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hyperlocomotion.

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (5) Amino acid Transporter (1) Dopamine Receptor (2) Drug Derivative (2) GPR35 (1) Histamine Receptor (1) iGluR (3) Integrin (1) mAChR (2) mGluR (3) Neurotensin Receptor (1) Phosphodiesterase (PDE) (1) Reference Standards (1) Sigma Receptor (1) Trace Amine-associated Receptor (TAAR) (1)
By Research Areas:	Endocrinology (1) Infection (1) Inflammation/Immunology (2) Metabolic Disease (5) Neurological Disease (23)
Click Chemistry:	Alkynes (1)

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Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-118424

JNJ-55511118	iGluR	Neurological Disease Metabolic Disease
JNJ-55511118 is a selective TARP γ-8 binding AMPA receptor modulator with oral bioavailability and blood-brain barrier permeability, with a K_i of 26 nM. JNJ-55511118 reduces voluntary intake of sweetened alcohol in male mice. In rodent models, JNJ-55511118 inhibits hippocampal neurotransmission, reduces specific electroencephalogram frequency bands, induces transient hyperlocomotion, impairs learning and memory abilities, and exerts anticonvulsant effects. JNJ-55511118 is applicable to research related to alcohol use disorder and seizures .

HY-103151

CP94253 hydrochloride	5-HT Receptor	Neurological Disease Metabolic Disease
CP94253 hydrochloride is an orally active, brain-penetrant and selective 5-HT_1B receptor agonist with an K_i of 2 nM. CP94253 hydrochloride induces antidepressant-like effects, waking enhancement, sleep inhibition, increased sleep latency, hyperlocomotion, and suppressed aggressive behavior. CP94253 hydrochloride can be used for the research of depression and heightened aggressive behavior .

HY-16639

ML314	GPR35 Neurotensin Receptor	Neurological Disease Endocrinology
ML314 is a potent, BBB-penetrant and β-arrestin biased molecule agonist of NTR1 (EC₅₀ = 1.9 μM). ML314 shows good selectivity against NTR2 and GPR35, but does not stimulate Ca2+ mobilization. ML314 can attenuate amphetamine-like hyperlocomotion in dopamine transporter knockout mice. ML314 attenuates methamphetamine-associated hyperlocomotion and potentiates the psychostimulant inhibitory effects of a ghrelin antagonist in wild type mouse model. ML314 also acts as an allosteric enhancer of endogenous neurotensin. ML314 antagonizes G protein signaling. ML314 can be studied in research for methamphetamine abuse conditions .

HY-139178

KVA-D-88	Phosphodiesterase (PDE)	Neurological Disease
KVA-D-88 is a blood-brain barrier-permeable PDE4 inhibitor with IC₅₀ values of 140 and 880 nM for PDE4B and PDE4D, respectively. KVA-D-88 induces cAMP accumulation and inhibits neuroactive substance-mediated hyperlocomotion, locomotor sensitization. KVA-D-88 can be used for the research of drug addiction .

HY-161137

LQFM215	Amino acid Transporter iGluR	Neurological Disease
LQFM215 is a proline transporter (PROT) inhibitor. LQFM215 inhibits proline transport by competitively binding to the active site of PROT. LQFM215 effectively reduces hyperlocomotion and enhances social interaction .

HY-N0927

(-)-Isocorypalmine Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine	Dopamine Receptor	Others Neurological Disease
(-)-Isocorypalmine (Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine) is a dopamine receptor ligand and modulator capable of crossing the blood-brain barrier. (-)-Isocorypalmine exhibits receptor selectivity, acting as a partial agonist of dopamine D1 and D5 receptors (coupled via Gs proteins), as well as an antagonist of D2, D3 and D4 receptors (by blocking Gi protein-mediated signaling). (-)-Isocorypalmine shows no significant binding to various non-dopamine receptors, ion channels and transporters. (-)-Isocorypalmine is metabolically stable in vivo, effectively inhibits spontaneous and cocaine-induced hyperlocomotion, sensitization and conditioned place preference in mice, and does not induce addictive place preference when administered alone. (-)-Isocorypalmine can be used in addiction research .

HY-179008A

(S)-5-HT2CR agonist 1	5-HT Receptor	Neurological Disease
(S)-5-HT2CR agonist 1 (Compound (S)-16k) is selective 5-HT_2CR agonist, with an EC₅₀ of 14 nM. FXa-IN-2 can be used in the research of hyperlocomotion .

HY-179008

5-HT2CR agonist 2	5-HT Receptor	Neurological Disease
5-HT2CR agonist 2 (Compound 16k) is a selective, blood-brain barrier-penetrating and Gq-biased 5-HT_2CR agonist, with an EC₅₀ of 36 nM. 5-HT2CR agonist 2 attenuates MK801 (HY-15084B)-induced hyperlocomotion and reverses Phencyclidine-induced hyperlocomotor activity .

HY-114753

Neboglamine CR-2249; XY-2401	iGluR	Neurological Disease
Neboglamine (CR-2249; XY-2401) is a modulator for N-methyl-D-aspartate (NMDA) receptor. Neboglamine increases the levels of fos-like immunoreactivity (FLI)-positive cells in the prefrontal cortex, nucleus accumbens, and lateral septal nucleus in rat models, .restores NMDA (HY-17551) -mediated neurotransmitter release, and inhibits phencyclidine-induced hyperlocomotion .

HY-123889

VK4-116	Dopamine Receptor	Neurological Disease
VK4-116 (Compound 19) is a selective Dopamine D3 receptor (D3R) antagonist with a K_i of 6.84 nM.VK4-116 significantly inhibits Oxycodone-induced hyperlocomotion and locomotor sensitization in mouse models. VK4-116 with pretreatment also inhibits the acquisition of Oxycodone-induced conditioned place preference (CPP) in rat models .

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-118022

VU0361747	mGluR	Neurological Disease
VU0361747 is a potent and selective positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM). VU0361737 has neuroprotective effect. VU0361737 significantly reverses Amphetamine-induced hyperlocomotion in vivo .

HY-120727

VU0364289	mGluR	Neurological Disease
VU0364289 is a highly selective mGlu5 positive allosteric modulator (PAM) (binds to the MPEP (HY-14609A) site), with an EC₅₀ of 1.6 μM. VU0364289 shows excellent central nervous system penetration. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research .

HY-103151A

CP94253	5-HT Receptor	Neurological Disease Metabolic Disease
CP94253 is an orally active, brain-penetrant and selective 5-HT_1B receptor agonist with an K_i of 2 nM. CP94253 induces antidepressant-like effects, waking enhancement, sleep inhibition, increased sleep latency, hyperlocomotion, and suppressed aggressive behavior. CP94253 can be used for the research of depression and heightened aggressive behavior .

HY-157172

MorHap	Integrin	Infection Neurological Disease
MorHap is a heroin hapten. MorHap conjugated to tetanus toxoid (TT), palm-CV2, and to monophosphoryl lipid A (MPLA)-containing liposomes partially blocks heroin-induced analgesia and hyperlocomotion in mice. MorHap designed conjugates also significantly inhibits HIV-1 binding to α4β7 receptors. MorHap can be used in research to develop vaccines related to heroin addiction and HIV-1 infection .

HY-173032

VU6033685	mGluR	Neurological Disease
VU6033685 is the orally active positive allosteric modulator (PAM) for mGlu1 that positively modulates human mGlu1 and human mGlu5 with EC₅₀ of 39 nM and 3960 nM. VU6033685 also inhibits CYP1A2, CYP2C9 and CYP2D6 with IC₅₀ of 26, 22.3 and 23.8 μM, respectively. VU6033685 reverses amphetamine-induced rats hyperlocomotion, protects rats from MK-801 (HY-15084B)-induced cognitive impairment. VU6033685 exhibits good pharmacokinetics characteristics in rats with an oral bioavailability of 42.8% .

HY-183428

LK00764	Trace Amine-associated Receptor (TAAR)	Neurological Disease
LK00764 is a TAAR1 agonist with an EC₅₀ of 4 nM. LK00764 alleviates Dizocilpine (HY-15084B)-induced hyperlocomotion, reduces vertical locomotor activity, attenuates spontaneous hyperlocomotion in dopamine transporter knockout rats, and inhibits stress-induced hyperthermia in rats. LK00764 can be used for the research of schizophrenia .

HY-W385577

(S)-2-Benzylpyrrolidine	Drug Derivative	Neurological Disease Inflammation/Immunology
(S)-2-Benzylpyrrolidine (Compound s1) serves as a METH hapten scaffold. (S)-2-Benzylpyrrolidine attenuates Methamphetamine-induced hyperlocomotion, hyperthermia and respiratory depression. (S)-2-Benzylpyrrolidine alleviates Fentanyl-induced respiratory depression .

HY-W385577A

(S)-2-Benzylpyrrolidine hydrochloride	Drug Derivative	Neurological Disease Metabolic Disease Inflammation/Immunology
(S)-2-Benzylpyrrolidine hydrochloride (Compound s1) serves as a METH hapten scaffold. (S)-2-Benzylpyrrolidine hydrochloride attenuates Methamphetamine-induced hyperlocomotion, hyperthermia and respiratory depression. (S)-2-Benzylpyrrolidine hydrochloride alleviates Fentanyl-induced respiratory depression .

HY-103151R

CP94253 hydrochloride (Standard)	Reference Standards 5-HT Receptor	Neurological Disease Metabolic Disease
CP94253 hydrochloride (Standard) is the analytical standard of CP94253 hydrochloride (HY-103151). This product is intended for research and analytical applications. CP94253 hydrochloride is an orally active, brain-penetrant and selective 5-HT_1B receptor agonist with an K_i of 2 nM. CP94253 hydrochloride induces antidepressant-like effects, waking enhancement, sleep inhibition, increased sleep latency, hyperlocomotion, and suppressed aggressive behavior. CP94253 hydrochloride can be used for the research of depression and heightened aggressive behavior .

HY-181559S

VU6025733 AG06827	mAChR	Neurological Disease
VU6025733 (AG06827) is a highly selective, orally active and blood-brain barrier-penetrant positive allosteric modulator of the muscarinic acetylcholine receptor subtype M4 (M₄ mAChR). VU6025733 exerts a potentiating effect on acetylcholine-induced receptor activation with an EC₅₀ of 23 nM for hM4 and 55 nM for rM4. VU6025733 shows high selectivity over other muscarinic acetylcholine receptor subtypes, dose-dependently reduces amphetamine-induced hyperlocomotion in rats. VU6025733 is applicable to the research of schizophrenia, Parkinson's disease, and Alzheimer's disease .

HY-181649

S1R agonist 3	Sigma Receptor	Neurological Disease
S1R agonist 3 is a potent, selective and brain-penetrant sigma-1 receptor (S1R) agonist with a K_i of 1.5 nM. S1R agonist 3 reduces hyperlocomotion in wfs1abKO zebrafish larvae without affecting locomotion in wildtype wfs1abWT zebrafish larvae. S1R agonist 3 reverses Aβ_25-35 (HY-P0128)-induced learning and memory impairments. S1R ligand 1 can be used for the research of Alzheimer’s disease .

HY-181960

BP1.3656B	Histamine Receptor	Neurological Disease
BP1.3656B is a selective, orally active, blood-brain barrier-permeable histamine H3 receptor (histamine H3 receptor) inverse agonist/antagonist, with a K_B value of 0.08 nM for antagonizing agonist-induced activity and an IC₅₀ value of 0.38 nM for directly inhibiting the basal activity of the receptor. BP1.3656B reduces alcohol consumption, alcohol-seeking behavior, alcohol self-administration, motivation to drink, alcohol relapse, alcohol-induced hyperlocomotion, and binge alcohol intake. BP1.3656B is applicable for the research of alcohol use disorder .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0927

(-)-Isocorypalmine Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine	Alkaloids Structural Classification Monophenols other families Classification of Application Fields Other Diseases Phenols Plants Isoquinoline Alkaloids Disease Research Fields Source Classification	Dopamine Receptor
(-)-Isocorypalmine (Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine) is a dopamine receptor ligand and modulator capable of crossing the blood-brain barrier. (-)-Isocorypalmine exhibits receptor selectivity, acting as a partial agonist of dopamine D1 and D5 receptors (coupled via Gs proteins), as well as an antagonist of D2, D3 and D4 receptors (by blocking Gi protein-mediated signaling). (-)-Isocorypalmine shows no significant binding to various non-dopamine receptors, ion channels and transporters. (-)-Isocorypalmine is metabolically stable in vivo, effectively inhibits spontaneous and cocaine-induced hyperlocomotion, sensitization and conditioned place preference in mice, and does not induce addictive place preference when administered alone. (-)-Isocorypalmine can be used in addiction research .

Cat. No.	Product Name		Classification

HY-118022

VU0361747		Alkynes
VU0361747 is a potent and selective positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM). VU0361737 has neuroprotective effect. VU0361737 significantly reverses Amphetamine-induced hyperlocomotion in vivo .

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hyperlocomotion.

Inhibitors & Agonists

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Click Chemistry

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