5-ht,antidepressant

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).

BIMU 8 is a selective agonist of 5-HT4 with EC50s of 18 nM, 77 nM, and 540 nM for wild-type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4.

Medifoxamine (LG 152) is a selective non-monoamine oxidase inhibitor that exhibits antidepressant activity through inhibition of 5 HT reuptake.Medifoxamine preferentially inhibits dopamine reuptake.

Roxindole (EMD 49980) is a selective dopamine autoreceptor and 5-HT1A dual agonist and inhibitor of 5-hydroxytryptamine (5-HT) uptake with antipsychotic and antidepressant activity.Roxindole can be used to study Parkinson's and neurodivergence.

Iprindole, a tricyclic indole antidepressant, is a dual weak inhibitor of noradrenaline and 5-HT uptake [1].

(+)-OSU 6162 (Piperidine, 3-[3-(methylsulfonyl)phenyl]-1-propyl-, (3R)-) is an agonist of 5-HT Receptor with anti-Alzheimer and antidepressant activities.

Quinupramine (LM 208) is an orally available classical tricyclic antidepressant compound with a strong affinity for muscarinic and 5-HT receptors.Quinupramine crosses the central nervous system and can be used in the study of neurologic disorders.

OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist with antidepressant-like activity, showing high affinity for the sigma receptor σ1/2 (IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM).

OPC-14523 dihydrochloride is the dihydrochloride form of the free base OPC-14523. OPC-14523 dihydrochloride is an orally active dual agonist of sigma receptors and 5-HT₁A receptors that also inhibits the 5-HT transporter, with IC₅₀ values of 47/56 nM for sigma receptors σ1/2, 5-HT₁A receptor IC₅₀ = 2.3 nM, and 5-HT transporter IC₅₀ = 80 nM. OPC-14523 dihydrochloride exhibits antidepressant-like activity. OPC-14523 dihydrochloride can be used in neuroscience research, including studies on antidepressants and neuroprotection.

Litoxetine is a selective 5-HT uptake inhibitor and is a 5-HT3 receptor antagonist. Litoxetine acts as an antidepressant and has shown antiemetic properties in ferrets. Litoxetine (1 and 10 mg/kg i.v.) dose-dependently reduced the number of regurgitations and vomiting and delayed the onset of vomiting. Litoxetine has an affinity for brain 5HT3 receptors (Ki = 85 nM).

Cericlamine is a selective 5-hydroxytryptamine (5-HT) reuptake blocker with antidepressant activity.

Femoxetine is a 5-HT inhibitor with antidepressant activity that potentiates morphine-induced anti-injury feelings and inhibits MAO-A and MAO-B required for the production of high exercise capacity in mice.

Seganserin, a non-selective 5-hydroxytryptamine 2-HT receptor antagonist, reversed the inhibitory effects of fluoxetine and quipazine on luteinizing hormone-induced hyperphagia, depression and nociception, and reversed the antidepressant and analgesic effects induced by fluoxetine and quipazine.

Tiflucarbine is a potential non-selective 5-HT agonist with antidepressant activity.Tiflucarbine dose-dependently increased the specific activity of soluble calmodulin (CaM)-dependent phosphodiesterase in rat brain.

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.

Clomipramine hydrochloride (Anafranil) is a tricyclic antidepressant similar to IMIPRAMINE that selectively inhibits the uptake of serotonin in the brain. It is readily absorbed from the gastrointestinal tract and demethylated in the liver to form its primary active metabolite, desmethylclomipramine.

Fluoxetine (LY-110140) is a highly specific serotonin uptake inhibitor and selective 5-hydroxytryptamine (5-HT) reuptake inhibitor. Fluoxetine has antidepressant activity.

Venlafaxine hydrochloride (Wy 45030 hydrochloride) is a cyclohexanol and phenylethylamine derivative functioning as a serotonin and noradrenaline reuptake inhibitor (SNRI) used as an antidepressive agent.

Sertraline hydrochloride (Sertraline HCl) is a selective serotonin uptake inhibitor that is used in the treatment of depression.

Trimipramine maleate (Surmontil maleate) appears to inhibit serotonin transport and norepinephrine uptake by nerve terminals. This increases available norepinephrine or serotonin and prolongs its action. Trimipramine Maleate is the maleate salt form of trimipramine, a tricyclic secondary amine of the dibenzazepine class, with an antidepressant property.

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.

Nortriptyline hydrochloride (ELF-101 hydrochloride) is a metabolite of AMITRIPTYLINE that is also used as an antidepressive agent. Nortriptyline is used in major depression, dysthymia, and atypical depressions.

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.

Doxepin hydrochloride (Aponal) is a dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors.