5-HT₇ Receptor Agonist

8-OH-DPAT is a potent, brain-penetrant and selective 5-HT agonist, with a pIC₅₀ of 8.19 for 5-HT1A and a K_i of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC₅₀, 5.42), 5-HT (pIC₅₀ <5).

AP521 is an agonist of human 5-HT_1A receptor with an IC₅₀ of 94 nM.

Frovatriptan (succinate hydrate) (Standard) is the analytical standard of Frovatriptan (succinate hydrate). This product is intended for research and analytical applications. Frovatriptan 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.

AGH-194 is a 5-HT7 receptor agonist with a K_i 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.

LP-211 is a selective and blood brain barrier penetrant 5-HT₇ receptor agonist, with a K_i of 0.58 nM, with high selectivity over 5-HT_1A receptor (K_i, 188 nM) and D₂ receptor (K_i, 142 nM).

LP44 (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.

AS19 is a potent, selective 5-HT₇ receptor agonist with an IC₅₀ value of 0.83 nM and a K_i of 0.6 nM. AS19 is selective for 5-HT₇ over 5-HT_1A, 5-HT_1B, 5-HT_1D, and 5-HT_5A receptors (K_is = 89.7 nM, 490 nM, 6.6 nM and 98.5 nM, respectively). AS19 enhances memory consolidation and reverses Scopolamine- or Dizocilpine-induced amnesia.

5-Carboxamidotryptamine maleate (5-CT maleate) is a potent 5-HT_1A, 5-HT_1B, 5-HT_1D, 5-HT₅ and 5-HT₇ receptors agonist.

Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active 5-HT_1B (pK₅₀ of 8.2) and 5-HT_1D receptor agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for 5-HT_1B and 5-HT_1D over 5-HT_1A, 5-HT_1F, 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.

5-Carboxamidotryptamine (5-CT) is a 5-HT_1A, 5-HT_1B, 5-HT_1D, 5-HT_5A, 5-HT₇ receptor agonist. 5-Carboxamidotryptamine has a K_i value of 4.6 nM for cloned human 5-HT_5A receptor. 5-Carboxamidotryptamine causes a dose-dependent reduction in rectal temperature of mice.

FPT, a 2-Aminotetralin, is an efficacious partial agonist at 5-HT_1AR, a full agonist at 5-HT_1BR and 5-HT_1DR 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.

LP 12 hydrochloride hydrate is a potent and selective 5-HT7 receptor agonist with a K_i of 0.13 nM. LP 12 hydrochloride hydrate displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (K_i values are 224 nM, 60.9 nM and >1000 nM, respectively).

ST1936 is a selective, nanomolar affinity 5-HT₆ receptor agonist with K_i values of 13 nM, 168 nM and 245 nM for human 5-HT₆, 5-HT₇ and 5-HT_2B receptors, respectively. ST1936 also shows moderate affinity (K_i of 300 nM) for human and rat α2 adrenergic receptor.

Frovatriptan-d₃ (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan 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.

AGH-107 is a high selective and brain-penetrant agonist of 5-HT7 receptor, with a K_i of 6 nM and EC₅₀ of 19 nM. AGH-107 exhibits high selectivity over related CNS targets, high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures.

Ensaculin free base (KA-672) is a NMDA antagonist and have high affinities to serotonergic 5-HT_1A and 5-HT₇ receptors, adrenergic α₁, and dopaminergic D₂ and D₃ receptors. Ensaculin free base is a memory-enhancing agent. Ensaculin free base has the potential as an antidementia agent acting on various transmitter systems.

5-HT7 agonist 2 is a potent 5-HT₇ receptor agonist with an IC₅₀ value of 28.7 nM. 5-HT7 agonist 2 can be used for research of central nervous system (CNS) disorders.

LP 12 hydrochloride (compound 21) is a potent and selective 5-HT7 receptor agonist with a K_i of 0.13 nM. LP 12 hydrochloride displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (K_i values are 224 nM, 60.9 nM and >1000 nM, respectively).

ST1936 oxalate is a selective, nanomolar affinity 5-HT₆ receptor agonist with K_i values of 13 nM, 168 nM and 245 nM for human 5-HT₆, 5-HT₇ and 5-HT_2B receptors, respectively. ST1936 oxalate also shows moderate affinity (K_i of 300 nM) for human and rat α2 adrenergic receptor.

CSP-2503 is a potent and selective 5-HT_1A receptor agonist , with an EC₅₀ of 0.15 μM and a K_i of 4.1 nM. CSP-2503 exhibits excellent selectivity over α1-adrenoceptors (K_i > 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.