HT 2 R antagonist/inverse agonist ritanserin (inactive state), further allowing a critical review of the receptor’s structural features and conformations for structure-based drug design (PDB...

Oct 1, 2018 · In a new Molecular Psychiatry report, researchers at Columbia University Irving Medical Center (CUIMC) have identified a likely culprit, the blockade which improves not only the side effect profile but also the therapeutic impact of SSRIs.

Apr 3, 2016 · Sertindole, a potent 5-HT2C antagonist, is a new antipsychotic drug with inverse agonist properties, shared with many other atypical and classical antipsychotic drugs (Herrick-Davis et al., 2000, Kuoppamaki et al., 1995).

At this time, there are no FDA-approved 5-HT 2C R-selective agonists, however, lorcaserin was marketed to promote weight loss in patients with a body mass index of greater than 30 or with a BMI of greater than 27 comorbid with type-2 diabetes, hypertension, or dyslipidemia.

This article explains how these ostensibly paradoxical actions of 5-HT2C antagonists and agonists can be reconciled and discusses both established and innovative strategies for the exploitation of 5-HT2C receptors in the improved management of depressed and anxious states.

Agomelatine, a 5-HT 2C antagonist and melatonin 1,2 receptor agonist is an antidepressant. Selective and potent 5-HT 2C receptor antagonists do exist: for example, RS 102221, FR260010, and SB 242084, whereas SDZ SER-082 is a mixed 5-HT 2C/2B receptor antagonist.