5-HT₇ Receptor Antagonist

SB-269970 hydrochloride is a potent, selective and brain-penetrant 5-HT7 receptor antagonist with a pK_i of 8.3. SB-269970 hydrochloride exhibits >50-fold selectivity against other 5-HT receptors.

Amisulpride ((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 K_i 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 K_i of 44 nM. Amisulpride can be used in psychiatric research.

Methiothepin (Metitepine) mesylate is a potent and non-selective 5-HT₂ receptor antagonist, with pK_ds of 7.10 (5-HT_1A), 7.28 (5HT_1B), 7.56 (5HT_1C), 6.99 (5HT_1D), 7.0 (5-HT_5A), 7.8 (5-HT_5B), 8.74 (5-HT₆), and 8.99 (5-HT₇), and pK_is of 8.50 (5HT_2A), 8.68 (5HT_2B), and 8.35 (5HT_2C).

Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pK_is of 8.64, 8.75 and 8.75 for 5-HT_2A, 5-HT_2B and 5-HT_2C, respectively. Metergoline is a high-affinity ligand for the h5-HT₇ receptor, with a K_i 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.

SB-269970 is a potent, selective and brain-penetrant 5-HT7 receptor antagonist with a pK_i of 8.3. SB-269970 exhibits >50-fold selectivity against other 5-HT receptors.

SB 258719 is a selective 5-HT₇ receptor antagonist with high affinity (pK_i=7.5) for the receptor. SB 258719 can be used for the research of cancer and neurological disease.

JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT₇) receptor antagonist, with pK_is of 8.19, 8.20 for rat and human 5-HT₇ in HEK293 cells, respectively.

Indophagolin 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 G_q-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-HT_1B, 5-HT_2B, 5-HT_4e, and 5-HT₇.

AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (K_i of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (K_i 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 (K_i of 0.58 nM) and adrenergic α2A, α2B, and α2C (K_i= 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.

Aramisulpride (R-(+)-Amisulpride) is the R-isomer of Amisulpride (HY-14545). Aramisulpride is a 5-HT₇ receptor antagonist with a K_i value of 22 nM. Aramisulpride is a D₂/D₃ receptor antagonist with a K_i value of 140 nM for D₂R and a K_i value of 13.9 nM for D₃R. Aramisulpride can be used in psychiatric research.

Esamisulpride ((S)-Amisulpride) is the S-isomer of Amisulpride (HY-14545). Esamisulpride is a potent dopamine D₂/D₃ receptor antagonist with K_i values of 4.43 nM for D₂R and 0.72 nM for D₃R. Esamisulpride is a 5-HT₇ receptor antagonist with a K_i of 900 nM. Esamisulpride can be used in the research of schizophrenia and depression.

Lurasidone 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.

Lurasidone-d₈ (hydrochloride) is the deuterium labeled Lurasidone, which is an inhibitor of Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C.

SB-656104 is a potent antagonist of 5-HT₇ receptor, with the pK_i of 8.70, blocking 5-carboxamidotryptamine (5-CT) stimulated adenylyl cyclase activity.

Methiothepin (Metitepine; Ro 8-6837) is a potent and non-selective 5-HT₂ receptor antagonist, with pK_ds of 7.10 (5-HT_1A), 7.28 (5HT_1B), 7.56 (5HT_1C), 6.99 (5HT_1D), 7.0 (5-HT_5A), 7.8 (5-HT_5B), 8.74 (5-HT₆), and 8.99 (5-HT₇), and pK_is of 8.50 (5HT_2A), 8.68 (5HT_2B), and 8.35 (5HT_2C).

Pellotine is an alkaloid that can be isolated from Lophophora. Pellotine is the inverse agonist for 5-HT7 receptor with an EC₅₀ of 291 nM. Pellotine exhibits good affinity to 5-HT1DR and 5-HT6R with K_i of 117 nM and 170 nM. Pellotine reduces intracellular cAMP levels, thereby reducing neuronal excitability and neurotransmitter release.

SB 258719 hydrochloride is a selective 5-HT₇ receptor antagonist displayed high affnity (pK_i=7.5) for the receptor. SB-258719 hydrochloride can be used for the research of cancer and neurological diseases.

Aramisulpride hydrochloride is a 5-HT₇ receptor antagonist with a K_i value of 22 nM. Aramisulpride hydrochloride is a D₂/D₃ receptor antagonist with a K_i value of 140 nM for D₂R and a K_i value of 13.9 nM for D₃R. Aramisulpride hydrochloride can be used in psychiatric research.

LY215840, a 5-HT₇ receptor ligand and a 5-HT₂ receptor antagonist, blocks serotonin-induced relaxation in canine coronary artery.

AVN-101 is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (K_i of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (K_i values of 2.04 nM, 1.56  nM, and 1.17  nM, respectively). AVN-101 also exhibits a rather high affinity toward histamine H1 (K_i of 0.58 nM) and adrenergic α2A, α2B, and α2C (K_i= 0.41-3.6 nM) receptors. AVN-101 can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis.