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5-HT positive allosteric modulator

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (11) Adrenergic Receptor (1) Calcium Channel (1) Dopamine Receptor (1) Dopamine Transporter (1) GABA Receptor (3) mAChR (1) Reference Standards (1)
By Research Areas:	Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (11)

Targets Recommended: 5-HT Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-103524

Valerenic acid 1 Publications Verification (-)-Valerenic Acid	GABA Receptor 5-HT Receptor	Neurological Disease
Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABA_A receptors. Valerenic acid is also a partial agonist of the 5-HT_5a receptor. Valerenic acid mediates anxiolytic activity via GABA_A receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties .

HY-118301

ADX71441	GABA Receptor 5-HT Receptor	Neurological Disease
ADX71441 is an orally active, blood-brain barrier penetrant positive allosteric modulator of GABA_B receptor. ADX71441 potentiates the activity of endogenous GABA at GABA_B receptor, with an EC₅₀ of 96 nM. ADX71441 functionally inhibits adenosine transporters and *5-HT_2B* receptor. ADX71441 produces anxiolytic-like, analgesic, muscle relaxant, hypothermic and overactive bladder inhibitory effects, reduces acute locomotor activity levels, decreases voluntary intake of alcohol and saccharin, attenuates stress-induced neuronal activation, and exhibits anti-hyperalgesic activity .

HY-124821

VA012	5-HT Receptor	Neurological Disease Metabolic Disease
VA012 (compound 11) is a positive allosteric modulator (PAM) of the serotonin *5-HT_2C* receptor. VA012 reduces food intake and body weight gain without causing CNS-related malaise during subchronic administration. VA012 can be utilized in obesity research .

HY-155672

JPC0323	5-HT Receptor	Neurological Disease
JPC0323 is a dual *5-HT_2C/5-HT_2A* receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .

HY-172982

CTW0419	5-HT Receptor	Neurological Disease
CTW0419 is a potent 5-HT Receptor positive allosteric modulators (PAMs). CTW0419 is promising for research of neuropsychiatric disorders .

HY-172981

CTW0404	5-HT Receptor	Neurological Disease
CTW0404 is a potent 5-HT Receptor positive allosteric modulators (PAMs). CTW0404 is promising for research of neuropsychiatric disorders .

HY-119806

TMPPAA	5-HT Receptor	Neurological Disease
TMPPAA is an allosteric agonist and positive allosteric modulator of the *5-HT3* receptor. TMPPAA enhances *5-HT*-mediated 5-HT3AR signaling .

HY-175532

M4 mAChR Modulator-2	mAChR	Neurological Disease
M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) (EC₅₀ = 513 nM). M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2) while specifically binding to M4 mAChR with a K_i of 377 nM and an inhibition rate of 62.8%. M4 mAChR Modulator-2 reverses Dizocilpine (MK-801) (HY-15084B)-induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia

HY-103524R

Valerenic acid (Standard) (-)-Valerenic Acid (Standard)	5-HT Receptor GABA Receptor Reference Standards	Neurological Disease
Valerenic acid (Standard) is the analytical standard of Valerenic acid. This product is intended for research and analytical applications. Valerenic acid ((-)-Valerenic Acid), a sesquiterpenoid, is an orally active positive allosteric modulator of GABA_A receptors. Valerenic acid is also a partial agonist of the 5-HT_5a receptor. Valerenic acid mediates anxiolytic activity via GABA_A receptors containing the β3 subunit. Valerenic acid also exhibits potent antioxidant properties .

HY-158627

JPC0323 Oleate	5-HT Receptor	Others
JPC0323 Oleate is a derivative of JPC0323 (HY-155672). JPC0323 is a dual *5-HT_2C/5-HT_2A* receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .

HY-180617

5-HT2CR allosteric modulator 1	5-HT Receptor	Neurological Disease Inflammation/Immunology
5-HT2CR modulator 1 (Compound 3B) is a selective, positive ago-allosteric modulator of *5HT_2CR* with an EC₅₀ of 8 nM. 5-HT2CR modulator 1 is also a selective *5HT_2CR* agonist with an EC₅₀ of 25 nM. 5-HT2CR modulator 1 reduces food intake .

HY-182091

CYD-1-79	5-HT Receptor Dopamine Receptor Dopamine Transporter Adrenergic Receptor Calcium Channel	Neurological Disease
CYD-1-79 is a selective positive allosteric modulator of *5-HT2C* receptor. CYD-1-79 potentiates 5-HT-evoked intracellular calcium release via a topographically distinct allosteric site. CYD-1-79 shows significant inhibition of binding at dopamine D3 receptor, DAT, and α2A/α2B adrenergic receptors. CYD-1-79 modulates 5-HT2C receptor-mediated spontaneous ambulation in rodents and synergizes with a low dose of a 5-HT2C receptor agonist. CYD-1-79 attenuates relapse vulnerability of psychoactive substance in a rodent self-administration model. CYD-1-79 can be used for the research of neurological disease .

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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-HT positive allosteric modulator

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