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Results for "

5-HT7 receptor ligand

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (10) Dopamine Receptor (5) Reference Standards (1) Sodium Channel (2)
By Research Areas:	Neurological Disease (9)

Targets Recommended: Target Protein Ligand-Linker Conjugates E3 Ligase Ligand-Linker Conjugates PD-1/PD-L1

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-B1033

Metergoline 2 Publications Verification	5-HT Receptor Dopamine Receptor Sodium Channel	Neurological Disease
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-147810

5-HT7 receptor ligand 1	5-HT Receptor	Neurological Disease
5-HT7 receptor ligand 1 (Compound 5c) is a **5-HT₇ receptor** ligand with a K_i of 8 nM. 5-HT7 receptor ligand 1 is not hepatotoxic and exhibit moderate potential interaction with other agents metabolized by CYP3A4 or CYP2D6 .

HY-159492

5-HT7 receptor ligand 2	5-HT Receptor	Neurological Disease
5-HT7 receptor ligand 2 (compound 32) is an arylpiperazinehydrazine ligand for *5-HT₇R* (K_i=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 .

HY-14545B

SEP-4199	5-HT Receptor Dopamine Receptor	Neurological Disease
SEP4199 is an orally active *5-HT7* receptor ligand, with a K_i 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 .

HY-103119

LP-20 hydrochloride	5-HT Receptor	Others
LP-20 hydrochloride acts as a ligand for the 5-HT7 receptor.

HY-103148

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

HY-B1033R

Metergoline (Standard)	5-HT Receptor Dopamine Receptor Sodium Channel Reference Standards	Neurological Disease
Metergoline (Standard) is the analytical standard of Metergoline. This product is intended for research and analytical applications. Metergoline 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 .

HY-173044

5-HT1AR/5-HT6R ligand-1	5-HT Receptor Dopamine Receptor	Neurological Disease
5-HT1AR/5-HT6R ligand-1 (Compound PP13) is the ligand for 5-HT receptor that exhibits good affinity to 5-HT1AR, 5-HT6R and 5-HT7R (K_i of 19, 69 and 198 nM, respectively), thereby inhibiting the cAMP production in HEK293 cell with EC₅₀ of 1535, 488 and 53 nM, respectively. 5-HT1AR/5-HT6R ligand-1 exhibits anti-proliferative activity against a variety of cancer cells (IC₅₀ for 1321N1, U87MG, MCF7, and AsPC-1 is 9.6, 13.6, 19.3 and 14.6 μM, respectively). 5-HT1AR/5-HT6R ligand-1 also exhibits antagonist activity for dopamine receptor D2R with K_i of 1903 nM .

HY-134483

5-HT7/5-HT2A receptor antagonist 1	5-HT Receptor	Neurological Disease
5-HT7/5-HT2A receptor antagonist 1 is a high-affinity, orally active, brain-penetrant *5-HT7* and 5-HT2A receptor ligand having a pK_i = 8.1 at both receptors. 5-HT7/5-HT2A receptor antagonist 1 behaves as an antagonist in an in vitro functional assay for 5-HT2A and as an inverse agonist in an in vitro functional assay for *5-HT7. 5-HT7/5-HT2A receptor* antagonist 1 blockade of 5-Carboxamidotryptamine (5-CT) (HY-135555) induced hypothermia in rats, and blockade of 2,5-dimethoxy-4-iodoamphetamine (DOI) induced head-twitches in mice. 5-HT7/5-HT2A receptor antagonist 1 occupied 5-HT2A receptor binding sites in the frontal cortex of the rat brain. 5-HT7/5-HT2A receptor antagonist 1 can be used for the study of Neurological diseases .

HY-179725

PZ-1129	5-HT Receptor Dopamine Receptor	Neurological Disease
PZ-1129 is a selective **5-HT7 receptor** ligand with a K_i of 7 nM. PZ-1129 shows K_i 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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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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5-HT7 receptor ligand

Inhibitors & Agonists