5-HT₁ Receptor Inhibitor

Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial agonist of 5-HT_1B (K_i: 15 nM, 33 nM).

Vortioxetine (Lu AA 21004) hydrobromide is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial 5-HT_1B agonist (K_i: 15 nM, 33 nM).

WAY-100635 maleate is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC₅₀ value of 0.91 nM and K_i value of 0.39 nM. WAY-100635 maleate has pIC₅₀ values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 maleate is also a potent dopamine D₄ receptor agonist.

TC-2153 is a selective inhibitor of striatal-enriched protein tyrosine phosphatase (STEP), with psychotropic activity and low acute toxicity. TC-2153 increases the expression of brain-derived neurotropic factor (BDNF) in the brain. And it decreases MAOA and 5-HT1A receptors mRNA level in midbrain. TC-2153 also inhibits 5-HT2A receptor-mediated signaling.

(E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. (E)-3,4,5-Trimethoxycinnamic acid is an orally active and potent GABA_A/BZ receptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to 5-HT_2C and 5-HT_1A receptor, with IC₅₀ values of 2.5 and 7.6 μM, respectively. (E)-3,4,5-Trimethoxycinnamic acid shows anticonvulsant and sedative activity. (E)-3,4,5-Trimethoxycinnamic acid can be used for the research of insomnia, headache and epilepsy.

Antidepressant agent 10 is an orally active antidepressant compound that inhibits the serotonin 5-HT1A and 5-HT2 receptors, with corresponding IC₅₀ values of 190 nM and 110 nM, respectively.

Vortioxetine (Standard) is an analytical standard for Vortioxetine. This product is intended for research and analytical applications. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial 5-HT_1B agonist (K_i: 15 nM, 33 nM).

Robalzotan hydrochloride (NAD-​299 hydrochloride) is a potent and selective 5-Hydroxytryptamine 1A (5-HT1A) inhibitor. Robalzotan hydrochloride increases the firing rate of 5-HT cells. Robalzotan hydrochloride induces 5-HT1A receptor occupancy. Robalzotan hydrochloride has the potential for the research of a cholinergic deficit in the central -nervous system.

Vilazodone-d₈ is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist.

ARC 239 is an α2B/C-adrenergic receptor antagonist with pK_i of 7.06 and 6.95 for rat kidney α2B and human α2C, respectively. ARC 239 also inhibits 5-HT1A receptor with a K_i of 63.1 nM.

Escholtzine is an Alkaloid. Escholtzine can be isolated from Eschscholzia californica. Escholtzine is a CYP3A4 inhibitor, 5-HT_1A receptor inhibitor with a CYP3A4 IC₅₀ of 13.4 μM, 5-HT_1A EC₅₀ of 11 μM. Escholtzine can be used for the research of anxiety, depression.

Vortioxetine-d₈ (Lu AA 21004-d₈) hydrobromide is the deuterated form of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial 5-HT_1B agonist (K_i: 15 nM, 33 nM).

Vortioxetine-d₈ (Lu AA 21004-d₈) is a deuterated version of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial 5-HT_1B agonist (K_i: 15 nM, 33 nM).

PZ-1657 (Compound 57) is an orally active, blood-brain barrier permeable, highly selective, and metabolically stable 5-HT₇ receptor inverse agonist with a K_i value of 5 nM. PZ-1657 inhibits constitutive cyclic adenosine monophosphate (cAMP) production mediated by the Gs signaling pathway (EC₅₀ value of 2.93 nM). PZ-1657 inhibits CYP3A4 P450 (IC₅₀ = 12.2 μM) and hERG channels. PZ-1657 reduces 5-HT₇ receptor-mediated MMP-9 activity. PZ-1657 reverses Phencyclidine-induced cognitive impairment. PZ-1657 possesses antidepressant properties.

PZ-1657 hydrochloride (Compound 57) is a potent, selective and orally active 5-HT7 receptor inverse agonist with a K_i of 5 nM. PZ-1657 hydrochloride can inhibit the constitutive cAMP production mediated by the Gs signaling pathway (EC₅₀ = 2.93 nM). PZ-1657 hydrochloride can significantly reduce the MMP-9 activity mediated by 5-HT7 receptors in the hippocampus of mice, and the effect is comparable to that of SB-269970 (HY-15370). PZ-1657 hydrochloride can reverse the cognitive deficits observed in the rat novel object recognition test induced by Phencyclidine without affecting the animals' spontaneous activities. PZ-1657 hydrochloride can be used for the research of emotional disorders, such as depression and bipolar disorder.

LY 178210 (Compound 24) is a selective partial agonist of the 5-HT1A receptor, with K_i values ​​of 0.67 and 380 nM for the 5-HT1A and 5-HT1D receptors, respectively. LY 178210 has almost no activity against α₂-adrenergic receptors, 5-HT₂, and other neurotransmitter receptors. LY 178210 inhibits Foscolin-stimulated cyclase activity, but its maximum potency is lower than that of the full agonist 8-OH-DPAT (HY-112061). LY 178210 significantly reduces 5-hydroxyindoleacetic acid (5-HIAA) levels in the greater hypothalamus and increases serum corticosterone concentrations.

AChE-IN-5 (compound 5) exhibits strong in vitro bioactivity against AChE/5-HT_1A/SERT and exhibits good BBB permeability. AChE-IN-5 shows IC₅₀ value 2.29 nM against AChE, EC₅₀ value 58.6 nM against 5-HT_1A and IC₅₀ value against SERT. Orally active.

5-Bromo-N,N-dimethyltryptamine, an active metabolite, is an antidepressant and sedative drug lead. 5-Bromo-N,N-dimethyltryptamine shows strong affinity towards 5-HT_1A, 5-HT_2B, 5-HT₆, and 5-HT₇.

Adafenoxate is a nootropic agent. Adafenoxate can improve Scopolamine (HY-N0296)-impaired memory, exploratory behavior and physical capabilities. Adafenoxate can be used for the research of neurological disease.