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 (88)
Related Products (88)
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Vortioxetine
0 ImagesSynonyms: Lu AA 21004Vortioxetine (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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8-OH-DPAT
0 ImagesSynonyms: 8-Hydroxy-DPAT8-OH-DPAT is a potent, brain-penetrant and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A and a Ki of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).
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Vortioxetine hydrobromide
0 ImagesSynonyms: Lu AA21004 hydrobromideVortioxetine (Lu AA 21004) hydrobromide 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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Nuciferine
0 ImagesNuciferine 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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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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AGH-194
0 ImagesCat. No.: HY-181984AGH-194 is a 5-HT7 receptor agonist with a Ki value of 2 nM. AGH-194 activates Gs protein-coupled signaling pathways associated with neuroprotection and neurite outgrowth, and stimulates neurite outgrowth in neuronal cells. AGH-194 reduces cell damage in undifferentiated neuronal cells. AGH-194 can be used in the research of neurodegenerative diseases.
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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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Lurasidone
0 ImagesSynonyms: SM-13496Lurasidone (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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Amisulpride
0 ImagesSynonyms: (Rac)-Aramisulpride; (Rac)-Esamisulpride; DAN 2163Amisulpride ((Rac)-Aramisulpride) is a racemic (50:50) mixture of the R-Amisulpride (HY-109167) and S-Amisulpride (HY-126068). Amisulpride is a dopamine D2/D3 receptor antagonist with Ki values of 2.8 and 3.2 nM for human dopamine b>D2 and b>D3, respectively. Amisulpride is a 5-HT7 receptor antagonist with a Ki of 44 nM. Amisulpride can be used in psychiatric research.
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Methiothepin mesylate
0 ImagesSynonyms: Metitepine mesylate; Ro 8-6837 mesylateMethiothepin (Metitepine) mesylate 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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Metergoline
0 ImagesMetergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na+ channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation.
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LP-211
0 ImagesLP-211 is a selective and blood brain barrier penetrant 5-HT7 receptor agonist, with a Ki of 0.58 nM, with high selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM).
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SB 258719
0 ImagesSB 258719 is a selective 5-HT7 receptor antagonist with high affinity (pKi=7.5) for the receptor. SB 258719 can be used for the research of cancer and neurological disease.
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JNJ-18038683
0 ImagesJNJ-18038683 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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Lurasidone Hydrochloride
0 ImagesSynonyms: SM-13496 HydrochlorideLurasidone (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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Norquetiapine
0 ImagesSynonyms: N-DesalkylquetiapineNorquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation.
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LP44 hydrochloride
0 ImagesLP44 (hydrochloride) is a selective 5-HT7 agonist with Ki of 0.22 nM. LP44 (hydrochloride) induces hypothermic effect in a dose-dependent manner by intracerebroventricular injection. LP44 (hydrochloride) not causes considerable hypothermic response by intraperitoneal administration.
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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.
