serotonin uptake

Gentisein (NSC-329491), a primary metabolite of Mangiferin, exhibits significant inhibition of serotonin uptake, demonstrating potency with an IC50 value of 4.7 µM[1][2].

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.

Fluoxetine hydrochloride (Lilly110140) is the first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants.

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

Reserpine (Serpalan) is an alkaloid isolated from the root of Rauwolfia serpentina. As an inhibitor of vesicular monoamine transporter 2 (VMAT2), it suppresses the uptake of norepinephrine into storage vesicles, leading to depletion of catecholamines and serotonin in central and peripheral nerve terminals. It has antihypertensive and antipsychotic effects and can be used to induce gastric ulcer and depression models.

Desipramine hydrochloride (Norimipramine) ,a secondary amine tricyclic antidepressant (TCA), is the hydrochloride salt form of desipramine. In the central nervous system (CNS), Desipramine hydrochloride blocks the re-uptake of neurotransmitters, including norepinephrine and serotonin. This leads to an increase in the amount of these neurotransmitters in the synaptic cleft and prolongs their activities postsynaptically.

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.

4-aminobenzoic acid is an organic acid with UV-absorbing and antifibrotic properties. When exposed to light, 4-aminobenzoic acid absorbs UV light and releases excess energy through a photochemical reaction, which may cause DNA damage.4-aminobenzoic acid also increases oxygen uptake at the tissue level and may enhance monoamine oxidase (MAO) activity to promote serotonin degradation, which in excess may lead to fibrotic Changes.

Duloxetine hydrochloride ((S)-Duloxetine hydrochloride) is a thiophene derivative and selective neurotransmitter uptake inhibitor for serotonin and noradrenaline (SNRI). It is an antidepressant agent and anxiolytic, also used for treating pain in patients with diabetes mellitus and fibromyalgia.

Trazodone hydrochloride (Trazodone HCl) is a serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety.

7-Chloro-4-(piperazin-1-yl)quinolone is an important scaffold in medicinal chemistry, exhibiting diverse pharmacological profiles either alone or as a hybrid with other active pharmacophores. It is a potent sirtuin inhibitor, also inhibiting serotonin uptake (IC50 of 50 μM), and demonstrates antimalarial activity on D10 and K1 strains of P. falciparum with IC50 values of 1.18 μM and 0.97 μM, respectively [1].

Escitalopram (Seroplex) is a furancarbonitrile that is one of the SEROTONIN UPTAKE INHIBITORS used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from tardive dyskinesia in preference to tricyclic antidepressants, which aggravate this condition.

Protriptyline Hydrochloride is the hydrochloride salt form of protriptyline, a tricyclic secondary amine with an antidepressant property. Protriptyline hydrochloride (Protriptyline HCl) blocks the re-uptake of norepinephrine and serotonin by nerve terminals, thereby increasing available norepinephrine and serotonin. In addition, this agent exhibits anticholinergic activity.

Amoxapine (CL-67772) exerts its antidepressant effect by inhibiting the re-uptake of norepinephrine and, to a lesser degree, of serotonin, at adrenergic nerve endings and blocks the response of dopamine receptors to dopamine. Amoxapine is a tricyclic antidepressant of the dibenzoxazepine class. This drug is used to treat symptoms of depression and may cause tardive dyskinesia. Amoxapine also binds to alpha-adrenergic, histaminergic, and cholinergic receptors which accounts for many of the side effects seen with this agent.

Paroxetine hydrochloride (Paroxetine HCl) is a serotonin uptake inhibitor that is effective in the treatment of depression.

PIM-35, an indole derivative with properties similar to antidepressants, exhibits weaker norepinephrine uptake inhibition compared to standard compounds. Prolonged use of PIM-35 does not affect the quantity or affinity of alpha 2, beta 1-, and beta 2-adrenergic receptors. Additionally, PIM-35 influences the serotonin system, resembling antidepressant compounds like paroxetine and clomipramine.

Lu 19005 is a potent inhibitor of dopamine, serotonin, and norepinephrine uptake.

5-IAI hydrochloride is a psychoactive analog of para-iodoamphetamine. 5-IAI hydrochloride significantly reduces serotonin uptake sites and hippocampal serotonin levels in rats.

5-APDI hydrochloride is an indane featuring an amphetamine-like aminopropyl group. It acts as an inhibitor of serotonin, dopamine, and norepinephrine uptake by synaptosomes, with IC50 values of 82 nM, 1,847 nM, and 849 nM, respectively.

Clomipramine (Clomicalm) is a tricyclic antidepressant (TCA). It is used for the treatment of the panic disorder, obsessive-compulsive disorder, major depressive disorder, and chronic pain. It may decrease the risk of suicide in those over the age of 65. It is similar to Imipramine in that selective inhibition of the serotonin uptake in the brain.

Reserpine hydrochloride is the salt form of Reserpine and acts as an inhibitor of vesicular monoamine transporter 2 (VMAT2). It blocks the uptake of norepinephrine into storage vesicles, leading to the depletion of catecholamines and serotonin at central and peripheral nerve terminals. It has antihypertensive and antipsychotic properties and is commonly used to induce models of gastric ulcer and depression.

Seproxetine HCl, a more active enantiomer of N-desmethyl metabolite fluoxetine, works by selectively inhibiting the serotonin uptake carrier.

Beloxepin is an oral dual selective inhibitor of serotonin and norepinephrine uptake.