Search Result

Results for "

withdrawal

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (5) Adenosine Receptor (1) Adrenergic Receptor (13) Akt (2) Apoptosis (3) Arrestin (2) Calcium Channel (6) Cholinesterase (ChE) (1) Complement System (1) CRFR (3) Cyclic GMP-AMP Synthase (2) Dopamine Receptor (3) Dopamine Transporter (4) Drug Derivative (2) Endogenous Metabolite (1) Epigenetic Reader Domain (1) ERK (5) Estrogen Receptor/ERR (3) Fat Mass and Obesity-associated Protein (FTO) (1) FOXO (1) GABA Receptor (10) Gap Junction Protein (1) Histone Demethylase (1) iGluR (4) Imidazoline Receptor (4) Interleukin Related (2) Isotope-Labeled Compounds (10) mAChR (3) Melatonin Receptor (4) mGluR (1) mTOR (2) nAChR (2) NADPH Oxidase (1) Neurokinin Receptor (1) Neuropeptide FF Receptor (1) Neuropeptide Y Receptor (1) Neurotensin Receptor (2) Opioid Receptor (19) PKA (2) Reference Standards (12) Ribosomal S6 Kinase (RSK) (1) SARS-CoV (1) Sodium Channel (3) Trk Receptor (1) Tyrosine Hydroxylase (1) Virus Protease (1)
By Research Areas:	Cancer (10) Cardiovascular Disease (8) Endocrinology (10) Infection (1) Inflammation/Immunology (5) Metabolic Disease (10) Neurological Disease (72)

By Targets:

5-HT Receptor (5)

Adenosine Receptor (1)

Adrenergic Receptor (13)

Akt (2)

Apoptosis (3)

Arrestin (2)

Calcium Channel (6)

Cholinesterase (ChE) (1)

Complement System (1)

CRFR (3)

Cyclic GMP-AMP Synthase (2)

Dopamine Receptor (3)

Dopamine Transporter (4)

Drug Derivative (2)

Endogenous Metabolite (1)

Epigenetic Reader Domain (1)

ERK (5)

Estrogen Receptor/ERR (3)

Fat Mass and Obesity-associated Protein (FTO) (1)

FOXO (1)

GABA Receptor (10)

Gap Junction Protein (1)

Histone Demethylase (1)

iGluR (4)

Imidazoline Receptor (4)

Interleukin Related (2)

Isotope-Labeled Compounds (10)

mAChR (3)

Melatonin Receptor (4)

mGluR (1)

mTOR (2)

nAChR (2)

NADPH Oxidase (1)

Neurokinin Receptor (1)

Neuropeptide FF Receptor (1)

Neuropeptide Y Receptor (1)

Neurotensin Receptor (2)

Opioid Receptor (19)

PKA (2)

Reference Standards (12)

Ribosomal S6 Kinase (RSK) (1)

SARS-CoV (1)

Sodium Channel (3)

Trk Receptor (1)

Tyrosine Hydroxylase (1)

Virus Protease (1)

By Research Areas:

Cancer (10)

Cardiovascular Disease (8)

Endocrinology (10)

Infection (1)

Inflammation/Immunology (5)

Metabolic Disease (10)

Neurological Disease (72)

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-14538

Haloperidol Maximum Cited Publications 21 Publications Verification	Dopamine Receptor	Neurological Disease Cancer
Haloperidol is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic agent. Haloperidol can be used in the study of schizophrenia, tics in Tourette syndrome, mania in bipolar disorder, delirium, agitation, acute psychosis, and hallucinations from alcohol withdrawal.

HY-A0014

Ramelteon 10+ Cited Publications TAK-375	Melatonin Receptor	Neurological Disease Endocrinology Cancer
Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation .

HY-B0696A

Tiagabine hydrochloride NO050328 hydrochloride; NO328 hydrochloride; TGB hydrochloride	GABA Receptor	Neurological Disease
Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

HY-136661

(-)-N6-Phenylisopropyl adenosine L-Phenylisopropyladenosine; L-PIA; R-PIA	Adenosine Receptor	Cardiovascular Disease Neurological Disease
(-)-N6-phenylisopropyl adenosine (L-Phenylisopropyladenosine) is a selective A1 adenosine receptor agonist. (-)-N6-phenylisopropyl adenosine inhibits K ⁺-induced Ca ²⁺ uptake with an IC₅₀ value of 0.5 µM. (-)-N6-phenylisopropyl adenosine protects against ischemia-induced ventricular arrhythmias and atrial fibrillation, and exacerbates ethanol withdrawal symptoms. (-)-N6-phenylisopropyl adenosine also has analgesic effects .

HY-B0696

Tiagabine NO050328; NO328; TGB	GABA Receptor	Neurological Disease
Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

HY-B1830

Estradiol enanthate E2EN	Estrogen Receptor/ERR	Endocrinology
Estradiol enanthate (E2EN) is a shorter-acting estrogen. Estradiol enanthate is an injectable contraceptive in combination with Dihydroxyprogesterone acetophenide. Estradiol enanthate promotes withdrawal bleeding, in a pattern similar to menstruation .

HY-100903

Norbinaltorphimine dihydrochloride 5+ Cited Publications nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride	Opioid Receptor	Neurological Disease
Norbinaltorphimine dihydrochloride (nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride) is a selective, long-acting competitive antagonist of the κ-opioid receptor. Norbinaltorphimine dihydrochloride blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. Norbinaltorphimine dihydrochloride suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. Norbinaltorphimine dihydrochloride is applicable to research related to neurological disorders such as pain .

HY-117040

nor-Binaltorphimine 5+ Cited Publications Norbinaltorphimine; NorBNI	Opioid Receptor	Neurological Disease
nor-Binaltorphimine (Norbinaltorphimine; NorBNI) is a selective, long-acting competitive antagonist of the κ-opioid receptor. nor-Binaltorphimine blocks κ-opioid receptor-mediated analgesic effects, and inhibits butorphanol-induced changes in κ-opioid receptor binding kinetics, desensitization and down-regulation. nor-Binaltorphimine suppresses specific opioid withdrawal symptoms, precipitates withdrawal behaviors in butorphanol-dependent rats, and serves as a molecular probe for studying κ-opioid receptor-agonist interactions. nor-Binaltorphimine is applicable to research related to neurological disorders such as pain .

HY-14127

R121919 5+ Cited Publications NBI30775	CRFR	Neurological Disease Endocrinology
R121919 (NBI30775) is a potent and selective CRF1R antagonist with a K_i of 2 to 5 nM. R121919 has antidepressant and anxiolytic effects. R121919 alleviates defensive withdrawal in rats .

HY-B0424

Nitrendipine 3 Publications Verification BAY-E-5009	Calcium Channel Apoptosis	Cardiovascular Disease Neurological Disease Cancer
Nitrendipine (BAY-E-5009) is an orally active analog of Nifedipine (HY-B0284) and dihydropyridine calcium channel blocker. Nitrendipine induces Apoptosis. Nitrendipine has antihypertensive effects. Nitrendipine blocks alcohol and Morphine withdrawal symptoms. Nitrendipine reduces right ventricular hypertrophy and pulmonary vascular changes induced by intermittent hypoxia. Nitrendipine has anticancer effects on neuroblastoma .

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-107111

GSK1034702	mAChR	Neurological Disease
GSK1034702 is an orally active and allosteric agonist of M1 mAChR (pEC₅₀=8.1) that can cross the blood-brain barrier. GSK1034702 activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions) .

HY-A0142A

Dapiprazole hydrochloride	Adrenergic Receptor	Endocrinology
Dapiprazole hydrochloride is a potent, selective and orally active alpha-1 adrenoceptor antagonist. Dapiprazole hydrochloride suppresses the opioid withdrawal symptoms. Dapiprazole hydrochloride is also used as eye drops for reversing mydriasis .

HY-129079

TFMB-(R)-2-HG 3 Publications Verification	Estrogen Receptor/ERR Histone Demethylase Fat Mass and Obesity-associated Protein (FTO)	Cancer
TFMB-(R)-2-HG is a cell membrane-permeable (R)-2-HG and acute myeloid leukemia (AML) oncogenic factor. TFMB-(R)-2-HG competitively inhibits α-ketoglutarate-dependent dioxygenases such as KDM2B and FTO. TFMB-(R)-2-HG impairs cell differentiation in response to Estrogen withdrawal. TFMB-(R)-2-HG is used in acute myeloid leukemia and glioma research .

HY-164795A

SBI-810 hydrochloride	Neurotensin Receptor Arrestin iGluR ERK Sodium Channel	Neurological Disease
SBI-810 hydrochloride is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 hydrochloride promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 hydrochloride inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 hydrochloride effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 hydrochloride is applicable to research related to multiple pain disorders .

HY-164795

SBI-810	Neurotensin Receptor Arrestin iGluR ERK Sodium Channel	Neurological Disease
SBI-810 is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 promotes the recruitment of β-arrestin-2 to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 is applicable to research related to multiple pain disorders .

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-12783A

SCH 50911	GABA Receptor	Neurological Disease
SCH 50911 is a selective, orally active, blood-brain barrier permeable GABA-B receptor (GABA-B Receptor) antagonist with an IC₅₀ of 1.1 μM in rats. SCH 50911 blocks baclofen-induced antitussive effects, regulates neuronal firing and GABA release. SCH 50911 promotes spontaneous seizures during withdrawal in ethanol-dependent rats, alters reward-related neurotransmission, and reduces or suppresses lever responding and self-administration behaviors of alcohol and sucrose in rats. SCH 50911 is applicable to research related to ethanol withdrawal syndrome, absence epilepsy and alcohol use disorder .

HY-14538A

Haloperidol hydrochloride Maximum Cited Publications 21 Publications Verification	Dopamine Receptor	Neurological Disease Cancer
Haloperidol hydrochloride is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic agent. Haloperidol hydrochloride can be used in the study of schizophrenia, tics in Tourette syndrome, mania in bipolar disorder, delirium, agitation, acute psychosis, and hallucinations from alcohol withdrawal.

HY-104006

CYM51010	Opioid Receptor	Neurological Disease
CYM51010 is a biased ligand of μ-opioid receptor – δ-opioid receptor heterodimers with an EC₅₀ of 403 nM. CYM51010 exhibits anti-nociceptive activity similar to morphine but with a decreased levels of tolerance development and withdrawal symptoms .

HY-A0014S1

Ramelteon-d3 TAK-375-d₃	Melatonin Receptor	Others
Ramelteon-d₃ (TAK-375-d₃) is a deuterium-labelled Ramelteon (HY-A0014). Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with K_i values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation.

HY-168366

R-6890	Opioid Receptor	Neurological Disease
R-6890 is a Brorphine-related opioid receptor antagonist that exhibits differential binding activities toward rat opioid receptors (IC₅₀=4.6 nM (0.05 M Tris; pH 7.4) and 170 nM (0.05 M Tris+0.1 M NaCl)). R-6890 displaces bound labeled opioids from receptors, and its binding affinity is affected by environmental factors, decreasing in the presence of NaCl. R-6890 crosses the blood-brain barrier (BBB) and exerts analgesic effects in the warm water-induced tail-flick reflex model of male Wistar rats .

HY-163905

EG-2184	Gap Junction Protein	Neurological Disease
EG-2184 is a Pannexin-1 channel inhibitor. EG-2184 can be used in opioid withdrawal related research .

HY-106865

Mivazerol	Dopamine Receptor Adrenergic Receptor	Cardiovascular Disease
Mivazerol is a selective α2-adrenoceptor agonist. Mivazerol decreases the spontaneous release of serotonin (5-HT) and significantly inhibits the immobilization stress-induced enhancement of norepinephrine (NE), dopamine (DA) and dihydroxyphenylacetic acid (DOPAC). Mivazerol inhibits intrathecal release of glutamate evoked by halothane withdrawal in rats, and exerts neuroprotective effects in forebrain ischemia rats. Mivazerol can be used for myocardial ischemia research _.

HY-15691

PF-04455242	Opioid Receptor mTOR	Neurological Disease Metabolic Disease
PF-04455242 is an orally bioavailable, blood-brain barrier-permeable κ-opioid receptor (KOR) inhibitor. PF-04455242 blocks in vivo effects induced by KOR and MOR agonists, and elicits KOR-independent outward currents in ventral tegmental area neurons. PF-04455242 promotes energy expenditure and activates the hypothalamic mTOR pathway. PF-04455242 attenuates stress-induced behavioral effects and produces antidepressant-like effects. PF-04455242 can be used in studies related to pain, depression, addictive disorders, and obesity induced by estrogen withdrawal .

HY-P11032

Mp-4D7-pF2	SARS-CoV Virus Protease	Infection
Mp-4D7-pF2, a cell-penetrating bicyclic peptide, is a noncovalent SARS-CoV-2 main protease inhibitor with an IC₅₀ of 4.51 μM. Mp-4D7-pF2 has an antiviral activity against SARS-CoV-2 with no cytotoxicity. Mp-4D7-pF2 can used for COVID-19 infections research .

HY-123468

HA-1004	Cyclic GMP-AMP Synthase PKA ERK Tyrosine Hydroxylase Calcium Channel	Cardiovascular Disease Metabolic Disease
HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .

HY-A0014S

Ramelteon-d5 TAK-375-d₅	Isotope-Labeled Compounds Melatonin Receptor	Neurological Disease Endocrinology Cancer
Ramelteon-d₅ is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with K_i values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation .

HY-B0424S

Nitrendipine-d5 AY-E-5009-d₅	Isotope-Labeled Compounds Calcium Channel Apoptosis	Cardiovascular Disease Neurological Disease Cancer
Nitrendipine-d₅ is the deuterium labeled Nitrendipine (HY-B0424). Nitrendipine (BAY-E-5009) is an orally active analog of Nifedipine (HY-B0284) and dihydropyridine calcium channel blocker. Nitrendipine induces Apoptosis. Nitrendipine has antihypertensive effects. Nitrendipine blocks alcohol and Morphine withdrawal symptoms. Nitrendipine reduces right ventricular hypertrophy and pulmonary vascular changes induced by intermittent hypoxia. Nitrendipine has anticancer effects on neuroblastoma .

HY-A0142

Dapiprazole	Adrenergic Receptor	Endocrinology
Dapiprazole is a potent, selective and orally active alpha-1 adrenoceptor antagonist. Dapiprazole suppresses the opioid withdrawal symptoms. Dapiprazole is also used as eye drops for reversing mydriasis .

HY-B1830R

Estradiol enanthate (Standard) E2EN (Standard)	Reference Standards Estrogen Receptor/ERR	Endocrinology
Estradiol enanthate (Standard) is the analytical standard of Estradiol enanthate. Estradiol enanthate (E2EN) is a shorter-acting estrogen. Estradiol enanthate is an injectable contraceptive in combination with Dihydroxyprogesterone acetophenide. Estradiol enanthate promotes withdrawal bleeding, in a pattern similar to menstruation .

HY-B1052S

Lofexidine-d4 hydrochloride Baq-168-d₄; MDL-14042-d₄	Isotope-Labeled Compounds Imidazoline Receptor Adrenergic Receptor	Neurological Disease Metabolic Disease
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-106234

ZP 120C	Opioid Receptor	Cardiovascular Disease Neurological Disease
ZP 120C is a potent and partial ORL1 receptor agonist. ZP 120C inhibits electrically induced contraction. ZP 120C can be used in the research of hyponatremia/hypokalemia .

HY-178235

MDAN-21	Opioid Receptor	Neurological Disease
MDAN-21 is a bivalent opioid ligand that contains both μ-opioid receptor agonists and δ-opioid receptor antagonists. MDAN-21 has a strong analgesic effect and does not produce tolerance in mouse studies. MDAN-21 can effectively inhibit the withdrawal of morphine dependent monkeys and alleviate abnormal pain in the study of rhesus monkeys. MDAN-21 can be used for the study of allodynia .

HY-18610A

Diclofensine Ro 8-4650	Dopamine Transporter Adrenergic Receptor 5-HT Receptor	Neurological Disease
Diclofensine (Ro 8-46500) is an orally active neuronal monoamine uptake inhibitor. Diclofensine blocks the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC₅₀ values of 0.74, 2.3 and 3.7 nM, respectively. Diclofensine potentiates norepinephrine-induced hypertension and attenuates Tyramine (HY-W007606)-induced hypertension. Diclofensine produces psychostimulant and mood-elevating effects without causing sudden disappearance or withdrawal reactions. Diclofensine can be used in the research of moderate to severe depression .

HY-B0424R

Nitrendipine (Standard) BAY-E-5009 (Standard)	Reference Standards Calcium Channel Apoptosis	Cardiovascular Disease Neurological Disease Cancer
Nitrendipine (Standard) is the analytical standard of Nitrendipine (HY-B0424). This product is intended for research and analytical applications. Nitrendipine (BAY-E-5009) is an orally active analog of Nifedipine (HY-B0284) and dihydropyridine calcium channel blocker. Nitrendipine induces Apoptosis. Nitrendipine has antihypertensive effects. Nitrendipine blocks alcohol and Morphine withdrawal symptoms. Nitrendipine reduces right ventricular hypertrophy and pulmonary vascular changes induced by intermittent hypoxia. Nitrendipine has anticancer effects on neuroblastoma .

HY-144609

Mu opioid receptor antagonist 4	Opioid Receptor	Neurological Disease
Mu opioid receptor antagonist 4 (compound 31) is a potent and selective μ opioid receptor (MOR) antagonist with a K_i of 0.38 nM and an EC₅₀ of 1.07 nM. Mu opioid receptor antagonist 4 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 4 Mu opioid receptor antagonist 4 can be used for researching opioid use disorders (OUD) .

HY-144607

Mu opioid receptor antagonist 2	Opioid Receptor	Neurological Disease
Mu opioid receptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with a K_i of 0.37 nM and an EC₅₀ of 0.44 nM. Mu opioid receptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 2 can be used for researching opioid use disorders (OUD) .

HY-100781B

L-AP4 monohydrate L-APB monohydrate	mGluR	Neurological Disease
L-AP4 (L-APB) monohydrate is a potent and specific agonist for the group III mGluRs, with EC₅₀s of 0.13, 0.29, 1.0, 249 μM for mGlu₄, mGlu₈, mGlu₆ and mGlu₇ receptors, respectively .

HY-151811

NAQ	Opioid Receptor	Neurological Disease
NAQ is a potent and selective μ opioid receptor partial agonist, with a K_i of 0.55 nM. NAQ shows selectivity for Mu opioid receptor over the δ receptor (K_i=132.50 nM) and the κ receptor (K_i=26.45 nM). NAQ can be used for the research of opioid withdrawal or dependence .

HY-165616

NS 1231	Trk Receptor	Neurological Disease
NS 1231 is a neurotrophic-like compound with neuroprotective effect. NS 1231 can rescue nerve growth factor (NGF)-differentiated PC12 cells from death induced by withdrawal of trophic factors. NS 1231 can stimulate NGF-induced neurite outgrowth of undifferentiated PC12 cells. NS 1231 can be used for the research of neurological disease, such as stroke .

HY-P10394

DP32	Opioid Receptor Neuropeptide FF Receptor	Neurological Disease
DP32 is a bifunctional compound that contains an opioid receptor (MOP) agonist and a neuropeptide FF receptor (NPFFR) antagonist. DP32 can be used in analgesia-related research .

HY-18610

Diclofensine hydrochloride Ro 8-4650 hydrochloride	Dopamine Transporter Adrenergic Receptor 5-HT Receptor	Neurological Disease
Diclofensine (Ro 8-46500) hydrochloride is an orally active neuronal monoamine uptake inhibitor. Diclofensine hydrochloride blocks the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC₅₀ values of 0.74, 2.3 and 3.7 nM, respectively. Diclofensine hydrochloride potentiates norepinephrine-induced hypertension and attenuates Tyramine (HY-W007606)-induced hypertension. Diclofensine hydrochloride produces psychostimulant and mood-elevating effects without causing sudden disappearance or withdrawal reactions. Diclofensine hydrochloride can be used in the research of moderate to severe depression .

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 .

HY-P1441A

Mambalgin 1 TFA	Sodium Channel	Neurological Disease
Mambalgin 1 TFA is a selective ASIC1a inhibitor (IC₅₀ values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 TFA binds to closed/inactive channel. Mambalgin 1 TFA is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 TFA increases latency of withdrawal response in mouse tail-flick and paw-flick tests.

HY-122189

Akuammine (-)-Akuammine; Vincamajoridine	Others	Neurological Disease
Akuammine is an indole alkaloid that has been found in Picralima nitida and has analgesic activity. It selectively binds to the μ- and κ-opioid receptors over the δ-opioid receptor (Kis=0.3, 1.68, and 10.4 μM for the human receptors, respectively). Akuammine inhibits forskolin-induced cAMP production in HEK293 cells expressing human μ- or κ-opioid receptors (IC₅₀s=2.6 and 0.073 μM, respectively). It increases the latency to withdrawal in the tail-flick or hot plate test in mice when administered at a dose of 60 mg/kg.

HY-B0696B

Tiagabine hydrochloride hydrate NO050328 hydrochloride hydrate; NO328 hydrochloride hydrate; TGB hydrochloride hydrate	GABA Receptor	Neurological Disease
Tiagabine (NO050328; NO328; TGB) hydrochloride hydrate is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride hydrate exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride hydrate is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

HY-A0142AR

Dapiprazole hydrochloride (Standard)	Adrenergic Receptor Reference Standards	Endocrinology
Dapiprazole (hydrochloride) (Standard) is the analytical standard of Dapiprazole (hydrochloride). This product is intended for research and analytical applications. Dapiprazole hydrochloride is a potent, selective and orally active alpha-1 adrenoceptor antagonist. Dapiprazole hydrochloride suppresses the opioid withdrawal symptoms. Dapiprazole hydrochloride is also used as eye drops for reversing mydriasis .

HY-144608

Mu opioid receptor antagonist 3	Opioid Receptor	Neurological Disease
Mu opioid receptor antagonist 3 (compound 26) is a potent and selective μ opioid receptor (MOR) antagonist with a K_i of 0.24 nM and an EC₅₀ of 0.54 nM. Mu opioid receptor antagonist 3 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 3 can be used for researching opioid use disorders (OUD) .

HY-A0014R

Ramelteon (Standard) TAK-375 (Standard)	Reference Standards Melatonin Receptor	Neurological Disease Endocrinology Cancer
Ramelteon (Standard) is the analytical standard of Ramelteon. This product is intended for research and analytical applications. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with Ki values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation .

Cat. No.	Product Name

HY-L140

Withdrawn Drug Compound Library

230 compounds

Withdrawal or delisting drugs refer to drugs that are recalled or discontinued from the market due to low efficiency, serious side effects, financial and regulatory problems and other reasons. Once the drug is withdrawn from the market, it will cause heavy losses to the original research company that invested a lot of time, finance and other costs to develop the drug.

Adverse drug reaction (ADR) is the main reason for drug withdrawal from the market. ADR refers to the unexpected effects caused by the reasons such as the target-directed interaction during the treatment. However, studying the mechanism of these ADRs may just be a breakthrough in finding new indications. For example, thalidomide, the protagonist of the drug damage event that caused numerous "seal babies" deformed infants, was found to be due to the degradation of a transcription factor - SALL4 after delisting, which made thalidomide have a new clinical application. In 1998, it was approved by FDA for the treatment of leprosy nodular erythema, and in 2006, it was approved for the treatment of multiple myeloma. ADR study of delisted drugs can not only avoid the loss of drug development in advance but also bring hope to new indications.

MCE has sorted out 230 drug compounds withdrawn from the market through FDA, EMA and other authoritative platforms. Each compound has withdrawal records in at least one country/market. It is a useful tool for conducting research on drug side effects or drug toxicity mechanisms and discovering new indications of drugs.

HY-L225

Cardiotoxic Compound Library

258 compounds

Drug development is both expensive and time-consuming, with approximately one-third of drug discontinuations caused by severe adverse drug reactions (ADRs). Among these, drug-induced cardiotoxicity (DICT) is one of the primary reasons for late-stage clinical drug failures and market withdrawals. To date, cardiotoxicity has been observed in multiple drug classes, such as anticancer drugs, antipsychotics, antidepressants, antibiotics, and neurodegenerative disease medications. To reduce cardiac ADRs, it is crucial to determine the clinical relevance of DICT to treatment, elucidate the underlying molecular mechanisms, identify reliable biomarkers, and develop new diagnostic and therapeutic approaches.

MCE offers 258 cardiotoxicity compounds, including some FDA-approved drugs as well as inhibitors/blockers of the hERG potassium channel.

HY-L076

Drug-Induced Liver Injury (DILI) Compound Library

641 compounds

Drug-induced liver injury (DILI; also known as drug-induced hepatotoxicity) is caused by medications (prescription or OTC), herbal and dietary supplements (HDS), or other xenobiotics that result in abnormalities in liver tests or in hepatic dysfunction that cannot be explained by other causes. Drugs are an important cause of liver injury. Drug-induced hepatic injury is the most common reason cited for withdrawal of an approved drug.

DILI is thought to occur via several different mechanisms. Among these are direct impairment of the structural (e.g., mitochondrial dysfunction) and functional integrity of the liver; production of a metabolite that alters hepatocellular structure and function; production of a reactive drug metabolite that binds to hepatic proteins to produce new antigenic drug-protein adducts, which are targeted by hosts’ defenses (the hapten hypothesis); and initiation of a systemic hypersensitivity response (i.e., drug allergy) that damages the liver.

MCE Drug-induced Liver Injury (DILI) Compound Library contains a unique collection of 641 hepatotoxicity causing compounds and is a powerful tool to research DILI and other drug toxicities. This library can be used to understand the mechanisms of DILI, identify biomarkers for early DILI prediction, and allow timely recognition during drug development, thus finally achieving successful DILI prevention and assessment in the pre-marketing phase.

Cat. No.	Product Name	Target	Research Area

HY-P11032

Mp-4D7-pF2	SARS-CoV Virus Protease	Infection
Mp-4D7-pF2, a cell-penetrating bicyclic peptide, is a noncovalent SARS-CoV-2 main protease inhibitor with an IC₅₀ of 4.51 μM. Mp-4D7-pF2 has an antiviral activity against SARS-CoV-2 with no cytotoxicity. Mp-4D7-pF2 can used for COVID-19 infections research .

HY-106234

ZP 120C	Opioid Receptor	Cardiovascular Disease Neurological Disease
ZP 120C is a potent and partial ORL1 receptor agonist. ZP 120C inhibits electrically induced contraction. ZP 120C can be used in the research of hyponatremia/hypokalemia .

HY-P3628

Dynorphin (2-17) (porcine)	Peptides	Neurological Disease
Dynorphin (2-17) (porcine) is a peptide derived from Prodynorphin, can improve somatic signs of Morphine-dependent withdrawal .

HY-P10394

DP32	Opioid Receptor Neuropeptide FF Receptor	Neurological Disease
DP32 is a bifunctional compound that contains an opioid receptor (MOP) agonist and a neuropeptide FF receptor (NPFFR) antagonist. DP32 can be used in analgesia-related research .

HY-P1441A

Mambalgin 1 TFA	Sodium Channel	Neurological Disease
Mambalgin 1 TFA is a selective ASIC1a inhibitor (IC₅₀ values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 TFA binds to closed/inactive channel. Mambalgin 1 TFA is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 TFA increases latency of withdrawal response in mouse tail-flick and paw-flick tests.

HY-P3252AS

Pegcetacoplan-13C3,15N TFA	Isotope-Labeled Compounds Complement System	Inflammation/Immunology
Pegcetacoplan- ¹³C₃, ¹⁵N TFA is the ¹³C- and ¹⁵N-labeled Pegcetacoplan TFA. Pegcetacoplan is a pegylated complement C3/C3b inhibitor. Pegcetacoplan acts by specifically binding to and inhibiting C3 and C3b, thereby suppressing the complement cascade at its proximal stage. Pegcetacoplan is not a known inhibitor or inducer of CYP450 isoenzymes. Pegcetacoplan can be used for the research of complement-mediated diseases, including paroxysmal nocturnal hemoglobinuria (PNH) and age-related macular degeneration (AMD).

Cat. No.	Product Name	Target	Research Area	Image

HY-P992150

Altrakincept	Interleukin Related	Inflammation/Immunology
Altrakincept is a recombinant hIL-4 receptor and IL-4 neutralizer. Altrakincept neutralizes endogenous IL-4, and prevents the decline of pulmonary function and acute asthma exacerbations after abrupt withdrawal of inhaled glucocorticoids .

HY-P992000

F8-IL-4	Interleukin Related	Inflammation/Immunology
F8-IL-4 is an immune cytokine targeting IL-4. F8-IL-4 specifically delivers IL-4 to inflammatory sites via binding to targets expressed on neovascular vessels. F8-IL-4 alleviates collagen-induced arthritis in mice by regulating T cell subsets and macrophage polarization. When combined with Dexamethasone (HY-14648), F8-IL-4 produces a synergistic and long-lasting therapeutic effect, and prevents arthritis recurrence after drug withdrawal by maintaining anti-inflammatory cell phenotypes and cytokine profiles. F8-IL-4 can be used in the research of collagen-induced arthritis .

Cat. No.	Product Name	Chemical Structure

HY-A0014S1

Ramelteon-d3

Ramelteon-d₃ (TAK-375-d₃) is a deuterium-labelled Ramelteon (HY-A0014). Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with K_i values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation.

HY-A0014S

Ramelteon-d5

Ramelteon-d₅ is deuterium labeled Ramelteon. Ramelteon is a potent, highly selective, and orally active agonist of MT1/MT2 with K_i values of 14 and 112 pM, respectively. Ramelteon has the potential for the research of insomnia. Ramelteon consistently reduces sleep onset after long-term treatment, with no next-morning residual effects or rebound insomnia or withdrawal symptoms upon discontinuation .

HY-B0424S

Nitrendipine-d5

Nitrendipine-d₅ is the deuterium labeled Nitrendipine (HY-B0424). Nitrendipine (BAY-E-5009) is an orally active analog of Nifedipine (HY-B0284) and dihydropyridine calcium channel blocker. Nitrendipine induces Apoptosis. Nitrendipine has antihypertensive effects. Nitrendipine blocks alcohol and Morphine withdrawal symptoms. Nitrendipine reduces right ventricular hypertrophy and pulmonary vascular changes induced by intermittent hypoxia. Nitrendipine has anticancer effects on neuroblastoma .

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-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-18610S

Diclofensine-d3 hydrochloride

Diclofensine-d₃ (Ro-8-4650-d₃) hydrochloride is the deuterium labeled Diclofensine hydrochloride. Diclofensine hydrochloride is an orally active neuronal monoamine uptake inhibitor. Diclofensine hydrochloride blocks the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC₅₀ values of 0.74, 2.3 and 3.7 nM, respectively. Diclofensine hydrochloride potentiates norepinephrine-induced hypertension and attenuates Tyramine (HY-W007606)-induced hypertension. Diclofensine hydrochloride produces psychostimulant and mood-elevating effects without causing sudden disappearance or withdrawal reactions. Diclofensine hydrochloride can be used in the research of moderate to severe depression.

HY-B0696S

Tiagabine-d6

Tiagabine-d₆ (NO050328-d₆) is deuterium labeled Tiagabine. Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

HY-B0696AS

Tiagabine-d4 hydrochloride

Tiagabine-d₄ hydrochloride is deuterated labeled Tiagabine hydrochloride (HY-B0696A). Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

HY-P3252AS

Pegcetacoplan-13C3,15N TFA

Pegcetacoplan- ¹³C₃, ¹⁵N TFA is the ¹³C- and ¹⁵N-labeled Pegcetacoplan TFA. Pegcetacoplan is a pegylated complement C3/C3b inhibitor. Pegcetacoplan acts by specifically binding to and inhibiting C3 and C3b, thereby suppressing the complement cascade at its proximal stage. Pegcetacoplan is not a known inhibitor or inducer of CYP450 isoenzymes. Pegcetacoplan can be used for the research of complement-mediated diseases, including paroxysmal nocturnal hemoglobinuria (PNH) and age-related macular degeneration (AMD).

HY-158252S

Tiagabine-d5 hydrochloride

Tiagabine-d₅ (hydrochloride) is deuterium labeled Tiagabine (hydrochloride). Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

HY-B0696S1

Tiagabine-d4

Tiagabine-d₄ (NO050328-d₄) is deuterium labeled Tiagabine. Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: