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Opioid receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Opioid Receptor (58) 5-HT Receptor (3) Dopamine Receptor (1) GABA Receptor (1) GlyT (2) iGluR (1) Isotope-Labeled Compounds (1) P2X Receptor (2) Potassium Channel (1) Sigma Receptor (4)
By Research Areas:	Cancer (2) Infection (1) Inflammation/Immunology (1) Metabolic Disease (5) Neurological Disease (61)

Inhibitors & Agonists

Peptides

Isotope-Labeled Compounds

Targets Recommended: Opioid Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-144610

*Mu opioid* receptor antagonist 5**	Opioid Receptor	Neurological Disease
Mu opioid receptor antagonist 5 (compound NAP) is a selective and blood-brain barrier (BBB) penetrant *μ opioid* receptor (MOR)** antagonist with an EC₅₀ value of 1.14 nM and a K_i value of 0.37 nM. Mu opioid receptor antagonist 5 can be used for researching opioid use disorders (OUD) .

HY-144606

*Mu opioid* receptor antagonist 1**	Opioid Receptor	Neurological Disease
Mu opioid receptor antagonist 1 (compound 19) is a selective and orally active *μ opioid* receptor (MOR) ligand with an K_i value of 0.58 nM and an EC₅₀** of 1.15 nM. Orally administrating with Mu opioid receptor antagonist 1 increases intestinal motility during morphine-induced constipation. Mu opioid receptor antagonist 1 can be used for researching opioid-induced constipation (OIC) .

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-17417A

Naloxone	Opioid Receptor	Neurological Disease
Naloxone is an antagonist of **Opioid receptor*. Naloxone alleviates opioid*-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias .

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-123689

Samidorphan ALKS-33; RDC-0313	Opioid Receptor	Neurological Disease
Samidorphan (ALKS-33) is an orally active *opioid* system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .

HY-120277

TIPP

H-Tyr-Tic-Phe-Phe-OH
Opioid Receptor Neurological Disease

TIPP is a potent and selective δ-opioid antagonist with a K_i value of 1.22 nM .
HY-10486

JDTic

Opioid Receptor Neurological Disease

JDTic is a highly selective antagonist for the κ-opioid receptor; without affecting the μ- or δ-opioid receptors.

TIPP H-Tyr-Tic-Phe-Phe-OH	Opioid Receptor	Neurological Disease
TIPP is a potent and selective δ-opioid antagonist with a K_i value of 1.22 nM .

JDTic	Opioid Receptor	Neurological Disease
JDTic is a highly selective antagonist for the κ-opioid receptor; without affecting the μ- or δ-opioid receptors.

HY-A0118

Naloxegol NKTR-118; AZ-13337019	Opioid Receptor	Neurological Disease
Naloxegol (NKTR-118; AZ-13337019) is a μ-opioid-receptor antagonist. Naloxegol inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .

HY-100903

Norbinaltorphimine dihydrochloride 3 Publications Verification nor-Binaltorphimine dihydrochloride; nor-BNI dihydrochloride	Opioid Receptor	Neurological Disease
Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.

HY-156614

Icalcaprant

Opioid Receptor Neurological Disease

Icalcaprant is a kappa-opioid receptor antagonist .

Icalcaprant	Opioid Receptor	Neurological Disease
Icalcaprant is a kappa-opioid receptor antagonist .

HY-A0118A

Naloxegol oxalate 2 Publications Verification NKTR-118 oxalate; AZ-13337019 oxalate	Opioid Receptor	Neurological Disease
Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a *μ-opioid-receptor* antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation .

HY-107748

5'-Guanidinonaltrindole hydrochloride 5'-GNTI hydrochloride	Opioid Receptor	Neurological Disease
5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent κ-opioid receptor antagonist with a K_i of 0.18 nM for human κ-opioid receptor .

HY-112263

ORL1 antagonist 1

Opioid Receptor Neurological Disease Metabolic Disease

ORL1 antagonist 1 is an opioid receptor-like 1 (ORL1) antagonist with an IC₅₀ of 61 nM.
HY-100122

Bevenopran

1 Publications Verification

CB-5945; ADL-5945
Opioid Receptor Neurological Disease

Bevenopran is a peripheral μ-opioid receptor antagonist .

ORL1 antagonist 1	Opioid Receptor	Neurological Disease Metabolic Disease
ORL1 antagonist 1 is an opioid receptor-like 1 (ORL1) antagonist with an IC₅₀ of 61 nM.

Bevenopran 1 Publications Verification CB-5945; ADL-5945	Opioid Receptor	Neurological Disease
Bevenopran is a peripheral μ-opioid receptor antagonist .

HY-17417

Naloxone hydrochloride 2 Publications Verification	Opioid Receptor	Neurological Disease
Naloxone hydrochloride is an antagonist of **Opioid receptor*. Naloxone hydrochloride alleviates opioid*-overdose-induced respiratory depression. Naloxone hydrochloride may cause pulmonary edema and cardiac arrhythmias .

HY-101306

Clocinnamox mesylate
Clocinnamox (mesylate) is a potent **opioid antagonist** acting at mu, kappa and delta-receptors. Clocinnamox is a selective mu-receptor antagonist than kappa and delta-receptors .

HY-17417AS

Naloxone-d5

Opioid Receptor Others

Naloxone D5 is deuterium labeled Naloxone. Naloxone is a a potent opioid receptor antagonist.

Naloxone-d5	Opioid Receptor	Others
Naloxone D5 is deuterium labeled Naloxone. Naloxone is a a potent **opioid receptor** antagonist.

HY-A0118AS

Naloxegol-d5 oxalate	Isotope-Labeled Compounds Opioid Receptor	Neurological Disease
Naloxegol-d₅ (oxalate) is deuterium labeled Naloxegol (oxalate). Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a μ-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation[1][2].

HY-P10177

Acetalin-3	Opioid Receptor	Neurological Disease
Acetalin-3 (Ac-RFMWMT-NH2), a hexapeptide, is a μ opioid receptor antagonist with high affinity for μ and κ3 opioid receptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .

HY-P10175

Acetalin-1	Opioid Receptor	Neurological Disease
Acetalin-1 (Ac-RFMWMK-NH2), a hexapeptide, is a μ opioid receptor antagonist with high affinity for μ and κ3 opioid receptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .

HY-101376

(+)-N-Allylnormetazocine hydrochloride (+)-SKF 10047 hydrochloride; (+)-N-Allyl-N-normetazocine hydrochloride	Opioid Receptor	Neurological Disease
(+)-N-Allylnormetazocine ((+)-SKF 10047) hydrochloride is a benzomorphan opioid with psychotomi metic effects. (+)-N-Allylnormetazocine hydrochloride is an **opioid receptor** antagonist with K_i values of 300 nM and 27 μM for σ1 and σ2 opioid receptors, respectively. (+)-N-Allylnormetazocine hydrochloride can be used for the research of neurological disease .

HY-101233

ICI 154129

M 154129

ICI 154 129 is a delta-opioid receptor antagonist and can be used for seizure research.

ICI 154129 M 154129
ICI 154 129 is a delta-opioid receptor antagonist and can be used for seizure research.

HY-101718

Aticaprant 4 Publications Verification CERC-501; LY-2456302	Opioid Receptor	Neurological Disease
Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a K_i of 0.807 nM.

HY-107749

ML 190

Opioid Receptor Neurological Disease

ML 190 is a selective κ opioid receptor (KOR) antagonist with an IC₅₀ of 120 nM and an EC₅₀ of 129 nM, respectively .

ML 190	Opioid Receptor	Neurological Disease
ML 190 is a selective *κ opioid* receptor (KOR)** antagonist with an IC₅₀ of 120 nM and an EC₅₀ of 129 nM, respectively .

HY-13274

JTC-801 4 Publications Verification	Opioid Receptor	Neurological Disease
JTC-801 is a selective **opioid receptor-like1 (ORL1) receptor** antagonist, binding to ORL1 receptor with a K_i value of 8.2 nM.

HY-13243

Alvimopan 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-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-101199

N-Benzylnaltrindole hydrochloride	Opioid Receptor	Neurological Disease
N-Benzylnaltrindole hydrochloride is a potent δ2-selective opioid receptor antagonist. Benzylnaltrindole hydrochloride has a long duration of action in vivo than Naltriben (NTB). N-Benzylnaltrindole hydrochloride iserve as a useful tool in the pharmacologic characterization of δ-opioid receptor function .

HY-117040

nor-Binaltorphimine Norbinaltorphimine; NorBNI	Opioid Receptor	Others
nor-Binaltorphimine is a selective antagonist of kappa-opioid receptor. nor-Binaltorphimine has a long-lasting effect in vivo .

HY-76657A

Alvimopan dihydrate 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-10487

JDTic dihydrochloride	Opioid Receptor	Neurological Disease
JDTic (dihydrochloride) is a potent antagonist of *kappa-opioid* receptors (KOR)*, blocking the κ-agonist* U50, 488-induced antinociception.

HY-136208

TAN-452	Opioid Receptor	Neurological Disease
TAN-452 is an orally active, selective peripherally acting *δ-opioid* receptor (DOR)** antagonist with a K_i of 0.47 nM and a K_b of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; K_i=36.56 nM and K_b=9.43 nM) and κ-opioid receptor (KOR; K_i=5.31 nM and K_b=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control .

HY-101011

Naloxonazine dihydrochloride	Opioid Receptor	Infection Neurological Disease
Naloxonazine dihydrochloride is a specific μ-opioid receptor antagonist with an IC₅₀ of 5.4 nM. Naloxonazine dihydrochloride also shows anti-leishmanial activity .

HY-114072A

(S,S)-J-113397

Opioid Receptor Neurological Disease

(S,S)-J-113397 is an isomer of J-113397 (HY-114072). J-113397 is an Opioid Receptor antagonist .

(S,S)-J-113397	Opioid Receptor	Neurological Disease
(S,S)-J-113397 is an isomer of J-113397 (HY-114072). J-113397 is an **Opioid Receptor** antagonist .

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-19627A

Naldemedine tosylate 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-P1335

CTAP	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-114072

J-113397	Opioid Receptor	Neurological Disease
J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (K_i: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors .

HY-19902

GSK1521498
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-101223

DIPPA hydrochloride
DIPPA (hydrochloride) is an irreversible, long-lasting, selective and high affinity κ-opioid receptor antagonist. DIPPA (hydrochloride) can be used for the research of anxiety and antidepressant .

HY-P1335A

CTAP TFA 1 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-163065

σ1 Receptor/μ Opioid receptor modulator 2	Opioid Receptor Sigma Receptor	Neurological Disease
σ1 Receptor/μ Opioid receptor modulator 2 (compound 4x) is a dual μOR agonist/σ1R antagonist, and displays picomolar μOR agonism activity (EC₅₀: 0.6 ± 0.2 nM) and good σ1R inhibitory activity (K_i: 363.7 ± 5.6 nM). σ1 Receptor/μ Opioid receptor modulator 2 exhibits robust analgesic effects in various pain models .

HY-17001

Flupirtine Maleate 1 Publications Verification	Potassium Channel iGluR	Neurological Disease
Flupirtine Maleate is a brain penetrant, and orally bioavailable, non-opioid and centrally acting analgesic agent. Flupirtine Maleate is an indirect N-methyl-D-aspartate receptor (NMDAR) antagonist. Neuroprotective properties .

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-135230

LY2444296 FP3FBZ	Opioid Receptor	Neurological Disease
LY2444296 is an orally bioavailable, high-affinity and selective short-acting *kappa opioid* receptor (KOPR)** antagonist, with a K_i value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects .

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 .

Cat. No.	Product Name	Target	Research Area

HY-P1335A

CTAP TFA 1 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-P10177

Acetalin-3	Opioid Receptor	Neurological Disease
Acetalin-3 (Ac-RFMWMT-NH2), a hexapeptide, is a μ opioid receptor antagonist with high affinity for μ and κ3 opioid receptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .

HY-P10175

Acetalin-1	Opioid Receptor	Neurological Disease
Acetalin-1 (Ac-RFMWMK-NH2), a hexapeptide, is a μ opioid receptor antagonist with high affinity for μ and κ3 opioid receptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .

HY-P1335

CTAP	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-P5892

β-Endorphin (1-27) (human)	Opioid Receptor	Neurological Disease
β-Endorphin (1-27) (human) is an *opioid* antagonist that binds μ-, δ-, and κ-opioid receptors with K_is of 5.31, 6.17, and 39.82 nM, respectively. β-Endorphin (1-27) (human) inhibits β-Endorphin (HY-P1502)-induced and etorphine-induced analgesia .

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-P3839

Nocistatin	Opioid Receptor	Neurological Disease
Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a G_i/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia .

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-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 .

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