- Citalopram is a selective inhibitor of ST (5-hydroxytryptamine/serotonin transporter) and therefore is a potent and selective serotonin reuptake inhibitor.
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5-HT Receptor agonist
Clomipramine is a blocker of the following transporters:Serotonin transporter (SERT) (Ki = 0.14 nM),Norepinephrine transporter (NET) (Ki = 54 nM),Dopamine transporter (DAT) (Ki = 3,020 nM),Glycine transporter (GlyT/LeuT). -
5-HT3 receptor antagonist
Granisetron HCl is a serotonin 5-HT3 receptor antagonist -
5-HT2/5-HT1 antagonist
Mianserin hydrochloride is a 5-HT2/5-HT1 antagonist. Has moderate affinity for 5-ht6 Non-selective 5-HT2 receptor antagonist. Has moderate affinity for 5-HT6. Antidepressant. -
5-HT Receptor agonist
Tianeptine sodium is a selective serotonin reuptake enhancer (SSRE) in vitro and in vivo. -
5-HT (serotonin) and dopamine receptor antagonist
Ziprasidone hydrochloride monohydrate (CP 88059 hydrochloride monohydrate) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. -
5-HT1D receptor antagonist
BRL-15572 is a selective h5-HT1D antagonist, displaying 60-fold selectivity over h5-HT1B, and exhibiting little or no affinity for a range of other receptor types.
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Serotonin 5HT3-receptor antagonist
Alosetron Hydrochloride(1:X) (GR 68755 Hydrochloride(1:X)) is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome. - Trazodone is an antidepressant of the serotonin antagonist and reuptake inhibitor (SARI) class. It is a phenylpiperazine compound. Trazodone also has anti-anxiety (anxiolytic) and sleep-inducing (hypnotic) effects.
- Duloxetine is a serotonin-norepinephrine reuptake inhibitor (SNRI). It is effective for major depressive disorder and generalized anxiety disorder (GAD).
- Duloxetine Hydrochloride is a dual serotonin and norepinephrine reuptake inhibitor (SNRI) that is used in the treatment of stress urinary incontinence, as well as depression.
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5-HT Receptor agonist
Almotriptan malate (Axert) is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults.- Li Li, .et al. , J Exp Med, 2022, Aug 1;219(8):e20212307 PMID: 35796804
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5-HT1A receptor agonist
Aripiprazole is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.- Jaime Osuna-Luque, .et al. , J Exp Neurosci, 2018, 12: 1179069518798628 PMID: 30245571
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5-HT2A receptor antagonist
Lumateperone Tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a SERT blocker (Ki = 61 nM). -
5HT2A antagonist
Ketanserin tartrate is a salt of Ketanserin. Ketanserin is reported to have a high affinity for multiple G protein-coupled receptors, such as serotonin receptors. -
5-HT2 receptor antagonist
Cyclobenzaprine HCl is a muscle relaxant by blocking pain sensations. -
5-HT1C receptor antagonist
Clozapine N-oxide is a major metabolite of Clozapine noted to decrease SR-2A (5-HT2 serotonin receptor) density in vitro. - Quetiapine is an atypical antipsychotic used in the treatment of schizophrenia, bipolar I mania, bipolar II depression, bipolar I depression.
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5HT(1A) receptor agonist
Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders. - Amitriptyline inhibits serotonin receptor, norepinephrine receptor, 5-HT4, 5-HT2 and sigma 1 receptor with IC50 of 3.45 nM, 13.3 nM, 7.31 nM, 235 nM and 287 nM, respectively.
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5-HT3 receptor antagonist
Azasetron HCl is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy. -
Serotonin reuptake inhibitor
Escitalopram oxalate ((S)-(+)Citalopram oxalate) is a selective serotonin reuptake inhibitor (SSRI) with Ki of 0.89 nM. - Harmine, also known as telepathine, is a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds. It occurs in a number of different plants, most notably the Middle Eastern plant harmal or Syrian rue (Peganum harmala) and the South American vine Banisteriopsis caapi (also known as "yage" or "ayahuasca"). Harmine reversibly inhibits monoamine oxidase A (MAO-A), an enzyme which breaks down monoamines, making it a RIMA. Harmine selectively binds to MAO-A but does not inhibit the variant MAO-B.
- Lei Tan, .et al. , Res Vet Sci, 2022, 145: 125-134 PMID: 35190327
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5-HT3 receptor antagonist
Dolasetron mesylate is a selective 5-HT3 receptor antagonist. -
Serotonin receptors agonist
Dihydroergotamine Mesylate, also known as DHE or Migranal, is an ergot alkaloid used to treat migraines. It has similar actions to the triptans, acting as an agonist to the serotonin receptors and causing vasoconstriction of the intracranial blood vessels, but also interacts centrally with dopamine and adrenergic receptors. -
5-HT1A receptor antagonist
Alprenolol (hydrochloride) is a non-selective beta blocker as well as 5-HT1A receptor antagonist. -
5-HT2 receptor antagonist
Methiothepin mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C). -
5-HT2B receptor antagonist
RS 127445 is a novel high affinity, selective 5-HT2B receptor antagonist with pKi of 9.5. -
serotonin reuptake inhibitor/5-HT2A receptor antagonist
Eplivanserin mixture is a selective serotonin reuptake inhibitor and a 5-HT2A receptor antagonist, extracted from patent WO 2005/002578 A1. -
5-HT receptor agonist
MK 212 hydrochloride is a 5-HT receptor agonist; displays selectivity for 5-HT2C over 5-HT2A (IC50 values are 0.028 and 0.42 μM for human 5-HT2C and 5-HT2A receptors expressed in HEK293 cells respectively).