5-HT7 Receptor
5-HT7 receptor (5-HT7R) is a G protein-coupled serotonin receptor encoded by HTR7 that primarily activates Gs-dependent adenylyl cyclase signaling and increases intracellular cyclic AMP, thereby regulating neuronal excitability, synaptic plasticity, circadian rhythm, learning, memory, and mood-associated functions[1][2]. The receptor also engages ERK/MAPK, Akt, mTOR, and Rho GTPase pathways through G protein-dependent mechanisms, linking serotonergic neurotransmission to cellular remodeling and neuroplasticity processes relevant to central nervous system function[3]. Mechanistically, 5-HT7R displays functional interactions with 5-HT1A receptors, and heterodimerization can alter downstream signaling, distinguishing 5-HT7R from related serotonin receptor isoforms that predominantly inhibit cyclic AMP production through Gi-coupled signaling[3]. In disease models, 5-HT7R has been implicated in depression, anxiety, cognitive dysfunction, epilepsy, sleep regulation, circadian rhythm disturbances, and intestinal inflammatory disorders, supporting its relevance as a therapeutic target across neuropsychiatric and inflammatory conditions[2][4][5]. Compared with other serotonin receptor subtypes, 5-HT7R exhibits unique splice variants and distinct pharmacological properties that influence receptor trafficking, constitutive activity, and ligand responsiveness[1]. For experimental applications, selective ligands including the brain-penetrant agonist LP-211 and antagonists such as SB-656104-A have enabled mechanistic studies of receptor signaling and evaluation of therapeutic potential in preclinical models[1].
References:
- [1]. Ogawa SK, et al. Volatile anesthetic effects on isolated GABA synapses and extrasynaptic receptors. Neuropharmacology. 2011 Mar;60(4):701-10. [Content Brief]
- [2]. Gottlieb N, et al. The 5-HT7 receptor system as a treatment target for mood and anxiety disorders: A systematic review. J Psychopharmacol. 2023 Dec;37(12):1167-1181. [Content Brief]
- [3]. Quintero-Villegas A, et al. Central nervous system effects of 5-HT7 receptors: a potential target for neurodegenerative diseases. Mol Med. 2022 Jun 20;28(1):70. [Content Brief]
- [4]. Kim JJ, et al. 5-HT7 receptor signaling: improved therapeutic strategy in gut disorders. Front Behav Neurosci. 2014 Dec 11;8:396. [Content Brief]
- [5]. Blattner KM, et al. Pharmacology and Therapeutic Potential of the 5-HT7 Receptor. ACS Chem Neurosci. 2019 Jan 16;10(1):89-119. [Content Brief]
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5-HT7 Receptor Related Products (89)
Related Products (89)
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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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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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Brilaroxazine
0 ImagesSynonyms: RP5063Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.
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Indophagolin
0 ImagesIndophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7.
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AVN-101 hydrochloride
0 ImagesAVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis.
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Aramisulpride
0 ImagesSynonyms: (R)-Amisulpride; (R)-Esamisulpride; (R)-DAN 2163Aramisulpride (R-(+)-Amisulpride) is the R-isomer of Amisulpride (HY-14545). Aramisulpride is a 5-HT7 receptor antagonist with a Ki value of 22 nM. Aramisulpride is a D2/D3 receptor antagonist with a Ki value of 140 nM for D2R and a Ki value of 13.9 nM for D3R. Aramisulpride can be used in psychiatric research.
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5-Carboxamidotryptamine
0 ImagesSynonyms: 5-CT5-Carboxamidotryptamine (5-CT) is a 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, 5-HT7 receptor agonist. 5-Carboxamidotryptamine has a Ki value of 4.6 nM for cloned human 5-HT5A receptor. 5-Carboxamidotryptamine causes a dose-dependent reduction in rectal temperature of mice.
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Esamisulpride
0 ImagesSynonyms: (S)-Amisulpride; (S)-Aramisulpride; (S)-DAN 2163Esamisulpride ((S)-Amisulpride) is the S-isomer of Amisulpride (HY-14545). Esamisulpride is a potent dopamine D2/D3 receptor antagonist with Ki values of 4.43 nM for D2R and 0.72 nM for D3R. Esamisulpride is a 5-HT7 receptor antagonist with a Ki of 900 nM. Esamisulpride can be used in the research of schizophrenia and depression.
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Vortioxetine (Standard)
0 ImagesSynonyms: Lu AA 21004 (Standard)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).
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Lurasidone metabolite 14326 hydrochloride
0 ImagesCat. No.: HY-G0002ALurasidone metabolite 14326 hydrochloride is a minor active metabolite of Lurasidone (HY-B0032A) generated via metabolism by CYP3A4. Lurasidone metabolite 14326 hydrochloride shares similar receptor-binding properties with Lurasidone, acting as an antagonist of the dopamine D2 receptor (dopamine D2 receptor), an antagonist of the serotonin 5-HT2A and 5-HT7 receptors (5-HT2A and 5-HT7 receptor), and a partial agonist of the serotonin 5-HT1A receptor. Lurasidone metabolite 14326 hydrochloride can be used in the research of schizophrenia and bipolar depression.
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FPT
0 ImagesFPT, a 2-Aminotetralin, is an efficacious partial agonist at 5-HT1AR, a full agonist at 5-HT1BR and 5-HT1DR with EC50s of 39.3 nM, 1.2 nM, 0.5 nM, respectively. FPT is a weak agonist at 5-HT7R. FPT shows in vivo efficacy as an antiepileptic in Fmr1 knockout mice and has anxiolytic-like and prosocial effects in Fmr1 knockout mice and other mouse models.
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LP 12 hydrochloride hydrate
0 ImagesCat. No.: HY-103105APurity: 99.0%LP 12 hydrochloride hydrate is a potent and selective 5-HT7 receptor agonist with a Ki of 0.13 nM. LP 12 hydrochloride hydrate displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (Ki values are 224 nM, 60.9 nM and >1000 nM, respectively).
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Octoclothepine
0 ImagesSynonyms: ClorotepineOctoclothepin (Clorotepine) is a D2 dopamine receptor antagonist and 5-HT2 serotonin receptor antagonist , with Ki values of 0.67 nM, 0.57 nM, and 0.19 nM for the dopamine D2, 5-HT2A, and 5-HT2C receptors, respectively. Octoclothepin also binds to adrenergic receptors, with Ki values of 0.66 nM, 0.56 nM, and 0.77 nM for α1a, α1b, and α1d, respectively. Octoclothepin can be used in schizophrenia research.
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ST1936
0 ImagesST1936 is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor.
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Lurasidone Hydrochloride (Standard)
0 ImagesSynonyms: SM-13496 Hydrochloride (Standard)Lurasidone (Hydrochloride) (Standard) is the analytical standard of Lurasidone (Hydrochloride). This product is intended for research and analytical applications. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
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LB-102
0 ImagesLB-102 is an orally active inhibitor of dopamine D2, D3, and 5-HT7 receptors, which can be used in research on schizophrenia and other psychiatric disorders.
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Vortioxetine-d8 hydrobromide
0 ImagesCat. No.: HY-15414ASSynonyms: Lu AA21004-d8 hydrobromideVortioxetine-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).
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SB-656104
0 ImagesCat. No.: HY-124135CAS No.: 446020-51-5SB-656104 is a potent antagonist of 5-HT7 receptor, with the pKi of 8.70, blocking 5-carboxamidotryptamine (5-CT) stimulated adenylyl cyclase activity.
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Methiothepin
0 ImagesCat. No.: HY-111491CAS No.: 20229-30-5Synonyms: Metitepine; Ro 8-6837Methiothepin (Metitepine; Ro 8-6837) 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).
