5-HT1 Receptor
5-HT1 receptors are serotonin-activated GPCRs within the 5-HT receptor family, excluding ionotropic 5-HT3 receptors[1]. Mechanistically, 5-HT1D receptors inhibit glutamate release, while 5-HT1A receptors inhibit NMDA/AMPA-linked cGMP responses in rat cerebellum[2]. In antidepressant research, presynaptic 5-HT1A and 5-HT1B autoreceptors reduce serotonergic function, whereas postsynaptic 5-HT1A stimulation appears beneficial[3]. Compared with related isoforms, 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT1F share high sequence homology, which complicates subtype-specific ligand design[4]. For experimental applications, 2-aminotetralin-type agonists showed high affinity and subtype-dependent efficacy across 5-HT1 receptors, supporting selective ligand discovery[4].
References:
- [1]. Barnes NM, et al. International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function. Pharmacol Rev. 2021 Jan;73(1):310-520. [Content Brief]
- [2]. Maura G, et al. Serotonin 5-HT1D and 5-HT1A receptors respectively mediate inhibition of glutamate release and inhibition of cyclic GMP production in rat cerebellum in vitro. J Neurochem. 1996 Jan;66(1):203-9. [Content Brief]
- [3]. Artigas F. Serotonin receptors involved in antidepressant effects. Pharmacol Ther. 2013 Jan;137(1):119-31. doi: 10.1016/j.pharmthera.2012.09.006. Epub 2012 Sep 26. PMID: 23022360. et al. Serotonin receptors involved in antidepressant effects. Pharmacol Ther. 2013 Jan;137(1):119-31. [Content Brief]
- [4]. McGlynn RP, et al. Development of 2-Aminotetralin-Type Serotonin 5-HT1 Agonists: Molecular Determinants for Selective Binding and Signaling at 5-HT1A , 5-HT1B , 5-HT1D , and 5-HT1F Receptors. ACS Chem Neurosci. 2024 Jan 17;15(2):357-370. [Content Brief]
All Product Categories
-
5-HT1 Receptor Inhibitors
(24)
View all products
-
5-HT1 Receptor Agonists
(231)
View all products
-
5-HT1 Receptor Antagonists
(117)
View all products
-
5-HT1 Receptor Activator
(1)
View all products
-
5-HT1 Receptor Modulators
(51)
View all products
-
5-HT1 Receptor Controls
(2)
View all products
-
5-HT1 Receptor Ligands
(5)
View all products
-
5-HT1 Receptor Related Products (451)
Related Products (451)
-
SCH-23390 hydrochloride
0 ImagesSynonyms: R-(+)-SCH-23390 hydrochlorideSCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis 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-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
-
Vortioxetine
0 ImagesSynonyms: Lu AA 21004Vortioxetine (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).
-
Volinanserin
0 ImagesSynonyms: MDL100907; M 100907Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity.
-
WAY-100635
0 ImagesWAY-100635 is a potent and selective 5-HT1A Receptor antagonist with a pIC50 of 8.87, an apparent pA2 of 9.71. WAY-100635 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 has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D4 receptor agonist.
-
8-OH-DPAT
0 ImagesSynonyms: 8-Hydroxy-DPAT8-OH-DPAT is a potent, brain-penetrant 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).
-
Quetiapine hemifumarate
0 ImagesQuetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.
-
Antidepressant agent 10
0 ImagesAntidepressant 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.
-
Quetiapine hemifumarate (Standard)
0 ImagesQuetiapine (hemifumarate) (Standard) is the analytical standard of Quetiapine (hemifumarate). This product is intended for research and analytical applications. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.
-
Aripiprazole
0 ImagesSynonyms: OPC-14597Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19.
-
Brexpiprazole
0 ImagesSynonyms: OPC-34712Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM).
-
Vilazodone
0 ImagesSynonyms: EMD 68843; SB659746AVilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders.
-
Vortioxetine hydrobromide
0 ImagesSynonyms: Lu AA21004 hydrobromideVortioxetine (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).
-
Buspirone
0 ImagesBuspirone is an orally active 5-HT1A receptor agonist, and a dopamine D2 autoreceptorsant antagonist. Buspirone is an anxiolytic agent, and can be used for the generalized anxiety disorder research.
-
Pindolol
0 ImagesSynonyms: LB-46Pindolol (LB-46) is the antagonist for 5-HT 1A (Ki=33 nM) and 5-HT 1B. Pindolol is the antagonist for β1/β2-adrenergic receptor. Pindolol exhibits anti-anxiety and antidepressant effects.
-
Quetiapine
0 ImagesSynonyms: ICI204636Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.
-
GR 113808
0 ImagesGR 113808 is a potent and highly selective 5-HT4 receptor antagonist (pKb= 8.8). GR 113808 shows 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors.
-
Vilazodone Hydrochloride
0 ImagesSynonyms: EMD 68843 Hydrochloride; SB659746A HydrochlorideVilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
-
Nuciferine
0 ImagesNuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
-
Cariprazine
0 ImagesSynonyms: RGH-188Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
-
WAY-100635 maleate
0 ImagesWAY-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.
