5-HT Receptor Agonist

Ethylpropyltryptamine (EPT) is a novel orally active psychoactive substance. Ethylpropyltryptamine (EPT) is predicted to be a partial agonist of the 5-HT_2A receptor.

Dihydroergotamine (mesylate) (Standard) is the analytical standard of Dihydroergotamine (mesylate). This product is intended for research and analytical applications. Dihydroergotamine mesylate is a BBB-permeable ergot alkaloid that can be used for the research of migraines.

Prucalopride (Standard) is the analytical standard of Prucalopride. This product is intended for research and analytical applications. Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pK_is of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer.

6-APDB is a class of monoamine neurotransmitter releaser and Monoamine Transporter modulator that exerts selective effects on human monoamine transporters and acts as a partial agonist at 5-HT₂ family receptors. For NET, 6-APDB has an IC₅₀ of 0.56 μM and a K_i of 18 μM; for SERT, it has an IC₅₀ of 2.3 μM and a K_i of 23 μM; for DAT, it has an IC₅₀ of 33 μM and a K_i of >30 μM, and affinity for rat and mouse TAAR1, with K_i values of 1.0 μM and 0.21 μM, respectively. 6-APDB inhibits norepinephrine and 5-HT reuptake, mediates the release of three types of monoamine neurotransmitters, shows a dose-dependent biphasic locomotor effect in mice, and fully substitutes the discriminative stimulus effect of MDMA. 6-APDB shows no significant cytotoxicity at high concentrations, and possesses empathogenic psychoactivity, potential hallucinogenic effects, and behavioral effects associated with intermittent abuse.

SCH-23390 hydrochloride (Standard) is the analytical standard of SCH-23390 hydrochloride (HY-19545A). This product is intended for research and analytical applications. SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D₁-like receptor antagonist with K_is of 0.2 nM and 0.3 nM for the D₁ and D₅ receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT_2C receptor agonist with a K_i of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT₂ and 5-HT_1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC₅₀ of 268 nM.

TCB2 (Standard) is the analytical standard of TCB2 (HY-103102). This product is intended for research and analytical applications. TCB2 is an agonist of serotonin 5-HT2A receptor.

Dehydroaripiprazole-d₈ is deuterium labeled Dehydroaripiprazole. Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole.

2-(2-Methoxyphenoxy)ethylamine hydrochloride (Standard) is the analytical standard of 2-(2-Methoxyphenoxy)ethylamine (hydrochloride) (HY-107847). This product is intended for research and analytical applications. 2-(2-Methoxyphenoxy)ethylamine hydrochloride (Compound 2b) is a mixed agonist/antagonist. 2-(2-Methoxyphenoxy)ethylamine hydrochloride is a5-HT1A receptor partial agonist and a α1-adrenergic receptor antagonist. 2-(2-Methoxyphenoxy)ethylamine hydrochloride can be used for neurological diseases research, such as anxiety, depression and psychosis.

IS-159 is a potent serotonin 5-HT1 agonist. IS-159 has the potential for the research of migraine.

Flesinoxan (Standard) is the analytical standard of Flesinoxan. This product is intended for research and analytical applications. Flesinoxan is a hypotensive agent and a potent, high affinity and selective 5-hydroxytryptamine1A (5-HT1A) receptor agonist with an EC50 value of 24 nM. Flesinoxan also has effective anxiolytic/antidepressant effects.

8-OH-DPAT (Standard) is the analytical standard of 8-OH-DPAT. This product is intended for research and analytical applications. 8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A and a Ki of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).

Xaliproden (hydrochloride) (Standard) is the analytical standard of Xaliproden (hydrochloride). This product is intended for research and analytical applications. Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [³⁵S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety.

Zalospirone (WY-47846) is a novel cyclic imide with 5-HT1A partial agonist activity. Zalospirone shows antidepressant efficacy.

Velusetrag (Standard) is the analytical standard of Velusetrag (HY-10457). This product is intended for research and analytical applications. Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pK_i of 7.7. Velusetrag exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease.

Urapidil (Standard) is the analytical standard of Urapidil. This product is intended for research and analytical applications. Urapidil is an α1 adrenoreceptor antagonist and a 5-HT_1A receptor agonist that can cross the blood-brain barrier.

CP94253 hydrochloride (Standard) is the analytical standard of CP94253 hydrochloride (HY-103151). This product is intended for research and analytical applications. CP94253 hydrochloride is an orally active, brain-penetrant and selective 5-HT_1B receptor agonist with an K_i of 2 nM. CP94253 hydrochloride induces antidepressant-like effects, waking enhancement, sleep inhibition, increased sleep latency, hyperlocomotion, and suppressed aggressive behavior. CP94253 hydrochloride can be used for the research of depression and heightened aggressive behavior.

WAY 163909 hydrochloride is an orally active, blood-brain barrier permeable 5-HT2C receptor-selective agonist. WAY 163909 hydrochloride exhibits an EC₅₀ of 8 nM and a K_i of 10.5 nM for h5-HT2C. Instead of triggering apoptosis, WAY 163909 hydrochloride induces anorectic, antipsychotic-like, antidepressant-like, anti-aggressive and anti-compulsive effects. WAY 163909 hydrochloride alleviates ketamine-induced hypothermia, but impairs sexual function at high doses. With rapid antidepressant-like properties, WAY 163909 hydrochloride can be used in research related to obesity, schizophrenia, depression, obsessive-compulsive disorder, and anesthesia-induced hypothermia.

25CN-NBOH hydrochloride exhibits agonist activity at the 5-HT_2a receptor, shows 90- to 100-fold selectivity over the 5-HT₂c receptor, and possesses blood-brain barrier permeability. 25CN-NBOH hydrochloride acts as an interoceptive agent with partial agonist-like properties. 25CN-NBOH hydrochloride serves as a pharmacological tool for 5-HT_2A receptor research, and its tritiated form functions as a selective agonist radioligand. 25CN-NBOH hydrochloride can be used to investigate diseases characterized by cognitive rigidity, schizophrenia, obsessive-compulsive disorder, depression, pain, inflammation, migraine, and cluster headache.

Sumatriptan (Standard) is the analytical standard of Sumatriptan. This product is intended for research and analytical applications. Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan can be used for migraine headache research.

DOI hydrochloride (Standard) is the analytical standard of DOI hydrochloride (HY-103124). This product is intended for research and analytical applications. DOI hydrochloride is a serotonin 5-HT2A/2C receptor agonist with K_i values of 0.7 nM, 2.4 nM and 20 nM for h5-HT2A, h5-HT2C and h5-HT2B receptors, respectively. DOI hydrochloride can across the blood-brain barrier. DOI hydrochloride increases head twitches in mice.