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]
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5-HT1 Receptor Related Products (456)
Related Products (456)
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Rotigotine
0 ImagesSynonyms: N-0923; (-)-N 0437Rotigotine is a potent dopamine receptor agonist with Ki values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research.
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Ziprasidone
0 ImagesSynonyms: CP-88059Ziprasidone (CP-88059), an orally active antipsychotic agent, is a combined 5-HT and dopamine receptor antagonist. Ziprasidone mesylate trihydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM).
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Spiperone
0 ImagesSpiperone (Spiroperidol) is a potent dopamine D2, serotonin 5-HT1A, and serotonin 5-HT2A antagonist. Spiperone is also a labelled ligand for neuroleptic receptors. Spiperone enhances intracellular calcium level and inhibits the Wnt signaling pathway. Spiperone has the potential for the research of neurology diseases.
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Rotigotine Hydrochloride
0 ImagesSynonyms: N-0923 HydrochlorideRotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Ki of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
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Lurasidone
0 ImagesSynonyms: SM-13496Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
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Alprenolol
0 ImagesSynonyms: (RS)-Alprenolol; dl-AlprenololAlprenolol ((RS)-Alprenolol; dl-Alprenolol) is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent.
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Buspirone hydrochloride
0 ImagesBuspirone hydrochloride is a 5-HT1A receptor agonist. Buspirone hydrochloride can be used for anxiety and depression research.
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Cariprazine hydrochloride
0 ImagesSynonyms: RGH188 hydrochlorideCariprazine hydrochloride 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).
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Methiothepin mesylate
0 ImagesSynonyms: Metitepine mesylate; Ro 8-6837 mesylateMethiothepin (Metitepine) mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
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8-OH-DPAT hydrobromide
0 ImagesSynonyms: 8-Hydroxy-DPAT hydrobromide8-OH-DPAT (8-Hydroxy-DPAT) hydrobromide is a potent, brain-penetrant and selective 5-HT1A agonist with a pIC50 of 8.19. 8-OH-DPAT hydrobromide has selectivity of almost 1000 fold for a subtype of the 5-HT1 binding site.
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Asenapine maleate
0 ImagesSynonyms: Org 5222 maleateAsenapine (Org 5222) maleate, a brain-penetrant atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine maleate can be used in the research of schizophrenia and bipolar disorder.
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Gepirone
0 ImagesGepirone is a selective and affinitive 5-HT1A agonist. Gepirone binds selectively to 5-HT1A receptor binding site. Gepirone acts as an antidepressant agent can be used for anxiety and major depressive disorder research.
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SB-224289 hydrochloride
0 ImagesSynonyms: SB-224289ASB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect.
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Alprenolol hydrochloride
0 ImagesSynonyms: (RS)-Alprenolol hydrochloride; dl-Alprenolol hydrochlorideAlprenolol ((RS)-Alprenolol; dl-Alprenolol) hydrochloride is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol hydrochloride is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent.
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LP-211
0 ImagesLP-211 is a selective and blood brain barrier penetrant 5-HT7 receptor agonist, with a Ki of 0.58 nM, with high selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM).
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BMY 7378
0 ImagesBMY 7378 is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 is a 5-HT1A receptor partial agonist.
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Trimipramine maleate
0 ImagesTrimipramine maleate is a 5-HT receptor antagonist, with blood-brain barrier permeability. Trimipramine maleate has pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine maleate has vascular activity and anxiolytic efficacy.
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RS 67333 hydrochloride
0 ImagesRS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pKi of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research.
