Search Result

Results for "

addiction

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (8) Adenosine Deaminase (2) Adenosine Receptor (1) Adrenergic Receptor (10) AP-1 (1) Apoptosis (5) Arrestin (1) Beta-secretase (1) Cannabinoid Receptor (2) Carboxylesterase (CES) (1) Caspase (1) CDK (1) CRFR (1) Dopamine Receptor (23) Dopamine Transporter (2) Drug Metabolite (1) Endogenous Metabolite (2) ERK (3) G Protein-coupled Receptor Kinase (GRK) (1) GABA Receptor (5) GPR6 (1) Histamine Receptor (1) HIV Integrase (1) iGluR (5) Imidazoline Receptor (4) Integrin (1) Interleukin Related (1) Isotope-Labeled Compounds (5) mGluR (9) Mitochondrial Metabolism (1) Monoamine Transporter (3) mTOR (3) nAChR (9) Neuropeptide S Receptor (1) Neuropeptide Y Receptor (2) Neurotensin Receptor (1) NF-κB (1) NO Synthase (1) Opioid Receptor (13) Orexin Receptor (OX Receptor) (4) Parasite (1) PARP (1) Phosphodiesterase (PDE) (1) PKC (2) Potassium Channel (2) PPAR (1) PROTACs (1) Pyruvate Kinase (1) Reference Standards (8) RGS Protein (1) Serotonin Transporter (3) Sigma Receptor (4) Sodium Channel (1) Target Protein Ligand-Linker Conjugates (1) TNF Receptor (1) Toll-like Receptor (TLR) (1) Trace Amine-associated Receptor (TAAR) (1)
By Research Areas:	Cancer (11) Cardiovascular Disease (4) Infection (2) Inflammation/Immunology (4) Metabolic Disease (13) Neurological Disease (107)

By Targets:

5-HT Receptor (8)

Adenosine Deaminase (2)

Adenosine Receptor (1)

Adrenergic Receptor (10)

AP-1 (1)

Apoptosis (5)

Arrestin (1)

Beta-secretase (1)

Cannabinoid Receptor (2)

Carboxylesterase (CES) (1)

Caspase (1)

CDK (1)

CRFR (1)

Dopamine Receptor (23)

Dopamine Transporter (2)

Drug Metabolite (1)

Endogenous Metabolite (2)

ERK (3)

G Protein-coupled Receptor Kinase (GRK) (1)

GABA Receptor (5)

GPR6 (1)

Histamine Receptor (1)

HIV Integrase (1)

iGluR (5)

Imidazoline Receptor (4)

Integrin (1)

Interleukin Related (1)

Isotope-Labeled Compounds (5)

mGluR (9)

Mitochondrial Metabolism (1)

Monoamine Transporter (3)

mTOR (3)

nAChR (9)

Neuropeptide S Receptor (1)

Neuropeptide Y Receptor (2)

Neurotensin Receptor (1)

NF-κB (1)

NO Synthase (1)

Opioid Receptor (13)

Orexin Receptor (OX Receptor) (4)

Parasite (1)

PARP (1)

Phosphodiesterase (PDE) (1)

PKC (2)

Potassium Channel (2)

PPAR (1)

PROTACs (1)

Pyruvate Kinase (1)

Reference Standards (8)

RGS Protein (1)

Serotonin Transporter (3)

Sigma Receptor (4)

Sodium Channel (1)

Target Protein Ligand-Linker Conjugates (1)

TNF Receptor (1)

Toll-like Receptor (TLR) (1)

Trace Amine-associated Receptor (TAAR) (1)

By Research Areas:

Cancer (11)

Cardiovascular Disease (4)

Infection (2)

Inflammation/Immunology (4)

Metabolic Disease (13)

Neurological Disease (107)

120

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-17030

Acamprosate calcium Calcium N-acetylhomotaurinate	GABA Receptor iGluR	Neurological Disease
Acamprosate calcium(Campral EC) is a GABA receptor agonist and modulator of glutamatergic systems; reduces alcohol consumption in animal models of alcohol addiction.

HY-114237

GDC-0276	Sodium Channel	Neurological Disease
GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC₅₀ value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects .

HY-P1335

CTAP 2 Publications Verification	Opioid Receptor	Neurological Disease
CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC₅₀ of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC₅₀=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .

HY-B1110

Nomifensine Maximum Cited Publications 6 Publications Verification (±)-Nomifensine; Nomifensin	Dopamine Receptor Adrenergic Receptor	Neurological Disease
Nomifensine ((±)-Nomifensine) is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC₅₀ values of 6.6 nM, 48 nM and 830 nM, and K_i values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine has antidepressant and analgesic effects. Nomifensine is used in neurodegenerative diseases, compound addiction, and pain research .

HY-B1110A

Nomifensine maleate Maximum Cited Publications 6 Publications Verification (±)-Nomifensine maleate; Nomifensin maleate	Dopamine Receptor Adrenergic Receptor	Neurological Disease
Nomifensine ((±)-Nomifensine) maleate is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine maleate inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC₅₀ values of 6.6 nM, 48 nM and 830 nM, and K_i values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine maleate has antidepressant and analgesic effects. Nomifensine maleate is used in neurodegenerative diseases, compound addiction, and pain research .

HY-N6960

L-Stepholidine Stepholidine; (-)-Stepholidine; L-SPD	Dopamine Receptor	Neurological Disease
L-Stepholidine (Stepholidine) is an alkaloid. L-Stepholidine exhibits mixed dopamine D1 receptor agonist and D2 antagonist properties. L-Stepholidine has neuroprotective effect. L-Stepholidine can be used for the researches of neurological disease, such as Parkinson disease, Alzheimer's disease and opiate addiction .

HY-135608

BD-1008	Sigma Receptor	Neurological Disease
BD-1008 is a nonselective σ receptor antagonist with K_is against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 has an extremely low affinity for the D2 receptor (K_i = 1112 nM) and dopamine transporter (DAT) (K_i > 10,000 nM). BD-1008 significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 blocks the self-administration behavior of σ agonists.BD-1008 can be used for the study of addiction therapy that target the σ receptor .

HY-B1052

Lofexidine hydrochloride Baq-168; MDL-14042	Adrenergic Receptor Imidazoline Receptor	Neurological Disease Metabolic Disease
Lofexidine hydrochloride (Baq-168) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α₂-adrenergic receptor (α2-adrenergic receptor). Lofexidine hydrochloride binds to the α₂A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine hydrochloride regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine hydrochloride is applicable to research on opioid addiction and withdrawal .

HY-108626

ML154 NCGC84	Neuropeptide S Receptor	Neurological Disease
ML154 (NCGC84) is a selective, brain-penetrant and non-peptide neuropeptide S receptor (NPSR) antagonist with a pA₂ of 9.98. ML154 potently inhibits NPS-stimulated cellular calcium, cAMP, and ERK phosphorylation responses with IC₅₀ values of 36.5 nM, 22.1 nM, and 9.3 nM, respectively .

HY-12844

Ro 64-6198 1 Publications Verification	Opioid Receptor	Neurological Disease
Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC₅₀ value of 25.6 nM. Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors. Ro 64-6198 can be used for stress and anxiety, addiction, neuropathic pain, cough, and anorexia .

HY-111308

RTI-118	Neuropeptide Y Receptor	Neurological Disease
RTI-118 is a novel small-molecule neuropeptide S receptor (NPSR) antagonist. RTI-118 can relieve agent addiction including selectively decrease self-administration .

HY-116649

CB1 antagonist 2 AM4113	Cannabinoid Receptor	Neurological Disease Metabolic Disease
CB1 antagonist 2 (AM4113) is an orally active cannabinoid receptor type 1 (CB1R) antagonist. CB1 antagonist 2 suppresses appetite, reduces body weight, and blocks addictive behaviors such as heroin addiction, without causing adverse effects like nausea and depression that are associated with traditional CB1 inverse agonists. CB1 antagonist 2 can be used in studies related to obesity and opioid addiction .

HY-101478

Fenobam	mGluR Apoptosis	Neurological Disease Cancer
Fenobam is a selective and orally active mGluR5 antagonist (IC₅₀=84 nM) that can penetrate the blood-brain barrier. Fenobam shows the K_d values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam has anxiolytic activity, inhibits self-administration behavior in mice, and induces apoptosis in cancer cells. Fenobam can be used for research on neurological diseases, cancer and drug addiction .

HY-112705

VU0529331	Potassium Channel	Neurological Disease Metabolic Disease
VU0529331 is a homomeric GIRK channel activator, with an EC₅₀ value of 5.1 μM for human GIRK2 and an EC₅₀ value of 22.3 μM for GIRK4. VU0529331 serves as a starting point for the development of non-GIRK1/X channel probes and also acts as a tool for studying homomeric GIRK channels. VU0529331 is applicable to research related to addiction, primary aldosteronism and delayed-onset obesity .

HY-103673

AMPD2 inhibitor 1	Adenosine Deaminase	Neurological Disease
AMPD2 inhibitor 1 is an adenosine monophosphate deaminase 2 (AMPD2) inhibitor, used in the research of sugar craving, salt craving, umami craving, and addictions including agent, tobacco, nicotine and alcohol addictions.

HY-135783

AT 1001 1 Publications Verification	nAChR	Neurological Disease Metabolic Disease Inflammation/Immunology
AT 1001 is an orally effective α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) antagonist with a K_i value of 2.64 nM. AT 1001 reversibly blocks Epibatidine (HY-101078)-induced inward currents in HEK cells transfected with α3β4 nAChR. AT 1001 dose-dependently blocks nicotine self-administration behavior in rats, alleviates gluten-induced gastrointestinal symptoms, blocks tight junction toxin-induced immune responses, and reduces the incidence of type 1 diabetes in rats. AT 1001 can be used in the research of nicotine addiction and celiac disease .

HY-W206168

Tetrahydropapaveroline hydrobromide Norlaudanosoline hydrobromide	Dopamine Receptor	Neurological Disease
Tetrahydropapaveroline (Norlaudanosoline) hydrobromide, an isoquinoline alkaloid, is a condensation product of dopamine and dopaldehyde. Tetrahydropapaveroline hydrobromide inhibits [ ³H]DA uptake with a K_i of 41 μM. Tetrahydropapaveroline hydrobromide can be used for the study of Parkinson's disease and/or alcohol addiction .

HY-107457

AZD-8529 1 Publications Verification	mGluR	Neurological Disease
AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC₅₀ of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.

HY-147428

Zolunicant MM-110; (±)-18-Methoxycoronaridine	nAChR Parasite	Infection Neurological Disease
Zolunicant (MM-110) is a potent inhibitor against nicotinic α3β4 receptors with an IC₅₀ of 0.90 μM to combat addiction. Zolunicant can decrease the self-administration of several addictive agents including morphine, methamphetamine, nicotine, and ethanol in rat model. Zolunicant can be studied as a potential research for multiple forms of agent abuse . Zolunicant also reveals a potent leishmanicide effect against Leishmania amazonensis .

HY-P2259

TAT-GluA2 3Y 2 Publications Verification	iGluR HIV Integrase Adenosine Receptor	Cardiovascular Disease Neurological Disease
TAT-GluA2 3Y is a blood-brain barrier-permeable AMPA receptor inhibitory peptide that crosses cell membranes via the HIV-1 TAT protein domain. TAT-GluA2 3Y blocks the endocytosis of AMPA receptors, including the internalization of GluA1/GluA2 subunits, by disrupting interactions with the AP2, Brag2 and Syt3-GluA2 complexes, while also inhibiting long-term depression. TAT-GluA2 3Y blocks hypoxia-mediated AMPAR internalization, alleviates A1R-induced persistent synaptic inhibition, and reduces cerebral ischemic volume, neurological deficits and spatial memory deficits. TAT-GluA2 3Y blocks the effect of NLRP3 deficiency on fear generalization, inhibits amphetamine-induced behavioral/neurochemical sensitization, weakens the unconditioned stimulus-conditioned stimulus association of morphine, and promotes the extinction of morphine CPP. TAT-GluA2 3Y can be used in studies related to fear generalization, ischemic stroke, hypoxia, drug addiction and opioid addiction .

HY-123538

GRK2 Inhibitor 1	Dopamine Receptor G Protein-coupled Receptor Kinase (GRK)	Cardiovascular Disease
GRK2 Inhibitor 1 (methyl 5-[2-(5-nitro-2-furyl)vinyl]-2-furoate) is a dual GRK2/β-ARK1 inhibitor that induces dopamine (DA) inhibition reversal (DIR). GRK2 Inhibitor 1 can also block serotonin-induced or neurotensin-induced DIR reversal. Note: DIR refers to the phenomenon in which neurons in addiction-related brain pathways become less sensitive to DA inhibition when exposed to moderate concentrations of DA for a long time .

HY-103475

GS39783	GABA Receptor	Neurological Disease
GS39783 is a positive allosteric modulator (PAM) of GABA_BR. Positive modulation of the GABA_BR can be used for the research of Nicotine addiction .

HY-101834

ACT-462206	Orexin Receptor (OX Receptor)	Others
ACT-462206 is an orally active and potent dual Orexin 1/Orexin 2 receptor antagonist with IC₅₀s of 60 nM (Orexin 1) and 11 nM (Orexin 2), respectively. ACT-462206 exhibits brain penetration properties, and can be used for insomnia, stress/anxiety-related disorders and addiction research .

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-147319

RTI-7470-44	Trace Amine-associated Receptor (TAAR)	Neurological Disease
RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with an IC₅₀ value of 8.4 nM and a K_i value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, agent addiction, and Parkinson’s disease (PD) .

HY-B1052A

Lofexidine Baq-168 free base; MDL-14042 free base	Imidazoline Receptor Adrenergic Receptor	Neurological Disease Metabolic Disease
Lofexidine (Baq-168 free base) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α₂-adrenergic receptor (α2-adrenergic receptor). Lofexidine binds to the α₂A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine is applicable to research on opioid addiction and withdrawal .

HY-103417

SKF 77434 hydrobromide	Dopamine Receptor	Neurological Disease
SKF 77434 hydrobromide is a selective dopamine D1 receptor partial agonist. SKF 77434 hydrobromide has the potential to study cocaine addiction .

HY-P1437

Neuropeptide S (mouse)	Neuropeptide Y Receptor	Neurological Disease
Neuropeptide S (mouse) is a bioactive peptide. Neuropeptide S (mouse), as a neurotransmitter/neuromodulator of 20 amino acids, can be used for the research of arousal, anxiety, locomotion, feeding behaviors, memory and agent addiction .

HY-12697

NGB 2904	Dopamine Receptor	Neurological Disease
NGB 2904 is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a K_i of 1.4 nM. NGB 2904 shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (K_is=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 antagonizes Quinpirole-stimulated mitogenesis .

HY-P1335A

CTAP TFA 2 Publications Verification	Opioid Receptor	Neurological Disease
CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC₅₀ of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC₅₀=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .

HY-N7506

13-Hydroxyisobakuchiol Delta3,2-Hydroxylbakuchiol	Monoamine Transporter Dopamine Transporter	Neurological Disease
13-Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol), an analog of Bakuchiol (HY-N0235) that can be isolated from Psoralea corylifolia (L.), is a potent selective monoamine transporter inhibitor. 13-Hydroxyisobakuchiol is more selective for the dopamine transporter (DAT) (IC₅₀ = 0.58 μM) and norepinephrine transporter (NET) (IC₅₀ = 0.69 μM) than for the serotonin transporter (SERT) (IC₅₀ = 312.02 μM). 13-Hydroxyisobakuchiol increases the activity of intact mice and improves the decreased activity of reserpinized mice in vivo. 13-Hydroxyisobakuchiol can be used for the research of disorders such as Parkinson's disease and depression .

HY-116910

CPP-115	GABA Receptor	Neurological Disease
CPP-115 is a GABA transaminase inactivator with higher affinity and lower retinal toxicity than Vigabatrin (HY-15399). CPP-115 increases brain GABA levels by inhibiting GABA transaminase catabolism. CPP-115 can be used in the study of drug addiction and infantile spasms .

HY-116181

YQA14	Dopamine Receptor	Neurological Disease
YQA14 is a high affinity dopamine D3 receptor antagonist. YQA14 is anti-opioid addiction agent. YQA14 inhibits Morphine/Cocaine-induced conditioned place preference (CPP) in animals .

HY-107457A

AZD-8529 mesylate 1 Publications Verification	mGluR	Neurological Disease
AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC₅₀ of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes .

HY-155850

CIAC001	Pyruvate Kinase	Neurological Disease
CIAC001 is a Pyruvate Kinase PKM2 inhibitor with anti-neuroinflammatory activity. CIAC001 inhibits LPS-induced proinflammatory nitric oxide (NO) production and protects immunologically active BV-2 cells (IC₅₀=2.5 μM). CIAC001 also has anti-neuroinflammation in mouse models and inhibits chronic morphine-induced addiction .

HY-P3646

[DAla2] Dynorphin A (1-9) (porcine)	Opioid Receptor	Neurological Disease
[DAla2] Dynorphin A (1-9) (porcine) is a dynorphin, which can be used in studies of analgesic, addiction, and depression.

HY-171746

F4-Trp 4,5,6,7-Tetrafluoro-L-tryptophan	nAChR	Neurological Disease
F4-Trp (4,5,6,7-Tetrafluoro-L-tryptophan) is a ligand targeting the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR). F4-Trp is promising for research of neurotransmission, addiction, and related diseases, such as neurological diseases .

HY-P10405A

TAT-D1 peptide acetate	Dopamine Receptor	Neurological Disease
TAT-D1 peptide acetate is a dopamine D1-D2 receptor heterodimer inhibitor. TAT-D1 peptide acetate disrupts the function of dopamine D1-D2 receptor heteromers, enhances subchronic amphetamine-induced locomotor activity, and exacerbates the expression of amphetamine-induced locomotor sensitization. TAT-D1 peptide acetate produces rapid anxiolytic and antidepressant-like effects in rat models of depression and anxiety, and inhibits c-fos expression in the nucleus accumbens of rats. TAT-D1 peptide acetate can be used in the research of psychostimulant addiction, depression and anxiety disorders .

HY-124110

TC299423	nAChR	Neurological Disease
TC299423 is an orally active, brain-penetrant, selective and potent agonist for α6β2 ^? and α4β2 ^? nicotinic acetylcholine receptors (nAChRs) with anxiolytic and antinociceptive properties. TC299423 acts primarily through α6β2 ^? nAChRs that are implicated in the anxiolytic effects of nicotine. TC299423 elicits reward-related behavior mediated through α6β2 ^? nAChRs in hypersensitive α6L90’S mice. TC299423 elicits dopamine release and dose not suppress nicotine self-administration in rats. TC299423 is proming for rasearch of addiction and Parkinson’s disease .

HY-137231B

(S)-UFR2709 hydrochloride	nAChR	Neurological Disease
(S)-UFR2709 (hydrochloride) is a competitive nAChR antagonist?and displays higher affinity for α₄β₂ nAChRs than for α₇ nAChRs. (S)-UFR2709 (hydrochloride) decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 (hydrochloride) acts as an anxiolytic agent and can be used for the study of nicotine addiction .

HY-117883

GZ-793A	Monoamine Transporter	Neurological Disease
GZ-793A is an orally active and selective vesicular monoamine transporter-2 (VMAT2) inhibitor, with an K_i of 0.029 µM. GZ-793A inhibits the neurochemical effects of methamphetamine (METH)-induced dopamine release. GZ-793A can be used for research of METH addiction .

HY-P2046

β-Endorphin (rat)	Opioid Receptor	Neurological Disease
β-Endorphin (rat) is an endogenous opioid neuropeptide and peptide hormone. β-Endorphin (rat) has analgesic activity and also contributes to food intake in satiated rats. β-Endorphin (rat) can be used in the research of neurological diseases such as analgesia and drug addiction .

HY-153458

Orexin receptor modulator-1	Orexin Receptor (OX Receptor)	Cardiovascular Disease Neurological Disease Metabolic Disease
Orexin receptor modulator-1 is an orexin receptor modulator. Orexin receptor modulator-1 can be used for the research of substance addiction, panic disorder, anxiety, post-traumatic stress disorder, pain, depression, seasonal affective disorder, an eating disorder, or hypertension .

HY-100966

BD-1008 dihydrobromide	Sigma Receptor	Neurological Disease
BD-1008 dihydrobromide is a nonselective σ receptor antagonist with K_is against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 dihydrobromide has an extremely low affinity for the D2 receptor (K_i = 1112 nM) and dopamine transporter (DAT) (K_i > 10,000 nM). BD-1008 dihydrobromide significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 dihydrobromide blocks the self-administration behavior of σ agonists.BD-1008 dihydrobromide can be used for the study of addiction therapy that target the σ receptor .

HY-14555

S 33138	Dopamine Receptor	Neurological Disease
S33138 is a D3 receptor antagonist. S33138 inhibits addiction in animal models of addiction. S33138 reduces cognitive impairment in rodent and primate models of schizophrenia and Parkinson's disease. S33138 can be used in research on neurological disorders such as schizophrenia and Parkinson's disease .

HY-P10405

TAT-D1 peptide	Dopamine Receptor	Neurological Disease
TAT-D1 peptide is a dopamine D1-D2 receptor heterodimer inhibitor. TAT-D1 peptide disrupts the function of dopamine D1-D2 receptor heteromers, enhances subchronic amphetamine-induced locomotor activity, and exacerbates the expression of amphetamine-induced locomotor sensitization. TAT-D1 peptide produces rapid anxiolytic and antidepressant-like effects in rat models of depression and anxiety, and inhibits c-fos expression in the nucleus accumbens of rats. TAT-D1 peptide can be used in the research of psychostimulant addiction, depression and anxiety disorders .

HY-106660

BP 897 hydrochloride	Dopamine Receptor	Neurological Disease
BP 897 hydrochloride is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 hydrochloride displays a high affinity at the dopamine D3 receptor (K_i=0.92 nM) and a 70 times lower affinity at the D2 receptor (K_i=61 nM) .

HY-158014

JJC8-089	Dopamine Transporter	Neurological Disease
JJC8-089 is a dopamine transporter (DAT) inhibitor that may improve motivational dysfunction and increase effortful behavior in goal-directed activities. JJC8-089 significantly reversed the low-effort effects induced by the VMAT-2 inhibitor Tetrabenazine (HY-B0590) in rats and increased the choice of high-effort fixed-ratio 5-bar presses versus food intake. .

HY-175285

5-HT2AR-IN-1	5-HT Receptor	Neurological Disease
5-HT_2AR-IN-1 (Compound Ie) is an orally active 5-hydroxytryptamine 2A receptor (5-HT_2AR) inhibitor with antidepressant efficacy. 5-HT_2AR-IN-1 reduces 5-HT_2AR expression and SERT protein levels. 5-HT_2AR-IN-1 is promising for research of central nervous system (CNS), such as depression and addiction-related disorders .

HY-14565

Pozanicline ABT-089	nAChR	Neurological Disease
Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (K_i=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (K_i, rat) for Pozanicline to [ ³H] cytisine sites is 16.7 nM. Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction .

Cat. No.	Product Name

HY-L083

Anti-Cancer Metabolism Compound Library

3,552 compounds

Mutations in oncogenes and tumor suppressor genes can modify multiple signaling pathways and in turn cell metabolism, which facilitates tumorigenesis. The paramount hallmark of tumor metabolism is “aerobic glycolysis” or the Warburg effect, coined by Otto Warburg in 1926, in which cancer cells produce most of energy from glycolysis pathway regardless of whether in aerobic or anaerobic condition. Usually, cancer cells are highly glycolytic (glucose addiction) and take up more glucose than do normal cells from outside. The increased uptake of glucose is facilitated by the overexpression of several isoforms of membrane glucose transporters (GLUTs). Likewise, the metabolic pathways of glutamine, amino acid and fat metabolism are also altered. Recent trends in anti-cancer drug discovery suggests that targeting the altered metabolic pathways of cancer cells result in energy crisis inside the cancer cells and can selectively inhibit cancer cell proliferation by delaying or suppressing tumor growth.

MCE provides a unique collection of 3,552 compounds which cover various tumor metabolism-related signaling pathways. These compounds can be used for anti-cancer metabolism targets identification, validation as well anti-cancer drug discovery.

Cat. No.	Product Name	Target	Research Area

HY-P1335

CTAP 2 Publications Verification	Opioid Receptor	Neurological Disease
CTAP is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC₅₀ of 3.5 nM. CTAP displays over 1200-fold selectivity over δ opioid (IC₅₀=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .

HY-P2259

TAT-GluA2 3Y 2 Publications Verification	iGluR HIV Integrase Adenosine Receptor	Cardiovascular Disease Neurological Disease
TAT-GluA2 3Y is a blood-brain barrier-permeable AMPA receptor inhibitory peptide that crosses cell membranes via the HIV-1 TAT protein domain. TAT-GluA2 3Y blocks the endocytosis of AMPA receptors, including the internalization of GluA1/GluA2 subunits, by disrupting interactions with the AP2, Brag2 and Syt3-GluA2 complexes, while also inhibiting long-term depression. TAT-GluA2 3Y blocks hypoxia-mediated AMPAR internalization, alleviates A1R-induced persistent synaptic inhibition, and reduces cerebral ischemic volume, neurological deficits and spatial memory deficits. TAT-GluA2 3Y blocks the effect of NLRP3 deficiency on fear generalization, inhibits amphetamine-induced behavioral/neurochemical sensitization, weakens the unconditioned stimulus-conditioned stimulus association of morphine, and promotes the extinction of morphine CPP. TAT-GluA2 3Y can be used in studies related to fear generalization, ischemic stroke, hypoxia, drug addiction and opioid addiction .

HY-P1437

Neuropeptide S (mouse)	Neuropeptide Y Receptor	Neurological Disease
Neuropeptide S (mouse) is a bioactive peptide. Neuropeptide S (mouse), as a neurotransmitter/neuromodulator of 20 amino acids, can be used for the research of arousal, anxiety, locomotion, feeding behaviors, memory and agent addiction .

HY-P1335A

CTAP TFA 2 Publications Verification	Opioid Receptor	Neurological Disease
CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC₅₀ of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC₅₀=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction .

HY-P3646

[DAla2] Dynorphin A (1-9) (porcine)	Opioid Receptor	Neurological Disease
[DAla2] Dynorphin A (1-9) (porcine) is a dynorphin, which can be used in studies of analgesic, addiction, and depression.

HY-171746

F4-Trp 4,5,6,7-Tetrafluoro-L-tryptophan	nAChR	Neurological Disease
F4-Trp (4,5,6,7-Tetrafluoro-L-tryptophan) is a ligand targeting the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR). F4-Trp is promising for research of neurotransmission, addiction, and related diseases, such as neurological diseases .

HY-P10405A

TAT-D1 peptide acetate	Dopamine Receptor	Neurological Disease
TAT-D1 peptide acetate is a dopamine D1-D2 receptor heterodimer inhibitor. TAT-D1 peptide acetate disrupts the function of dopamine D1-D2 receptor heteromers, enhances subchronic amphetamine-induced locomotor activity, and exacerbates the expression of amphetamine-induced locomotor sensitization. TAT-D1 peptide acetate produces rapid anxiolytic and antidepressant-like effects in rat models of depression and anxiety, and inhibits c-fos expression in the nucleus accumbens of rats. TAT-D1 peptide acetate can be used in the research of psychostimulant addiction, depression and anxiety disorders .

HY-P2046

β-Endorphin (rat)	Opioid Receptor	Neurological Disease
β-Endorphin (rat) is an endogenous opioid neuropeptide and peptide hormone. β-Endorphin (rat) has analgesic activity and also contributes to food intake in satiated rats. β-Endorphin (rat) can be used in the research of neurological diseases such as analgesia and drug addiction .

HY-P10405

TAT-D1 peptide	Dopamine Receptor	Neurological Disease
TAT-D1 peptide is a dopamine D1-D2 receptor heterodimer inhibitor. TAT-D1 peptide disrupts the function of dopamine D1-D2 receptor heteromers, enhances subchronic amphetamine-induced locomotor activity, and exacerbates the expression of amphetamine-induced locomotor sensitization. TAT-D1 peptide produces rapid anxiolytic and antidepressant-like effects in rat models of depression and anxiety, and inhibits c-fos expression in the nucleus accumbens of rats. TAT-D1 peptide can be used in the research of psychostimulant addiction, depression and anxiety disorders .

HY-P3625

Dynorphin (2-17), amide (porcine)	Endogenous Metabolite Opioid Receptor	Neurological Disease
Dynorphin (2-17), amide (porcine) is a dynorphin derivative with some analgesic effects. Dynorphin is a class of opioid peptides produced by the precursor protein dynorphinogen and is involved in pain, addiction and mood regulation .

HY-P2298

TAT-P4-(DATC5)2	PKC	Neurological Disease
TAT-P4-(DATC5)2 is a high-affinity peptide inhibitor of the PICK1 (protein interacting with C kinase-1) PDZ domain, with a K_i of 1.7 nM. TAT-P4-(DATC5)2 can inhibit addiction in rats .

HY-P2298A

TAT-P4-(DATC5)2 TFA	PKC	Neurological Disease
TAT-P4-(DATC5)2 TFA is a high-affinity peptide inhibitor of the PICK1 (protein interacting with C kinase-1) PDZ domain, with a K_i of 1.7 nM. TAT-P4-(DATC5)2 TFA can inhibit addiction in rats .

HY-P1625

Daeatal Dynorphin A ethylamide (1-9)	Opioid Receptor	Neurological Disease
Daeatal (Dynorphin A ethylamide (1-9)) is an ethylamine-modified dynorphin fragment that can be used in the study of analgesia, addiction, depression, etc. Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N6960

L-Stepholidine Stepholidine; (-)-Stepholidine; L-SPD	Alkaloids Stephania intermedia Plants Isoquinoline Alkaloids Menispermaceae Source Classification	Dopamine Receptor
L-Stepholidine (Stepholidine) is an alkaloid. L-Stepholidine exhibits mixed dopamine D1 receptor agonist and D2 antagonist properties. L-Stepholidine has neuroprotective effect. L-Stepholidine can be used for the researches of neurological disease, such as Parkinson disease, Alzheimer's disease and opiate addiction .

HY-N7506

13-Hydroxyisobakuchiol Delta3,2-Hydroxylbakuchiol	Structural Classification Monophenols Leguminosae Phenols Psoralea corylifolia L. Plants Source Classification	Monoamine Transporter Dopamine Transporter
13-Hydroxyisobakuchiol (Delta3,2-Hydroxylbakuchiol), an analog of Bakuchiol (HY-N0235) that can be isolated from Psoralea corylifolia (L.), is a potent selective monoamine transporter inhibitor. 13-Hydroxyisobakuchiol is more selective for the dopamine transporter (DAT) (IC₅₀ = 0.58 μM) and norepinephrine transporter (NET) (IC₅₀ = 0.69 μM) than for the serotonin transporter (SERT) (IC₅₀ = 312.02 μM). 13-Hydroxyisobakuchiol increases the activity of intact mice and improves the decreased activity of reserpinized mice in vivo. 13-Hydroxyisobakuchiol can be used for the research of disorders such as Parkinson's disease and depression .

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	Chemical Structure

HY-B1052S

Lofexidine-d4 hydrochloride

Lofexidine-d₄ hydrochloride (Baq-168-d₄) is the deuterium labeled Lofexidine hydrochloride (HY-B1052). Lofexidine hydrochloride (Baq-168) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α₂-adrenergic receptor (α2-adrenergic receptor). Lofexidine hydrochloride binds to the α₂A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine hydrochloride regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine hydrochloride is applicable to research on opioid addiction and withdrawal .

HY-10019AS1

Varenicline-d4 hydrochloride

Varenicline-d₄ hydrochloride is a deuterium labeled Varenicline (dihydrochloride) (HY-10019A) . Varenicline (CP 526555) dihydrochloride is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC₅₀ value of 2.3 μM. Varenicline dihydrochloride is a full agonist for α3β4 and α7 nAChRs with EC₅₀ values of 55 μM and 18 μM, respectively . Varenicline dihydrochloride is a nicotinic ligand based on the structure of cytosine, and has the potential for smoking cessation treatment .

HY-B1110S

Nomifensine-d3 maleate

Nomifensine-d₃ ((±)-Nomifensine-d₃) maleate is the deuterium labeled Nomifensine maleate (HY-B1110A). Nomifensine ((±)-Nomifensine) maleate is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine maleate inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC₅₀ values of 6.6 nM, 48 nM and 830 nM, and K_i values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine maleate has antidepressant and analgesic effects. Nomifensine maleate is used in neurodegenerative diseases, compound addiction, and pain research .

HY-B1052S1

Lofexidine-d4

Lofexidine-d₄ (Baq-168 free base-d₄) is deuterium labeled Lofexidine (HY-B1052A). Lofexidine (Baq-168 free base) is an orally active agonist of the imidazoline I1 receptor (imidazoline I1 receptor) (Ki: 1.9 nM) and α₂-adrenergic receptor (α2-adrenergic receptor). Lofexidine binds to the α₂A-adrenergic receptor, reduces sympathetic outflow, lowers blood pressure, and exhibits vasoconstrictive effects. Lofexidine regulates the expression of c-fos and alleviates opioid withdrawal symptoms. Lofexidine is applicable to research on opioid addiction and withdrawal .

HY-100966S

BD-1008-d5 dihydrobromide

BD-1008-d₅ dihydrobromide is the deuterium labeled BD-1008 dihydrobromide (HY-100966). BD-1008 dihydrobromide is a nonselective σ receptor antagonist with K_is against σ1 receptor and σ2 receptor of 2 nM and 8 nM. The BD-1008 dihydrobromide has an extremely low affinity for the D2 receptor (K_i = 1112 nM) and dopamine transporter (DAT) (K_i > 10,000 nM). BD-1008 dihydrobromide significantly antagonizes dopamine release in the shell region of the nucleus accumbens via the σ₂ receptor. BD-1008 dihydrobromide blocks the self-administration behavior of σ agonists.BD-1008 dihydrobromide can be used for the study of addiction therapy that target the σ receptor .

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