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potent mu opioid receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Opioid Receptor (35) 5-HT Receptor (1) Angiotensin-converting Enzyme (ACE) (1) Drug Metabolite (1) Endogenous Metabolite (1) Isotope-Labeled Compounds (1) Reference Standards (3) Sigma Receptor (1) TRP Channel (2)
By Research Areas:	Cancer (5) Cardiovascular Disease (1) Inflammation/Immunology (1) Metabolic Disease (3) Neurological Disease (34)

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Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Opioid Receptor

Cat. No.	Nombre del producto	Target	Áreas de investigación	Chemical Structure

HY-19627A

Naldemedine tosylate 1 Publications Verification S-297995 tosylate	Opioid Receptor	Neurological Disease Metabolic Disease
Naldemedine (S-297995) tosylate is an orally active μ-opioid receptor antagonist (PAMORA) . Naldemedine tosylate shows potent binding affinities (K_i=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC₅₀=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors . Naldemedine can be used in opioid-induced constipation (OIC) research . Naldemedine tosylate is predicted to bind to 3CL ^pro encoded by SARS-CoV2 genome .

HY-13243

Alvimopan 2 Publications Verification ADL 8-2698; LY 246736	Opioid Receptor	Neurological Disease
Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC₅₀ of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (K_i=0.47 nM) over κ- and δ-opioid receptors (K_is=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus .

HY-101302

Naltriben mesylate 2 Publications Verification	Opioid Receptor TRP Channel	Inflammation/Immunology
Naltriben mesylate is a potent δ2-opioid receptor antagonist and a TRPM7 activator. Naltriben mesylate shows K_i values of 0.013 nM, 19 nM and 152 nM for δ, μ and κ receptors, respectively. Naltriben mesylate enhances glioblastoma cell migration and invasion. Naltriben mesylate can be used in research into neurological diseases and cancer .

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-145404

Mitragynine pseudoindoxyl 1 Publications Verification	Opioid Receptor	Metabolic Disease
Mitragynine pseudoindoxyl is a potent orally active agonist of the μ-opioid receptor (MOR-1, K_i=0.8 nM) and an antagonist of the δ-opioid receptor (DOR-1, K_i=3.0 nM). Mitragynine pseudoindoxyl has moderate affinity for the κ-opioid receptor (KOR-1, K_i=24 nM) and does not recruit β-arrestin-2, acting through G protein-mediated signaling pathways without β-arrestin-2-related activation. Mitragynine pseudoindoxyl produces potent analgesic activity through a mixed μ-agonist/δ-antagonist mechanism, with low side effects such as physical dependence, respiratory depression, and constipation, and no rewarding or aversive behaviors. Mitragynine pseudoindoxyl reduces hyperactivity, inhibits GI transit, and enhances characteristics, making it a potential analgesic .

HY-115066

GSK1521498 free base	Opioid Receptor	Neurological Disease
GSK1521498 free base is a potent and selective *μ-opioid* receptor (MOR)** antagonist. GSK1521498 free base has the potential for disorders of compulsive consumption of food, alcohol, and agents .

HY-19627

Naldemedine S-297995	Opioid Receptor	Neurological Disease Metabolic Disease
Naldemedine (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA) . Naldemedine shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC₅₀=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors . Naldemedine can be used in opioid-induced constipation (OIC) research . Naldemedine is predicted to bind to 3CL ^pro encoded by SARS-CoV2 genome .

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-P1329A

CTOP TFA 1 Publications Verification	Opioid Receptor	Neurological Disease
CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity .

HY-76657A

Alvimopan dihydrate 2 Publications Verification ADL 8-2698 dihydrate; LY 246736 dihydrate	Opioid Receptor	Neurological Disease Cancer
Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC₅₀ of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (K_i=0.47 nM) over κ- and δ-opioid receptors (K_is=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .

HY-107743

Naloxone benzoylhydrazone NalBzoH	Opioid Receptor	Neurological Disease
Naloxone benzoylhydrazone (NalBzoH) is a mixed agonist/antagonist. Naloxone benzoylhydrazone is a prototypic κ3-opioid receptor agonist, and a partial agonist at the cloned μ and δ opioid receptors, and an antagonist at **opioid-like NOP receptors*. Naloxone benzoylhydrazone has potently* analgesia effect .

HY-19902

GSK1521498	Opioid Receptor	Neurological Disease
GSK1521498 is a potent and selective *μ-opioid* receptor (MOR)** antagonist. GSK1521498 has the potential for disorders of compulsive consumption of food, alcohol, and agents .

HY-A0115R

Ramiprilat (Standard) HOE 498 diacid (Standard); Ramipril diacid (Standard)	Drug Metabolite Reference Standards Angiotensin-converting Enzyme (ACE) Endogenous Metabolite	Cardiovascular Disease
Alvimopan (dihydrate) (Standard) is the analytical standard of Alvimopan (dihydrate). This product is intended for research and analytical applications. Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .

HY-115066A

GSK1521498 free base hydrochloride	Opioid Receptor	Neurological Disease
GSK1521498 free base (hydrochloride) is a potent and selective *μ-opioid* receptor (MOR)** antagonist. GSK1521498 free base (hydrochloride) is being used for the treatment of disorders of compulsive consumption of food, alcohol, and agents .

HY-P1329

CTOP	Opioid Receptor	Neurological Disease
CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .

HY-P1299A

UFP-101 TFA	Opioid Receptor	Neurological Disease
UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pK_i of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect .

HY-16979

TRK-851	Opioid Receptor	Neurological Disease
RK-851 is a highly selective and orally active δ-opioid receptor antagonist, with a negative logarithm of the antagonist concentration (pA₂) of 8.84. TRK-851 exhibits the selectivity for the δ receptor of more than 100 times higher than that for the μ or κ receptors. TRK-851 exhibits a potent antitussive effect in a rat model of capsaicin-induced cough. TRK-851 can be used for research on antitussive effects .

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-155320

Mu opioid receptor antagonist 7	Opioid Receptor	Neurological Disease
Mu opioid receptor antagonist 7 (compound 24) is a potent and CNS permeable antagonist of µOR (µ-opioid receptor), with an IC₅₀ of 29 ± 3.0 nM. Mu opioid receptor antagonist 7 can be used for the research of pain and opioid use disorder .

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-76657

Alvimopan monohydrate ADL 8-2698 monohydrate; LY 246736 monohydrate	Opioid Receptor	Neurological Disease Cancer
Alvimopan monohydrate (ADL 8-2698 monohydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC₅₀ of 1.7 nM. Alvimopan monohydrate has selectivity for μ-opioid receptor (K_i=0.47 nM) over κ- and δ-opioid receptors (K_is=100, 12 nM, respectively). Alvimopan monohydrate can be used for the research of postoperative ileus .

HY-106601A

Picenadol hydrochloride LY-150720 hydrochloride	Opioid Receptor	Neurological Disease
Picenadol (LY-150720) hydrochloride is an opioid mixed agonist-antagonist analgesic. Picenadol hydrochloride is an external racemic mixture, where its d-isomer (LY136596) is a potent μ-opioid receptor agonist, and the l-isomer (LY136595) is a weak μ-receptor competitive antagonist, which can inhibit the agonist effect and reduce the risk of dependence. Picenadol hydrochloride has anticholinergic activity .

HY-P1299

UFP-101	Opioid Receptor	Neurological Disease
UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pK_i of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect .

HY-176063

TRPV1 antagonist 11	TRP Channel Opioid Receptor	Neurological Disease
TRPV1 antagonist 11 (compound 2ac) is a potent TRPV1 antagonist with an IC₅₀ of 29.3 nM. TRPV1 antagonist 11 is a potent *μ-opioid* receptor (MOR)** agonist with a K_i of 60.3 nM. TRPV1 antagonist 11, a pyrimidine piperazine, exhibits pain relieving effects by antagonizing TRPV1 and stimulating MOR. TRPV1 antagonist 11 shows a potent, dose-dependent anti-nociceptive effect in a Formalin-induced pain model in mice .

HY-179282

Mu opioid receptor antagonist 9	Opioid Receptor	Neurological Disease
Mu opioid receptor antagonist 9 is potent, selective and CNS-pentrant mu-opioid receptor (MOR) antagonist with a K_i of 77.3 nM. Mu opioid receptor antagonist 9 exhibits selectivity over kappa-opioid receptor (KOR), and delta-opioid receptor (DOR). Mu opioid receptor antagonist 9 effectively blocks the antinociceptive effects of psychoactive substances. Mu opioid receptor antagonist 9 can reverse psychoactive substances-induced respiratory depression in mice. Mu opioid receptor antagonist 9 can be used for the research of Opioid Use Disorder (OUD) .

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-147560

σ1 Receptor/μ Opioid receptor modulator 1	Sigma Receptor Opioid Receptor	Neurological Disease
σ1 Receptor/μ Opioid receptor modulator 1 (Compound 44) is a potent σ1 receptor antagonist and μ opioid receptor agonist with K_is of 1.86 nM and 2.1 nM, respectively.σ1 Receptor/μ Opioid receptor modulator 1 exhibits potent analgesic activity. σ1 Receptor/μ Opioid receptor modulator 1 can be used for the research of neuropathic pain .

HY-123142

RX809055AX	Opioid Receptor	Neurological Disease
RX 809055AX is a potent long lasting *opioid* antagonist with selectivity towards at mu and delta receptors .

HY-106601

Picenadol LY-150720	Opioid Receptor	Neurological Disease
Picenadol (LY-150720) is an opioid mixed agonist-antagonist analgesic. Picenadol is an external racemic mixture, where its d-isomer (LY136596) is a potent μ-opioid receptor agonist, and the l-isomer (LY136595) is a weak μ-receptor competitive antagonist, which can inhibit the agonist effect and reduce the risk of dependence. Picenadol has anticholinergic activity .

HY-13243R

Alvimopan (Standard) ADL 8-2698 (Standard); LY 246736 (Standard)	Opioid Receptor Reference Standards	Neurological Disease Cancer
Alvimopan (Standard) is the analytical standard of Alvimopan. This product is intended for research and analytical applications. Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus .

HY-76657AR

Alvimopan dihydrate (Standard) ADL 8-2698 dihydrate (Standard); LY 246736 dihydrate (Standard)	Reference Standards Opioid Receptor	Neurological Disease Cancer
Alvimopan (dihydrate) (Standard) is the analytical standard of Alvimopan (dihydrate). This product is intended for research and analytical applications. Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .

HY-170437

MOR modulator-1	Opioid Receptor	Neurological Disease
MOR modulator-1 (compound 6) is a potent and selective *μ opioid* receptor (MOR)** modulator. MOR modulator-1 exhibits improved opioid receptor selectivity, enhanced in vivo antagonistic effect, and overall fewer withdrawal symptoms compared to NAT (6α-configuration). MOR modulator-1 links with carboxamido linker μ, δ, γ with K_is of 0.25, 41.1, 1.30 nM, respectively_[1]

HY-123582

CP-866,087	Opioid Receptor	Neurological Disease
CP-866,087 is a novel, potent and selective μ-opioid receptor antagonist with activity to inhibit opioid effects. CP-866,087 has shown promising preclinical efficacy data in disease models associated with alcohol consumption. CP-866,087 has also been used to study female sexual dysfunction .

HY-11052A

Trap-101 hydrochloride	Opioid Receptor	Neurological Disease
Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ ³⁵S binding to CHO_hNOP membranes with pK_i values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases .

HY-119733

BU09059	Opioid Receptor	Neurological Disease
BU09059 is a potent and selective Kappa-opioid receptor antagonist with a pA₂ of 8.62. BU09059 has nanomolar affinity for the κ-receptor, with 15-fold and 616-fold selectivity over μ- and δ-receptors, respectively. BU09059 significantly blocks U50488 (HY-15997B)-induced antinociception .

HY-101343

RS 39604	5-HT Receptor	Neurological Disease
RS 39604 is a potent, selective, and orally active 5-HT₄ receptor antagonist with a pK_i of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pK_i<6.5) for 5-HT_1A, 5-HT_2C, 5-HT₃, α_1c, D₁, D₂, M₁, M₂, AT₁, B₁ and opioid mu receptors and moderate affinity for δ₁, (pK_i=6.8) and δ₂ (pK_i=7.8) sites .

HY-13243S1

Alvimopan-d7 ADL 8-2698-d₇; LY 246736-d₇	Isotope-Labeled Compounds Opioid Receptor	Neurological Disease Cancer
Alvimopan-d₇ (ADL 8-2698-d₇) is deuterium labeled Alvimopan. Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC₅₀ of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (K_i=0.47 nM) over κ- and δ-opioid receptors (K_is=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus .

Cat. No.	Nombre del producto	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-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-P1329A

CTOP TFA 1 Publications Verification	Opioid Receptor	Neurological Disease
CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity .

HY-P1329

CTOP	Opioid Receptor	Neurological Disease
CTOP is a potent and highly selective μ-opioid receptor antagonist. CTOP antagonizes the acute morphine-induced analgesic effect and hypermotility. CTOP enhances extracellular dopamine levels in the nucleus accumbens. CTOP dose-dependently enhances locomotor activity .

HY-P1299A

UFP-101 TFA	Opioid Receptor	Neurological Disease
UFP-101 TFA is a potent, selective, and competitive antagonist of the N/OFQ peptide (NOP) receptor, with a pK_i of 10.24. UFP-101 TFA displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 TFA shows antidepressant-like effect .

HY-P1299

UFP-101	Opioid Receptor	Neurological Disease
UFP-101 is a potent, selective, and competitive antagonist of the NOP receptor, with a pK_i of 10.24. UFP-101 displays >3000-fold selectivity over δ, μ and κ opioid receptors. UFP-101 shows antidepressant-like effect .

Cat. No.	Nombre del producto	Category	Target	Chemical Structure

HY-A0115R

Ramiprilat (Standard) HOE 498 diacid (Standard); Ramipril diacid (Standard)	Structural Classification Alkaloids Pyrrole Alkaloids Endogenous metabolite Source Classification	Drug Metabolite Reference Standards Angiotensin-converting Enzyme (ACE) Endogenous Metabolite
Alvimopan (dihydrate) (Standard) is the analytical standard of Alvimopan (dihydrate). This product is intended for research and analytical applications. Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC50 of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (Ki=0.47 nM) over κ- and δ-opioid receptors (Kis=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus .

Cat. No.	Nombre del producto	Chemical Structure

HY-13243S1

Alvimopan-d7

Alvimopan-d₇ (ADL 8-2698-d₇) is deuterium labeled Alvimopan. Alvimopan (ADL 8-2698) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC₅₀ of 1.7 nM. Alvimopan has selectivity for μ-opioid receptor (K_i=0.47 nM) over κ- and δ-opioid receptors (K_is=100, 12 nM, respectively). Alvimopan can be used for the research of postoperative ileus .

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potent mu opioid receptor antagonist

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