2. Vías de señalización
  3. GPCR/G Protein
    Neuronal Signaling
  4. 5-HT Receptor
  5. 5-HT1 Receptor Isoform
  6. 5-HT1 Receptor Inhibitor

5-HT1 Receptor Inhibitor

5-HT1 Receptor Inhibitors (23):

Cat. No. Nombre del producto Efecto Pureza
  • HY-15414
    Vortioxetine
    		Inhibitor 98.61%
    Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (Ki: 15 nM, 33 nM).
  • HY-179724
    PZ-1657
    		Inhibitor
    PZ-1657 (Compound 57) is an orally active, blood-brain barrier permeable, highly selective, and metabolically stable 5-HT7 receptor inverse agonist with a Ki 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.
  • HY-15414A
    Vortioxetine hydrobromide
    		Inhibitor 99.87%
    Vortioxetine (Lu AA 21004) hydrobromide is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM).
  • HY-10349A
    WAY-100635 maleate
    		Inhibitor 99.57%
    WAY-100635 maleate is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki 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.
  • HY-124591
    TC-2153
    		Inhibitor 98.19%
    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.
  • HY-W050162
    (E)-3,4,5-Trimethoxycinnamic acid
    		Inhibitor 99.90%
    (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 GABAA/BZ receptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to 5-HT2C and 5-HT1A 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.
  • HY-W009754
    Antidepressant agent 10
    		Inhibitor 99.96%
    Antidepressant agent 10 (Compound 4) is an orally active compound. Antidepressant agent 10 has IC50 values of 190 nM and 110 nM for 5-HT1A and 5-HT2, respectively. Antidepressant agent 10 can be used in the research of mental disorders.
  • HY-15414R
    Vortioxetine (Standard)
    		Inhibitor
    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-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM).
  • HY-10351A
    Robalzotan hydrochloride
    		Inhibitor 99.5%
    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.
  • HY-14261S
    Vilazodone-d8
    		Inhibitor 99.0%
    Vilazodone-d8 is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist.
  • HY-12709
    ARC 239
    		Inhibitor 99.71%
    ARC 239 is an α2B/C-adrenergic receptor antagonist with pKi of 7.06 and 6.95 for rat kidney α2B and human α2C, respectively. ARC 239 also inhibits 5-HT1A receptor with a Ki of 63.1 nM.
  • HY-N16471
    Escholtzine
    		Inhibitor
    Escholtzine is an Alkaloid. Escholtzine can be isolated from Eschscholzia californica. Escholtzine is a CYP3A4 inhibitor, 5-HT1A receptor inhibitor with a CYP3A4 IC50 of 13.4 μM, 5-HT1A EC50 of 11 μM. Escholtzine can be used for the research of anxiety, depression.
  • HY-15414AS
    Vortioxetine-d8 hydrobromide
    		Inhibitor 99.41%
    Vortioxetine-d8 (Lu AA 21004-d8) hydrobromide is the deuterated form of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM).
  • HY-10351
    Robalzotan
    		Inhibitor
    Robalzotan (NAD-​299) is a potent and selective 5-Hydroxytryptamine 1A (5-HT1A) inhibitor. Robalzotan increases the firing rate of 5-HT cells. Robalzotan induces 5-HT1A receptor occupancy. Robalzotan has the potential for the research of a cholinergic deficit in the central -nervous system.
  • HY-15414S
    Vortioxetine-d8
    		Inhibitor
    Vortioxetine-d8 (Lu AA 21004-d8) is a deuterated version of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM).
  • HY-179724A
    PZ-1657 hydrochloride
    		Inhibitor
    PZ-1657 hydrochloride (Compound 57) is a potent, selective and orally active 5-HT7 receptor inverse agonist with a Ki 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.
  • HY-129481
    LY 178210
    		Inhibitor
    LY 178210 (Compound 24) is a selective partial agonist of the 5-HT1A receptor, with Ki 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.
  • HY-144272
    AChE-IN-5
    		Inhibitor
    AChE-IN-5 (compound 5) exhibits strong in vitro bioactivity against AChE/5-HT1A/SERT and exhibits good BBB permeability. AChE-IN-5 shows IC50 value 2.29 nM against AChE, EC50 value 58.6 nM against 5-HT1A and IC50 value against SERT. Orally active.
  • HY-W296398
    5-Bromo-N,N-dimethyltryptamine
    		Inhibitor
    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-HT1A, 5-HT2B, 5-HT6, and 5-HT7.
  • HY-106489
    Adafenoxate
    		Inhibitor
    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.