5-HT Receptor

Deramciclane has a high affinity for 5-HT_2A and 5-HT_2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT_2C receptors without direct stimulatory agonist.

SB-616234-A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.

Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a K_i of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT₃Rs with a K_i value of 1.2 nM.

YM348 is a potent and orally active 5-HT_2C receptor agonist, which shows a high affinity for cloned human 5-HT_2C receptor (K_i: 0.89 nM).

7-Desmethyl-agomelatine-d₃ is a deuterium labeled 7-Desmethyl-agomelatine. 7-Desmethyl-agomelatine is a metabolite of Agomelatine.

5-HT4 antagonist 1 is a 5-HT₄ receptor antagonist with a pK_i of 9.6.

Repinotan hydrochloride (BAY x 3702) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with K_i values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus Repinotan hydrochloride has a weak affinity for other related receptors. Repinotan hydrochloride has pronounced neuroprotective effects.

Clothiapine, an atypical antipsychotic agent, shares with clozapine its strong antiserotonergic properties.

Desmethyl cariprazine-d₈ is the deuterium labeled Desmethyl cariprazine (HY-100656). Desmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotonin receptors, showing a pEC₅₀ of 8.90 at human D2 receptors, a pEC₅₀ of 8.09 at D3 receptors, and a pEC₅₀ of 6.28 at 5-HT1A receptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT1A receptors, and suppresses serotonin-induced Ca²⁺ release at 5-HT2B receptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.

Didesmethyl cariprazine-d₈ is the deuterium labeled Didesmethyl cariprazine (HY-100658). Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (K_i: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons.

Harmine (Standard) is the analytical standard of Harmine. This product is intended for research and analytical applications. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.

Hordenine hydrochloride (Ordenina hydrochloride; Peyocactine hydrochloride) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine hydrochloride inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine hydrochloride promotes M2 macrophage polarization, restores blood-milk barrier integrity, alleviates oxidative stress by reducing ROS and MDA, and attenuates LPS-induced lung injury and pulmonary edema. Hordenine hydrochloride inhibits cAMP production, CREB phosphorylation, and MITF expression, thereby suppressing melanin synthesis in melanocytes and reconstructed epidermis. Hordenine hydrochloride activates the Wnt/β-catenin signaling pathway, promotes dermal papilla cell proliferation and hair shaft elongation, and accelerates hair regeneration. Hordenine hydrochloride activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine hydrochloride inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine hydrochloride limits alcohol intake, reduces relapse drinking behavior, and modulates alcohol-induced conditioned place preference. Hordenine hydrochloride can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder.

S)-Praziquantel is a inactive distomer of R-praziquantel.

cis-Urocanic acid-¹³C₃ is the ¹³C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.

Harmine (GMP) (Telepathine (GMP)) is Harmine (HY-N0737A) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT_2A serotonin receptor, with an K_i of 397 nM.

MT-1207 is an orally active, selective adrenergic α1 and 5-HT2A receptor antagonist. The IC₅₀ values of MT-1207 for α1A, α1B, α1D, and 5-HT2A are <0.1 nM, 0.15 nM, 1.40 nM, and 0.27 nM, respectively. MT-1207 induces vasodilation, improves baroreflex sensitivity, and reduces heart rate in isolated hearts. MT-1207 lowers blood pressure, protects the heart, brain, and kidneys, improves cognition, delays stroke, reduces mortality, and lowers uric acid without impairing renal function in SHR/2K1C/2K2C models. MT-1207 exhibits high plasma protein binding, resistance to plasma esterases, and NADPH-dependent hepatic metabolism. MT-1207 can be used for research related to hypertension.

S-15535 is a highly selective 5-HT_1A receptor ligand. S-15535 is an antagonist of postsynaptic 5-HT_1A receptors and an agonist of presynaptic 5-HT_1A receptors. S-15535 can be used in research on psychiatric disorders, such as anti-anxiety.

AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (K_i=91 pM).

Clozapine-d₈ is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors.

Aramisulpride (R-(+)-Amisulpride) is the R-isomer of Amisulpride (HY-14545). Aramisulpride is a 5-HT₇ receptor antagonist with a K_i value of 22 nM. Aramisulpride is a D₂/D₃ receptor antagonist with a K_i value of 140 nM for D₂R and a K_i value of 13.9 nM for D₃R. Aramisulpride can be used in psychiatric research.