serotonergic

Mirtazapine (6-Azamianserin) is a tetracyclic antidepressant with a somewhat unique mechanism of action. Mirtazapine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.

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.

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.

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].

Laprafylline is a xanthine compound with inhibitory effects on bronchoconstriction in vivo and antitumor activity.Laprafylline acts as a competitive serotonergic antagonist at low concentrations, and inhibits constriction induced by hist at high difficulties.

Vilazodone (SB659746A) is a selective serotonin (5-HT) reuptake inhibitor (SSRI) and a 5-HT-1A receptor partial agonist, with antidepressant and anti-anxiety activities. Vilazodone inhibits the reuptake of serotonin from the synaptic cleft while stimulating the release of 5-HT into the synaptic cleft. This increases the concentration of 5-HT in the synaptic cleft and potentiates serotonergic neurotransmission in the central nervous system.

Citalopram hydrobromide (XU-62-320) , a selective serotonin reuptake inhibitor (SSRI), selectively inhibits the CNS neuronal reuptake of serotonin, thereby potentiating serotonergic activity in the central nervous system (CNS). Citalopram hydrobromide is the orally bioavailable hydrobromide salt of the racemic bicyclic phthalene derivative citalopram with antidepressant activity. This agent has minimal effects on the CNS neuronal reuptake of norepinephrine (NE) and dopamine (DA).

Citalopram (Lu 10-171 is an orally active, selective serotonin reuptake inhibitor (SSRI), a selective 5-hydroxytryptamine reuptake inhibitor, and a racemic mixture of the S(+)-enantiomer (Escitalopram) and the R(-)-enantiomer.Citalopram exhibits antidepressant activity and enhances serotonergic neurotransmission. It can be used to study Alzheimer's disease.

Vortioxetine (Lu AA 21004) is a serotonergic antidepressant used for major depression disorders. Vortioxetine has been associated with a low rate of minor serum aminotransferase elevations during treatment.

Flibanserin (Girosa) is a serotonergic antidepressant used to treat hypoactive sexual desire disorder. Flibanserin has been associated with a low rate of minor serum aminotransferase elevations during treatment but has not been linked to instances of clinically apparent acute liver injury.

1. Carvacrol (O-Thymol) presents anxiolytic effects. 2. 5-Isopropyl-2-methylphenol presents antinociceptive activity. 3. Carvacrol presents antidepressant effects, seems to be dependent on its interaction with the dopaminergic system, but not with the serotonergic and noradrenergic systems.

MPP+ iodide, the metabolite of a neurotoxin MPTP, causes symptom of Parkinson's disease (PD) in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ induces dopamine transporter (DAT) externalization in dopaminergic (DA) neurons, but internalization of serotonin transporter (SERT) in serotonergic (5-HT) neurons. MPP+ induces autophagic cell death in SH-SY5Y cells.

Frovatriptan is a highly potent and cerebroselective agonist of the 5-HT1B/1D receptors, demonstrating the greatest receptor potency among clinically used triptan compounds, and it robustly activates serotonergic signaling pathways to modulate cranial vasoconstriction and trigeminal neurotransmission relevant to migraine pathophysiology, while showing demonstrated clinical efficacy and, in certain predefined endpoints, superiority when administered during the headache phase of migraine attacks accompanied by aura, supporting the optimized pharmacodynamic profile for targeted antimigraine therapy and translational neuropharmacology research.

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.

1-(1-Naphthyl) piperazine hydrochloride (1-naphthalen-1-ylpiperazine hydrochloride) is a serotonergic ligand which could bind nonselectively with multiple serotonin (5-HT) receptors.

4i (CHEMBL1269981) is a 5-HT3 receptor antagonist,It modulates the serotonergic system.

Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand [125I-ICYP] to [5HT1B-serotonergic] receptor sites. It is an antihypertensive agent.

(Z)-Thiothixene (Thiothixene) is an antagonist of serotonergic receptor.

Buspirone (Buspirone free base) is an azaspiro compound which has a role as an anxiolytic drug, a sedative, a serotonergic agonist and an EC 3.4.21.26 (prolyl oligopeptidase) inhibitor.

HPTP is a monoaminergic neurotoxin related to MPTP. It is the dehydration product of haloperidol. The agent is specifically a dopaminergic and serotonergic neurotoxin. HPTP is a prodrug of HPP+, which mediates its monoaminergic neurotoxicity, HPTP can be utilized for building neurotoxic or immuno-deficient model for research related to neuroscience.

α-Guanidinoglutaric Acid is found in cobalt-induced epileptogenic focus tissue in the cerebral cortex of cats. α-Guanidinoglutaric Acid-induced seizures are associated with abnormal serotonergic function and that they are initiated by a decrease in the 5-HT level.

Loxapine is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent,used primarily in the treatment of schizophrenia. The drug is a member of the dibenzoxazepine class and structurally related to clozapine (which belongs to the chemically akin class of dibenzodiazepines).

dopamine D4 and serotonergic 5-HT2A receptor antagonist

Clothiapine (HF 2159) is an atypical antipsychotic agent with potent anti 5-hydroxytryptaminergic and serotonergic activity, which has been used in the study of schizophrenia.