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 (454)
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![(E)-[10]-Shogaol](https://file.medchemexpress.com/product_pic/hy-n2434a.gif "Click to View (E)-[10]-Shogaol Product Detail")
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