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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ST1936 oxalate
0 ImagesCat. No.: HY-103110ACAS No.: 1782228-83-4ST1936 oxalate 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 oxalate also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor.
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SB 258741 hydrochloride
0 ImagesCat. No.: HY-136678ASB 258741 hydrochloride is a specific 5-HT7 receptor antagonist and can be used for the research of schizophrenia.
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5-Bromo-N,N-dimethyltryptamine
0 ImagesCat. No.: HY-W296398CAS No.: 17274-65-6Synonyms: 5-Bromo-N,N-DMT5-Bromo-N,N-dimethyltryptamine, an active metabolite, is an antidepressant and sedative drug lead. 5-Bromo-N,N-dimethyltryptamine shows strong affinity towards 5-HT1A, 5-HT2B, 5-HT6, and 5-HT7.
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JNJ-18038683 free base
0 ImagesCat. No.: HY-19889ACAS No.: 851373-91-6JNJ-18038683 free base is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist, with pKis of 8.19, 8.20 for rat and human 5-HT7 in HEK293 cells, respectively.
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CSP-2503
0 ImagesCat. No.: HY-180372CAS No.: 581813-10-7CSP-2503 is a potent and selective 5-HT1A receptor agonist , with an EC50 of 0.15 μM and a Ki of 4.1 nM. CSP-2503 exhibits excellent selectivity over α1-adrenoceptors (Ki > 1000 nM), 5-HT4 receptors, and benzodiazepine receptors. CSP-2503 inhibits cAMP increase in vitro and exhibits anxiolytic activity in vivo. CSP-2503 can be used for the research of anxiety-related disorders.
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5-HT7 receptor ligand 2
0 ImagesCat. No.: HY-1594925-HT7 receptor ligand 2 (compound 32) is an arylpiperazinehydrazine ligand for 5-HT7R (Ki=178 nM). 5-HT7 receptor ligand 2 has good membrane permeability, low hepatotoxicity and cardiotoxicity, and high plasma protein binding. 5-HT7 receptor ligand 2 shows neuroprotective effects in SH-SY5Y cells and can be used for the study of central nervous system related diseases.
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DR4485 hydrochloride
0 ImagesCat. No.: HY-103126CAS No.: 402942-53-4DR4485 (hydrochloride) is an orally active and selective 5-HT7 antagonist (pKi=8.14).
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PZ-1129
0 ImagesCat. No.: HY-179725CAS No.: 1919029-61-0PZ-1129 is a selective 5-HT7 receptor ligand with a Ki of 7 nM. PZ-1129 shows Ki values of 159 and 24 nM for 5-HT1A receptor and D2 receptor. PZ-1129 can inhibit the constitutive cAMP production mediated by the Gs signaling pathway (EC50 = 13.7 nM). PZ-1129 can be used for the research of emotional disorders, such as depression and bipolar disorder.
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Methiothepin maleate
0 ImagesCat. No.: HY-101009CAS No.: 19728-88-2Synonyms: Metitepine maleate; Ro-8-6837 maleateMethiothepin maleate 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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E-55888
0 ImagesCat. No.: HY-113866CAS No.: 1034142-33-0
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5-HT7 agonist 1
0 ImagesCat. No.: HY-109527CAS No.: 334974-31-15-HT7 agonist 1 is a selective 5-HT7 receptor agonist, with an IC50 of 222.93 nM, can be used for the 5-HT7 receptor related disease, such as CNS disorders.
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Nuciferine (Standard)
0 ImagesNuciferine (Standard) is the analytical standard of Nuciferine. This product is intended for research and analytical applications. Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
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PDE4B/7A-IN-1
0 ImagesPDE4B/7A-IN-1 is a dual PDE4B/PDE7A inhibitor. PDE4B/7A-IN-1 shows IC50 values of 69.0 μM for PDE4B and 57.0 μM for PDE7A, as well as Ki values of 539 nM for 5-HT1A and 328 nM for 5-HT7. PDE4B/7A-IN-1 shows favorable membrane permeability. PDE4B/7A-IN-1 can be used for the study of cognitive impairment and depression.
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5-HT7R antagonist 3
0 ImagesCat. No.: HY-159942CAS No.: 1887043-58-45-HT7R antagonist 3 (Compound 6.4) is a selective 5-HT7R antagonist (Ki: 8 nM), with Ki of 511 nM (D2), 8930 nM (5-HT1A) and 5786 nM (5-HT2A), respectively. 5-HT7R antagonist 3 possesses antidepressant and anxiolytic effects in mice.
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DR-4004
0 ImagesCat. No.: HY-118575CAS No.: 201608-41-5DR-4004 is a 5-HT7 receptor antagonist that attenuates the decreased level of performance produced by mCPP and the performance levels after p-chloroamphetamine (PCA) lesion of the 5-HT system. DR-4004 also reverses amnesia induced by Scopolamine (HY-N0296) and Dizocilpine (HY-15084B). DR-4004 is promising for research of schizophrenia, cognitive deficits and atypical antipsychotic agents.
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WAY 208466
0 ImagesCat. No.: HY-W794785CAS No.: 633304-27-5WAY 208466 is a selective 5-HT6 receptor agonist with an EC50 of 7.3 nM. WAY-208466 increases GABA levels following both acute and chronic administration in the dorsolateral frontal cortex of rat models with stereotaxic surgery. WAY 208466 can be used for anxiety-related disorders like obsessive compulsive disorder (OCD) research.
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Frovatriptan succinate
0 ImagesCat. No.: HY-B1658BCAS No.: 158930-09-7Synonyms: (R)-Frovatriptan succinate; SB 209509 succinate; VML 251 succinateFrovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate 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 has the potential for migraine research.
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Lurasidone-d8-1 hydrochloride
0 ImagesCat. No.: HY-W654010Synonyms: SM-13496-d8-1 hydrochlorideLurasidone-d8-1 (hydrochloride) is deuterium labeled Lurasidone (Hydrochloride). 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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RS-64459-193
0 ImagesCat. No.: HY-120498CAS No.: 123882-89-3RS-64459-193 is a 5-HT1A receptor partial agonist with a Ki of 24.9 nM. RS-64459-193 also shows high affinity for 5-HT2C, 5-HT2A and 5-HT7 with pKi values of 6.87, 7.02, and 7.18, respectively. RS-64459-193 is almost devoid of activity at the m 5-HT3 receptor.
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SEP-4199
0 ImagesCat. No.: HY-14545BCAS No.: 2974362-88-2SEP4199 is an orally active 5-HT7 receptor ligand, with a Ki value of 66 nM for human 5-HT7R and 16 nM for human D2R. SEP4199 mediates antidepressant effects. SEP4199 is applicable for the research of bipolar depression.
