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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Tiospirone
0 ImagesCat. No.: HY-105034CAS No.: 87691-91-6Synonyms: BMY 13859-1 free baseTiospirone is a 5-HT2 receptor antagonist with affinity for D2, 5-HT1a, and 5-HT7, and sigma receptors. Tiospirone decreases consumption of ethanol while increasing food intake of rats. Tiospirone can also reduce the reinforcing properties of Cocaine exhibited in the conditioned place preference paradigm.
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Lurasidone (Standard)
0 ImagesSynonyms: SM-13496 (Standard)Lurasidone (Standard) is the analytical standard of Lurasidone. This product is intended for research and analytical applications. Lurasidone (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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WAY 163909 (hydrochloride)
0 ImagesCat. No.: HY-15401ACAS No.: 428868-35-3WAY 163909 hydrochloride is an orally active, blood-brain barrier permeable 5-HT2C receptor-selective agonist. WAY 163909 hydrochloride exhibits an EC50 of 8 nM and a Ki of 10.5 nM for h5-HT2C. Instead of triggering apoptosis, WAY 163909 hydrochloride induces anorectic, antipsychotic-like, antidepressant-like, anti-aggressive and anti-compulsive effects. WAY 163909 hydrochloride alleviates ketamine-induced hypothermia, but impairs sexual function at high doses. With rapid antidepressant-like properties, WAY 163909 hydrochloride can be used in research related to obesity, schizophrenia, depression, obsessive-compulsive disorder, and anesthesia-induced hypothermia.
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SB-699551 free base
0 ImagesCat. No.: HY-136700CAS No.: 791789-61-2SB-699551 free base is a selective and brain penetrant 5-HT5A receptor antagonist with a pKi of 8.2 nM. SB-699551 free base shows high selectivity over most other 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptor. SB-699551 free base disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, alters CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 phosphorylation in breast tumor cells. SB-699551 free base can be used for the research of anxiety, breast cancer, and Alzheimer's disease.
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Vortioxetine-d4
0 ImagesCat. No.: HY-15414S2Synonyms: Lu AA 21004-d4Vortioxetine-d4 (Lu AA 21004-d4) is the deuterium labeled Vortioxetine (HY-15414). Vortioxetine 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).
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Brilaroxazine (Standard)
0 ImagesSynonyms: RP5063 (Standard)Brilaroxazine (Standard) is the analytical standard of Brilaroxazine. This product is intended for research and analytical applications. Brilaroxazine (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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5-HT7R antagonist 4
0 ImagesCat. No.: HY-116581CAS No.: 1386927-90-75-HT7R antagonist 4 (Compound 4) is a potent 5-HT7 receptor antagonist (Ki=2.6 nM) with low binding affinity for the 5-HT1A receptor (Ki= 476 nM). 5-HT7R antagonist 4 is promising for research of neurological diseases.
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Vortioxetine-d6
0 ImagesCat. No.: HY-15414S1CAS No.: 1629684-23-6Synonyms: Lu AA 21004-d6Vortioxetine-d6 (Lu AA 21004-d6) is the deuterium labeled Vortioxetine (HY-B1490A). 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 agonist of 5-HT1B (Ki: 15 nM, 33 nM).
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Lurasidone metabolite 14326
0 ImagesCat. No.: HY-G0002CAS No.: 186204-33-1Lurasidone metabolite 14326 is a minor active metabolite of Lurasidone (HY-B0032A) generated via metabolism by CYP3A4. Lurasidone metabolite 14326 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 can be used in the research of schizophrenia and bipolar depression.
