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opioid dependence

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By Targets:	Opioid Receptor (12) Adrenergic Receptor (1) Apoptosis (2) Imidazoline Receptor (1) NF-κB (2) NO Synthase (2) p38 MAPK (2) Phospholipase (1) Reactive Oxygen Species (ROS) (2) Reference Standards (1) Toll-like Receptor (TLR) (2)
By Research Areas:	Cardiovascular Disease (2) Inflammation/Immunology (3) Metabolic Disease (2) Neurological Disease (11)

Targets Recommended: Opioid Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-107744

Nalmefene 1 Publications Verification	Opioid Receptor Apoptosis Reactive Oxygen Species (ROS) NO Synthase Toll-like Receptor (TLR) p38 MAPK NF-κB	Cardiovascular Disease Neurological Disease Inflammation/Immunology
Nalmefene is a BBB-penetrable opioid receptor modulator. Nalmefene is an antagonist of MOR and DOR, and a partial agonist of KOR. Nalmefene has anti-inflammatory and neuroprotective activities. Nalmefene can be used in the research of reducing alcohol-dependent disorders .

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-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-B1485

Nalmefene hydrochloride	Opioid Receptor	Neurological Disease
Nalmefene hydrochloride is a long acting opioid (MOR and DOR antagonist), and a partial KOR agonist. Nalmefene hydrochloride is used for opioid overdose and alcohol dependence .

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-171758

BU72	Opioid Receptor	Neurological Disease
BU72 is a highly potent and long-acting agonist of *μ and κ opioid* receptors*, and also has a partial agonist effect on δ opioid* receptors (EC₅₀ values are 0.054, 0.033, and 0.58 nM, respectively). BU72 has a strong and long-lasting analgesic effect, which is mainly mediated by μ opioid receptors. BU72 has a long-lasting activity and can partially reverse the analgesic effect of morphine. BU72 can be used in the study of opioid dependence .

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-107744R

Nalmefene (Standard)	Opioid Receptor Apoptosis Reactive Oxygen Species (ROS) NO Synthase Toll-like Receptor (TLR) p38 MAPK NF-κB Reference Standards	Cardiovascular Disease Neurological Disease Inflammation/Immunology
Nalmefene (Standard) is the analytical standard of Nalmefene. This product is intended for research and analytical applications. Nalmefene is a long acting opioid (MOR and DOR antagonist), and a partial KOR agonist. Nalmefene is used for opioid overdose and alcohol dependence .

HY-136654

LPK-26 hydrochloride	Opioid Receptor	Neurological Disease
LPK-26 hydrochloride is a selective *kappa-opioid* receptor agonist with a K_i** of 0.68 nM. LPK-26 exhibits potent antinociceptive effects with low physical dependence potential and can be utilized in relevant research .

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-11051

JNJ-20788560	Opioid Receptor	Inflammation/Immunology
JNJ-20788560 is a selective and orally active delta opioid receptor agonist with an affinity of 2.0 nM for DOR (rat brain cortex binding assay). JNJ-20788560 also is a potent and efficacious antihyperalgesic agent that does not produce respiratory depression, pharmacologic tolerance, or physical dependence. JNJ-20788560 can be used for the research of the relief of inflammatory hyperalgesia .

HY-159924

DBPR116	Opioid Receptor	Neurological Disease
DBPR116 is a prodrug of BPRMU191 (HY-159923) with blood-brain barrier penetration capability. DBPR116 significantly improves the delivery of centrally targeted drugs. In combination with the antagonist Naltrexone (HY-76711), DBPR116 demonstrated superior safety and analgesic efficacy compared to morphine in various in vivo pharmacological studies, including thermal pain models, cancer pain models, constipation, sedation, psychological dependence, heart rate, and respiratory frequency. As a prodrug strategy for peripheral administration, DBPR116 effectively alleviates pain while reducing adverse effects, showing potential as a safer opioid analgesic .

HY-177218

M119 NSC 119910	Phospholipase Opioid Receptor	Neurological Disease
M119 (NSC 119910) is a selective Gβγ-subunit inhibitor. M119 selectively potentiates *μ-opioid*-dependent antinociception. M119 inhibits μ-receptor-dependent phospholipase (PLC) activation. M119 can enhance opioid analgesia and attenuate its acute tolerance and dependence in mice. M119 can be used for pain research .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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opioid dependence

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