5-ht

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

Tedatioxetine hydrobromide (Lu AA 24530 hydrobromide) is a serotonin-norepinephrine-dopamine reuptake inhibitor and an antagonist of 5-HT2A, 5-HT2C, 5-HT3, and α1A-adrenergic receptors, which can be used to treat depression and anxiety.

SPD-473 citrate (BTS 74398 citrate) is a dopamine reuptake inhibitor, a norepinephrine transporter protein (NET) inhibitor, and a 5-hydroxytryptamine reuptake inhibitor, and is used in the study of neurological disorders and endocrine and metabolic diseases.

Pancopride(LAS 30451) is a novel, orally available, long-acting, selective 5-HT3 receptor antagonist that blocks nitrogen mustard and dacarbazine-induced vomiting.

Donitriptan hydrochloride (Donitriptan monohydrochloride) is a potent, high efficacy agonist of 5-HT1B/1D receptors with pKis of 9.4 and 9.3, respectively

Hymenidin, an alkaloid isolated from the Okinawan sponge Hymeniacidon sp. is a 5-hydroxytryptaminergic receptor antagonist and voltage-gated potassium channel inhibitor with potential antiprotozoal effects.It selectively binds to FOXO1 DNA and reduces depolarization-induced elevation of cellular calcium.

Lecozotan HCl (SRA-333) is a potent and selective 5-HT antagonist that significantly enhances KCl-stimulated glutamate and acetylcholine release from the hippocampal dentate gyrus and has cognitive enhancing properties. Chronic administration of Lecozotan HCl did not induce 5-HT(1A) receptor tolerance or desensitization in a behavioral model demonstrating 5-HT(1A) receptor function.

SLV-310 is a potent dopamine D2 receptor antagonist and 5-HT reuptake receptor inhibitor used in the study of neurological disorders such as bipolar disorder and schizophrenia.

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

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).

Litoxetine HCl is a selective 5-hydroxytryptamine (5-HT) reuptake inhibitor (SSRI) and mixed 5-hydroxytryptamine antagonist used in the treatment of urinary incontinence. Litoxetine HCl in the absence of antimuscarinic concentrations without antimuscarinic properties (10 nM-1 microM) caused concentration-dependent relaxation of isolated oesophageal muscle mucosa in rats, reducing carbachol tone by up to 37%. Higher concentrations of Litoxetine HCl (3 microM-300 microM) were associated with significant relaxation up to abolition of carbachol tone. The antiarrhythmic activity of Litoxetine HCl, previously demonstrated in the isolated guinea pig intestine, was exerted in the isolated rat oesophageal muscle mucosa at concentrations greater than 1 microM. The 5-HT-releasing effect of Litoxetine HCl could explain the potency of Litoxetine HCl on 5-HT-induced relaxation in untreated rat tissue, which was reversed by pCPA treatment.

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.

p-MPPF dihydrochloride is a selective 5-HT antagonist that dose-dependently antagonizes hypothermia induced by 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and can be used to study neurological diseases.

p-MPPF is a selective 5-HT antagonist that dose-dependently antagonizes hypothermia induced by 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and can be used to study neurological diseases.

Diclofensine (Ro 8-4650) is a monoamine reuptake inhibitor that blocks dopamine (IC50=0.74 nM), norepinephrine (IC50=2.3 nM), and 5-hydroxytryptophan (IC50=3.7 nM) in synaptosomes of the rat brain. dAURK-4 hydrochloride is an inhibitor of dopamine (IC50=0.74 nM), norepinephrine (IC50=2.3 nM) and 5-hydroxytryptophan (IC50=3.7 nM).

SB 216641 is a 5-HT (1B/1D) antagonist with anxiolytic activity for the study of anxiety and depression.

Haloperidol is an effective dopamine D2 receptor antagonist that can be used to induce models of tardive dyskinesia and Parkinson’s disease.

Paliperidone (9-hydroxyrisperidone)(Invega) is used as an atypical antipsychotic. It applies to the acute and maintenance treatment of schizophrenia. Chemically, paliperidone is the primary active metabolite of the older atypical antipsychotic risperidone.

Urapidil hydrochloride (Urapidil HCl) is 5-HT1A receptor agonist and an α1-adrenoceptor antagonist.

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.

Urapidil (Ebrantil), a sympatholytic antihypertensive drug, acts as a 5-HT1A receptor agonist and as an α1-adrenoceptor antagonist.

Maprotiline hydrochloride (Psymion) is a bridged-ring tetracyclic antidepressant that is both mechanistically and functionally similar to the tricyclic antidepressants, including side effects associated with its use.

Sumatriptan succinate (GR 43175), a serotonin1 (5-HT1) receptor agonist, is used in the acute treatment of a migraine headache.