5-HT₇ Receptor Antagonist

5-HT₇ Receptor Antagonists (27):

Cat. No.	Product Name	Effect	Purity

HY-15370A

SB-269970 hydrochloride	Antagonist	98.62%
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.

HY-170908

Pellotine	Antagonist
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.

HY-B1033

Metergoline	Antagonist	99.89%
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.

HY-107836

Methiothepin mesylate	Antagonist	99.60%
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).

HY-U00443

SB 258719	Antagonist	99.04%
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.

HY-19889

JNJ-18038683	Antagonist	99.76%
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.

HY-15370

SB-269970	Antagonist	98.48%
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.

HY-134807

Indophagolin	Antagonist	98.05%
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.

HY-126068

(S)-Amisulpride	Antagonist	99.04%
(S)-Amisulpride (Esamisulpride) is a potent dopamine D₂/D₃ receptor antagonist. (S)-Amisulpride is an antagonist at the 5-HT₇ receptor with a K_I of 900 nM. (S)-Amisulpride has antipsychotic and antidepressant effects.

HY-B0032S

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

HY-124135

SB-656104	Antagonist
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.

HY-111491

Methiothepin	Antagonist
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).

HY-103123

SB 258719 hydrochloride	Antagonist
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.

HY-103148

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

HY-117046

AVN-101	Antagonist
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.

HY-163345

5-HT7R antagonist 2	Antagonist
5-HT7R antagonist 2 (compound 4h) is a 5-HT7R antagonist that antagonizes the G protein and β-arrestin signaling pathways, with a K_i of 67 nM, the IC₅₀ values in cAMP and Tango tests were 2.59 μM and 39.57 μM, respectively. 5-HT7R antagonist 2 has an effect on neurogenesis and can reduce repetitive behaviors related to autism spectrum disorder (ASD) and restore neurogenesis of ASD impairment.

HY-163150

5-HT6R antagonist 3	Antagonist
5-HT6R antagonist 3 (compound 15) is a potent, selective and brain-penetrant 5-HT6R antagonist with K_i values of 14 nM, 3533 nM, 35 nM, 1449 nM for 5-HT6, 5-HT1A, 5-HT2A, 5-HT7, respectively. 5-HT6R antagonist 3 shows anxiolytic-like and properties neuroprotective and procognitive-like effects. 5-HT6R antagonist 3 has the potential for the research of Alzheimer’s Disease.

HY-136678A

SB 258741 hydrochloride	Antagonist
SB 258741 hydrochloride is a specific 5-HT₇ receptor antagonist and can be used for the research of schizophrenia.

HY-19889A

JNJ-18038683 free base	Antagonist
JNJ-18038683 free base 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.

HY-103126

DR4485 hydrochloride	Antagonist
DR4485 (hydrochloride) is an orally active and selective 5-HT₇ antagonist (pK_i=8.14).

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