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)
Related Products (454)
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Befiradol
0 ImagesSynonyms: NLX-112; F13640Befiradol (NLX-112) is a highly selective 5-HT1A receptor agonist that acts on both presynaptic and postsynaptic sites. Befiradol attenuates sedative agent-induced respiratory depression in neonatal and adult rats. Befiradol reduces the duration of sedative agent-induced analgesia and sedation in adult rats. Befiradol can be used in studies related to opioid-induced respiratory depression.
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AS19
0 ImagesAS19 is a potent, selective 5-HT7 receptor agonist with an IC50 value of 0.83 nM and a Ki of 0.6 nM. AS19 is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis = 89.7 nM, 490 nM, 6.6 nM and 98.5 nM, respectively). AS19 enhances memory consolidation and reverses Scopolamine- or Dizocilpine-induced amnesia.
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Gepirone hydrochloride
0 ImagesGepirone is a selective 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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2-(1-Piperazinyl)pyrimidine
0 Images2-(1-Piperazinyl)pyrimidine is an orally effective α2-adrenoceptor antagonist and 5-HT1A receptor agonist. 2-(1-Piperazinyl)pyrimidine is an in vivo metabolite related to buspirone. 2-(1-Piperazinyl)pyrimidine modulates excitatory synaptic transmission in the hippocampus and the release of monoamine transmitters such as norepinephrine and 5-HT by blocking α2-adrenoceptor and activating 5-HT1A Receptor. 2-(1-Piperazinyl)pyrimidine is used in research on psychiatric disorders such as anxiety and depression.
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Xaliproden hydrochloride
0 ImagesSynonyms: SR57746A; SR57746 hydrochlorideXaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety.
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Naratriptan hydrochloride
0 ImagesSynonyms: GR-85548A hydrochlorideNaratriptan (GR-85548A) hydrochloride is a selective 5-HT1B/1D receptor agonist. Naratriptan hydrochloride is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan hydrochloride also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan hydrochloride is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms.
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Ziprasidone hydrochloride
0 ImagesSynonyms: CP-88059 hydrochlorideZiprasidone (CP-88059) hydrochloride is an orally active combined 5-HT and dopamine receptor antagonist. Ziprasidone hydrochloride 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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Ocaperidone
0 ImagesSynonyms: R79598Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT2, a1-adrenergic receptor, dopamine D2, histamine H1 and a2-adrenergic receptor, respectively, and a pEC50 and pKi of 7.60 and 8.08 for h5-HT1A.
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5-Carboxamidotryptamine maleate
0 ImagesSynonyms: 5-CT maleate5-Carboxamidotryptamine maleate (5-CT maleate) is a potent 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5 and 5-HT7 receptors agonist.
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TC-2153
0 ImagesTC-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.
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SB-216641A
0 ImagesSynonyms: SB-216641 hydrochlorideSB-216641A (SB-216641 hydrochloride) is a selective antagonist of 5-HT1B/D receptor. SB-216641A shows high affinity and selectivity for h5-HT1B receptors over h5-HT1D receptors. SB-216641A inhibits the function of SKF-99101H.
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Frovatriptan succinate hydrate
0 ImagesSynonyms: (R)-Frovatriptan succinate hydrate; SB 209509 succinate hydrate; VML 251 succinate hydrateFrovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research.
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CP 93129 dihydrochloride
0 ImagesCP 93129 dihydrochloride is a potent 5HT1B receptor agonist. CP 93129 dihydrochloride has the potential for parkinson's disease research.
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(E)-3,4,5-Trimethoxycinnamic acid
0 ImagesSynonyms: TMCA(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.
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Sarizotan
0 ImagesSynonyms: EMD 128130Sarizotan (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively.
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PNU-142633
0 ImagesPNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy.
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Hypidone hydrochloride
0 ImagesSynonyms: YL0919Hypidone hydrochloride (YL0919) is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective 5-HT1A receptor agonist (Ki=0.19 nM). Hypidone hydrochloride inhibits the uptake of [3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC50s of 1.78 nM and 1.93 nM, respectively. Hypidone hydrochloride shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder.
