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κ-opioid Receptor Agonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) Adenylate Cyclase (2) Apoptosis (5) Autophagy (3) Caspase (2) Dopamine Receptor (3) Drug Isomer (1) Endogenous Metabolite (3) ERK (5) Ferroptosis (3) Histamine Receptor (5) Interleukin Related (1) Isotope-Labeled Compounds (8) mAChR (1) Mas-related G-protein-coupled Receptor (MRGPR) (1) Mitophagy (3) mTOR (2) Opioid Receptor (98) p38 MAPK (5) PINK1/Parkin (3) Protein Arginine Deiminase (1) Reference Standards (5) Sigma Receptor (1) Sodium Channel (1) TNF Receptor (1) Vasopressin Receptor (1)
By Research Areas:	Cancer (5) Cardiovascular Disease (5) Endocrinology (1) Infection (1) Inflammation/Immunology (12) Metabolic Disease (7) Neurological Disease (82)

By Targets:

5-HT Receptor (2)

Adenylate Cyclase (2)

Apoptosis (5)

Autophagy (3)

Caspase (2)

Dopamine Receptor (3)

Drug Isomer (1)

Endogenous Metabolite (3)

ERK (5)

Ferroptosis (3)

Histamine Receptor (5)

Interleukin Related (1)

Isotope-Labeled Compounds (8)

mAChR (1)

Mas-related G-protein-coupled Receptor (MRGPR) (1)

Mitophagy (3)

mTOR (2)

Opioid Receptor (98)

p38 MAPK (5)

PINK1/Parkin (3)

Protein Arginine Deiminase (1)

Reference Standards (5)

Sigma Receptor (1)

Sodium Channel (1)

TNF Receptor (1)

Vasopressin Receptor (1)

By Research Areas:

Cancer (5)

Cardiovascular Disease (5)

Endocrinology (1)

Infection (1)

Inflammation/Immunology (12)

Metabolic Disease (7)

Neurological Disease (82)

102

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Nom du produit	Target	Áreas de investigación	Chemical Structure

HY-N0164

Matrine 15+ Cited Publications Matridin-15-one; Vegard; α-Matrine	PINK1/Parkin Opioid Receptor Autophagy Mitophagy Ferroptosis Apoptosis	Inflammation/Immunology Cancer
Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a **kappa opioid receptor and u-receptor** agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .

HY-110252

Salvinorin B	Opioid Receptor	Neurological Disease Inflammation/Immunology
Salvinorin B is a selective and brain-penetrant kappa opioid receptor (KOPr) agonist with an EC₅₀ of 248 nM and K_i of 2.95 μM. Salvinorin B activates downstream signaling pathways by binding to KOPr, inhibits pain transmission and reduces inflammatory response. Salvinorin B can be used for the researches of inflammation, immunology and neurological disease, such as neuropathic pain, multiple sclerosis and anxiety .

HY-B0188A

Mianserin hydrochloride 1 Publications Verification Org GB 94	Histamine Receptor Opioid Receptor ERK p38 MAPK	Neurological Disease Metabolic Disease
Mianserin hydrochloride (Org GB 94) is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate **κ-opioid receptor** and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy .

HY-17609

Difelikefalin 1 Publications Verification CR-845; FE-202845	Opioid Receptor	Neurological Disease Inflammation/Immunology
Difelikefalin (CR-845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .

HY-10487

JDTic dihydrochloride 3 Publications Verification	Opioid Receptor	Neurological Disease
JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.

HY-P1333

Dynorphin A 1 Publications Verification	Opioid Receptor Apoptosis Caspase Endogenous Metabolite	Neurological Disease
Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .

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-B0188

Mianserin 1 Publications Verification Mianserine	Histamine Receptor Opioid Receptor ERK p38 MAPK	Neurological Disease
Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate **κ-opioid receptor** and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .

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-156131

Loperamide 10+ Cited Publications ADL 2-1294	Opioid Receptor	Neurological Disease Inflammation/Immunology
Loperamide (ADL 2-1294) is selective and orally active μ opioid receptor agonist with K_i valuess of 3, 48 and 1156 nM against μ, δ and κ opioid receptor, respectively. Loperamide produces antinociception and antihyperalgesia. Loperamide exhibits peripheral selectivity, enhancing fluid, electrolyte, and glucose absorption, reversing PGE₂(HY-101952)- and Cholera toxin (HY-P1446)-induced intestinal secretion, and reducing intestinal motility. Loperamide can be used for the researches of inflammatory pain and protracted diarrhoea .

HY-P2159

Dynorphin A (1-8)	Opioid Receptor Endogenous Metabolite	Neurological Disease
Dynorphin A (1-8) is a ligand with preference for the **κ-opioid receptor, and its IC₅₀** value against human placental κ-opioid receptor is 330 nM. Dynorphin A (1-8) mediates neuroprotective effects by inhibiting oxidative stress, suppressing apoptosis, and competitively displacing the binding of κ partial agonists. Dynorphin A (1-8) is the dominant opioid peptide in human placental villi and tissue extracts; it undergoes rapid hydrolysis and can enter the central nervous system via intranasal administration. Dynorphin A (1-8) can be used in studies related to ischemic stroke .

HY-P3445A

Anrikefon acetate HSK21542 acetate	Opioid Receptor	Neurological Disease
Anrikefon (HSK21542) acetate is a kappa opioid receptor agonist with analgesic effect .

HY-100845

Salvinorin A Divinorin A	Opioid Receptor	Cardiovascular Disease
Salvinorin A is a potent, unique and short-acting high efficacy kappa-opioid receptor (KOPr) agonist with K_i value of 4.3 nm. Salvinorin A is a non-nitrogenous neoclerodane isolated from Salvia divinorum.

HY-176710

PAD-PF2	Protein Arginine Deiminase Opioid Receptor mAChR	Neurological Disease Inflammation/Immunology Cancer
PAD-PF2 is a PAD family inhibitor, as well as a κ-opioid receptor agonist (EC₅₀ = 7.55 μM) and an M1 muscarinic acetylcholine receptor antagonist (IC₅₀ = 12.3 μM). The IC₅₀ values of PAD-PF2 against PAD1, PAD2, PAD3 and PAD4 are 109 nM, 27.9 nM, 106 nM and 20.1 nM, respectively. PAD-PF2 binds to the common allosteric pocket of PAD1-4, and its inhibitory effects on PAD2 and PAD4 are Ca ²⁺-dependent. PAD-PF2 inhibits protein citrullination in neutrophils. PAD-PF2 is applicable to research related to rheumatoid arthritis, neurodegenerative diseases and cancer .

HY-130118

MRGPRX1 agonist 1	Mas-related G-protein-coupled Receptor (MRGPR)	Neurological Disease
MRGPRX1 agonist 1 is a highly potent MRGPRX1 agonist (EC₅₀=50 nM) with greater than 50-fold selectivity for δ, μ, and κ opioid receptors. MRGPRX1 agonist 1 is inactive against MRGPRC11. MRGPRC11 inhibits high voltage-activated (HVA) Ca ²⁺ currents, reduces neurotransmitter release, and mitigates nociceptive transmission in the spinal cord. MRGPRX1 agonist 1 is useful for the study of chronic pain, especially neuropathic pain .

HY-P3609

CR 665 2 Publications Verification JNJ 38488502; FE 200665	Opioid Receptor	Neurological Disease
CR 665 (JNJ 38488502) is a peripherally selective *κ-opioid* agonist. CR 665 can activate the kappa opioid receptor with EC₅₀ value of 10.9 nM. CR 665 can be used for the research of peripheral pain .

HY-P3445

Anrikefon HSK21542	Opioid Receptor	Neurological Disease
Anrikefon (HSK21542) is a kappa opioid receptor agonist with analgesic effect .

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. Samidorphan can improve the behavior of depressed animals .

HY-P0088

Porcine dynorphin A(1-13) Dynorphin A Porcine Fragment 1-13	Opioid Receptor	Others
Porcine dynorphin A (1-13) is a potent, endogenous **κ opioid receptor** agonist and is antinociceptive at physiological concentrations.

HY-101205

ICI-199441 hydrochloride	Opioid Receptor	Cardiovascular Disease Neurological Disease
ICI-199441 hydrochloride is a potent and selective *κ-opioid* receptor agonist with analgesic effects. ICI 199441 hydrochloride can improve heart resistance to ischemia/reperfusion .

HY-101079

BRL 52537 hydrochloride	Opioid Receptor	Neurological Disease
BRL 52537 hydrochloride is a highly selective κ-Opioid receptor (KOR) agonist with K_is of 0.24 nM and 1560 nM for κ and μ subtypes, respectively. BRL 52537 hydrochloride decreases ischemia-evoked NO production as a potential mechanism of neuroprotection. BRL 52537 hydrochloride attenuates early stroke damage .

HY-15997B

(±)-U-50488 hydrochloride (±)-Trans-(1R,2R)-U-50488 hydrochloride	Opioid Receptor	Neurological Disease
(±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrochloride is a selective κ opioid receptor (KOR) agonist .

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-110302

6'-GNTI dihydrochloride	Opioid Receptor	Neurological Disease
6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons .

HY-121800

ML138	Opioid Receptor	Others
ML138, a **κ opioid receptor** agonist, is a MLPCN probe .

HY-B0188AR

Mianserin hydrochloride (Standard) Org GB 94 (Standard)	Reference Standards Histamine Receptor Opioid Receptor ERK p38 MAPK	Neurological Disease Metabolic Disease
Mianserin hydrochloride (Org GB 94) (Standard) is the analytical standard of Mianserin hydrochloride. This product is intended for research and analytical applications. Mianserin hydrochloride is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate **κ-opioid receptor** and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy .

HY-B0188S

Mianserin-d3 Mianserine-d₃	Histamine Receptor Isotope-Labeled Compounds Opioid Receptor ERK p38 MAPK	Neurological Disease
Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate **κ-opioid receptor** and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .

HY-19231

DPI-3290 Org 41793	Opioid Receptor	Neurological Disease
DPI-3290 (Org 41793) is a potent and specific **opioid receptors** agonist with K_i values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively. DPI-3290 is one of a series of novel centrally acting agents with potent antinociceptive activity .

HY-10486

JDTic	Opioid Receptor	Neurological Disease
JDTic is a blood-brain barrier-permeable **κ-opioid receptor antagonist (K_i*=0.02 nM) with favorable in vitro ADME properties. JDTic blocks agonist*-mediated Gi and β-arrestin signaling pathways as well as analgesic effects by stabilizing the inactive conformation of hKOR and activating JNK. JDTic may also induce transient asymptomatic ventricular tachycardia. JDTic is widely applicable to studies related to depression, anxiety, stress-induced addictive behaviors, and nicotine withdrawal .

HY-15997C

(±)-U-50488 hydrate hydrochloride (±)-Trans-(1R,2R)-U-50488 hydrate hydrochloride	Opioid Receptor	Neurological Disease
(±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrate hydrochloride is a selective κ opioid receptor (KOR) agonist .

HY-105235

Enadoline CI-977	Opioid Receptor	Neurological Disease
Enadoline (CI-977) is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (K_i=1.25 nM). Antinociceptive effects .

HY-120949

(1R,2R)-U-50488 hydrochloride	Opioid Receptor	Neurological Disease
(1R,2R)-U-50488 hydrochloride is the absolute stereochemistry of (±)-U-50488 hydrochloride. (±)-U-50488 hydrochloride is a selective κ opioid receptor (KOR) agonist .

HY-106756

Spiradoline U-62066	Opioid Receptor	Neurological Disease
Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a K_i of 8.6 nM in guinea pig. The K_i values of Spiradoline for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier .

HY-170973

KOR agonist 4	Opioid Receptor
KOR agonist 4 (compound 39) is an agonist of **Kappa Opioid Receptor*. KOR agonist* 4 is an activator of G-protein signaling. KOR agonist 4 binds with GTPγS with an EC₅₀ of 14 nM and with an E_max of 83 %. KOR agonist 4 demonstrates moderate to high intrinsic clearance in human hepatocytes. KOR agonist 4 exhibits 60- and 810-fold selectivities versus the related mu (MOR) and delta (DOR) opioid receptors. KOR agonist 4 is potential for central nervous system (CNS) disorders research .

HY-17609S1

Difelikefalin-d5 hydrochloride CR-845-d5 hydrochloride; FE-202845-d5 hydrochloride	Isotope-Labeled Compounds Opioid Receptor	Neurological Disease Inflammation/Immunology
Difelikefalin-d₅ (CR-845-d₅) hydrochloride is the deuterium labeled Difelikefalin (HY-17609). Difelikefalin (CR-845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .

HY-163017

NP-5497-KA	Opioid Receptor	Neurological Disease
NP-5497-KA is a *κ-opioid* receptor agonist. NP-5497-KA has orally activity[1].

HY-145128

GR103545 fumarate	Opioid Receptor	Neurological Disease
GR103545 is a potent and selective agonist of the κ-opioid receptor (κ-OR). ¹¹GR103545 is a radiotracer for imaging κ-OR in vivo ^[1]

HY-B0188AS

Mianserin-d3 hydrochloride Org GB 94-d₃	Isotope-Labeled Compounds Histamine Receptor Opioid Receptor ERK p38 MAPK	Neurological Disease Metabolic Disease
Mianserin-d₃ hydrochloride is the deuterium labeled Mianserin. Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate **κ-opioid receptor** and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .

HY-106605

Flumezapine LY 120363	Dopamine Receptor 5-HT Receptor	Neurological Disease
Flumezapine (LY 120363) is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine can be used in antipsychotic research .

HY-123689S1

Samidorphan-d5 ALKS-33-d₅; RDC-0313-d₅	Isotope-Labeled Compounds Opioid Receptor	Neurological Disease
Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound of Samidorphan. Samidorphan is an orally active *opioid* system modulator that binds with high affinity to *μ-opioid, κ-opioid, and δ-opioid* receptors. Samidorphan is a *μ-opioid* receptor antagonist and a partial agonist at *k-opioid* and *δ-opioid* receptors. Samidorphan acts primarily as an *opioid* receptor antagonist in vivo .

HY-108043

AZD-2327	Opioid Receptor	Neurological Disease
AZD-2327 is a potent and selective δ-opioid receptor agonist. AZD-2327 binds to the human opioid receptor (K_i of 0.49 and 0.75 nM and EC₅₀ of 24 and 9.2 nM at the C27 and F27 isoforms, respectively). AZD-2327 shows selectivity of >1000-fold over the human μ- and κ-opioid receptor subtypes as well as >130 other receptors and channels. AZD-2327 exhibits antidepressant and anxiolytic activities and can be used for the research of neurological disease .

HY-178945

KOR agonist 7	Opioid Receptor Interleukin Related TNF Receptor Sigma Receptor	Neurological Disease Inflammation/Immunology
KOR agonist 7 (Compound 29) is a highly selective **κ-opioid receptor (KOR*) agonist* with a K_i of 138 nM. KOR agonist 7 shows no activity at μ- and δ-opioid receptors or σ1 receptor, and exhibits extremely low affinity for σ2 receptor (K_i = 2.8 μM). KOR agonist 7 significantly reduces the secretion of pro-inflammatory cytokines such as IL-6, TNF-α, and IFN-γ, while increasing the production of the anti-inflammatory cytokine IL-10. KOR agonist 7 downregulates the expression of the pro-inflammatory M1 macrophage marker CD80 and upregulates the anti-inflammatory M2 macrophage marker CD163. KOR agonist 7 holds potential for applications in analgesia and immune modulation .

HY-136786

RU-24213 hydrochloride	Dopamine Receptor Opioid Receptor	Neurological Disease
RU-24213 hydrochloride is a selective D-2 dopamine receptor agonist. RU-24213 hydrochloride is also a *KAPPA-opioid* receptor antagonist. RU-24213 hydrochloride induces stereotyped behaviors .

HY-171236

FEKAP	Opioid Receptor
FEKAP is a brain-penetrant and selective kappa opioid receptor (KOR) agonist (K_i = 0.43 nM) which isotope labeled form exhibits excellent imaging properties. ¹¹C-FEKAP can be utilized as a radiotracer for imaging KOR .

HY-124959

Spiradoline mesylate U-62066 mesylate	Opioid Receptor	Neurological Disease
Spiradoline mesylate (U-62066 mesylate), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a K_i of 8.6 nM in guinea pig. The K_i values of Spiradoline mesylate for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline mesylate has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier .

HY-163277

PIPE-3297	Opioid Receptor	Inflammation/Immunology
PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC₅₀ of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity .

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-17609S

Difelikefalin-d5 CR-845-d₅; FE-202845-d₅	Isotope-Labeled Compounds Opioid Receptor	Neurological Disease
Difelikefalin-d₅ (CR-845-d₅) is deuterium labeled Difelikefalin. Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .

HY-135698

Methocinnamox M-CAM	Opioid Receptor	Neurological Disease
Methocinnamox (M-CAM) a selective and long-acting μ-opioid receptor (MOR) antagonist with a K_i of 0.6 nM. Methocinnamox binds to the orthosteric site of the MOR in a pseudo-irreversible, non-covalent manner, resulting in prolonged receptor blockade that persists until new receptors are synthesized. Methocinnamox acts as a reversible antagonist at both the kappa-opioid receptor (KOR) (K_i = 4.9 nM) and delta-opioid receptor (DOR) (K_i = 2.2 nM), and it exhibits no intrinsic agonist activity at these receptors. Methocinnamox can be used to reverse and prevent opioid overdose and addiction .

Cat. No.	Nom du produit	Target	Research Area

HY-17609

Difelikefalin 1 Publications Verification CR-845; FE-202845	Opioid Receptor	Neurological Disease Inflammation/Immunology
Difelikefalin (CR-845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .

HY-P1333

Dynorphin A 1 Publications Verification	Opioid Receptor Apoptosis Caspase Endogenous Metabolite	Neurological Disease
Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .

HY-P2159

Dynorphin A (1-8)	Opioid Receptor Endogenous Metabolite	Neurological Disease
Dynorphin A (1-8) is a ligand with preference for the **κ-opioid receptor, and its IC₅₀** value against human placental κ-opioid receptor is 330 nM. Dynorphin A (1-8) mediates neuroprotective effects by inhibiting oxidative stress, suppressing apoptosis, and competitively displacing the binding of κ partial agonists. Dynorphin A (1-8) is the dominant opioid peptide in human placental villi and tissue extracts; it undergoes rapid hydrolysis and can enter the central nervous system via intranasal administration. Dynorphin A (1-8) can be used in studies related to ischemic stroke .

HY-P3445A

Anrikefon acetate HSK21542 acetate	Opioid Receptor	Neurological Disease
Anrikefon (HSK21542) acetate is a kappa opioid receptor agonist with analgesic effect .

HY-P3609

CR 665 2 Publications Verification JNJ 38488502; FE 200665	Opioid Receptor	Neurological Disease
CR 665 (JNJ 38488502) is a peripherally selective *κ-opioid* agonist. CR 665 can activate the kappa opioid receptor with EC₅₀ value of 10.9 nM. CR 665 can be used for the research of peripheral pain .

HY-P3445

Anrikefon HSK21542	Opioid Receptor	Neurological Disease
Anrikefon (HSK21542) is a kappa opioid receptor agonist with analgesic effect .

HY-P0088

Porcine dynorphin A(1-13) Dynorphin A Porcine Fragment 1-13	Opioid Receptor	Others
Porcine dynorphin A (1-13) is a potent, endogenous **κ opioid receptor** agonist and is antinociceptive at physiological concentrations.

HY-P3647

[DPro10] Dynorphin A (1-11), porcine	Opioid Receptor Adenylate Cyclase	Neurological Disease
[DPro10] Dynorphin A (1-11), porcine, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a K_i value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine has analgesic property .

HY-P3647A

[DPro10] Dynorphin A (1-11), porcine hydrochloride	Opioid Receptor Adenylate Cyclase	Neurological Disease
[DPro10] Dynorphin A (1-11), porcine hydrochloride, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a K_i value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine hydrochloride has analgesic property .

HY-P3376

Riminkefon	Opioid Receptor	Neurological Disease
Riminkefon is a **kappa opioid receptor** agonist .

HY-P10006

Leumorphin, human	Opioid Receptor	Neurological Disease
Leumorphin, human is a potent **kappa opioid receptor (κ opioid receptor)** agonist. Leumorphin, human inhibits the contraction of the myenteric plexus-longitudinal muscle preparation of the guinea pig ileum .

HY-P10203

*μ/κ/δ opioid* receptor agonist 1**	Opioid Receptor	Inflammation/Immunology
μ/κ/δ opioid receptor agonist 1 is a μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR) agonist. μ/κ/δ opioid receptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .

HY-P1333A

Dynorphin A TFA	Opioid Receptor Apoptosis Caspase Endogenous Metabolite	Neurological Disease
Dynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease .

HY-P3634

[DAla2] Dynorphin A (1-13), amide (porcine)	Opioid Receptor	Neurological Disease
[DAla2] Dynorphin A (1-13), amide (porcine) is a petide. [DAla2] Dynorphin A (1-13), amide (porcine) might have the κ opioid receptor agonist effect. [DAla2] Dynorphin A (1-13), amide (porcine) can be used for the research of nervous system .

HY-P1625

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

HY-P4679

(N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8) E2078	Opioid Receptor	Neurological Disease
(N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8) (E-2078), a stable Dynorphin A (1–8) (HY-P2159) analog, is a kappa opioid receptor (KOR) agonist .

Cat. No.	Nom du produit	Category	Target	Chemical Structure

HY-N0164

Matrine 15+ Cited Publications Matridin-15-one; Vegard; α-Matrine	Alkaloids Piperidine Alkaloids Classification of Application Fields Leguminosae Sophora flavescens Aiton Plants Inflammation/Immunology Disease Research Fields Biological Pesticide Research Source Classification Cancer Agricultural Research	PINK1/Parkin Opioid Receptor Autophagy Mitophagy Ferroptosis Apoptosis
Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a **kappa opioid receptor and u-receptor** agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .

HY-110252

Salvinorin B	Terpenoids Labiatae Encelia stenophylla Greene Diterpenoids Plants Source Classification	Opioid Receptor
Salvinorin B is a selective and brain-penetrant kappa opioid receptor (KOPr) agonist with an EC₅₀ of 248 nM and K_i of 2.95 μM. Salvinorin B activates downstream signaling pathways by binding to KOPr, inhibits pain transmission and reduces inflammatory response. Salvinorin B can be used for the researches of inflammation, immunology and neurological disease, such as neuropathic pain, multiple sclerosis and anxiety .

HY-B0188A

Mianserin hydrochloride 1 Publications Verification Org GB 94	Alkaloids Structural Classification Neurological Disease Classification of Application Fields Leguminosae Other Alkaloids Crotalaria pallida Ait. Plants Disease Research Fields Endocrinology Source Classification	Histamine Receptor Opioid Receptor ERK p38 MAPK
Mianserin hydrochloride (Org GB 94) is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate **κ-opioid receptor** and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy .

HY-P2159

Dynorphin A (1-8)	Structural Classification Productos naturales Neurological Disease Classification of Application Fields Endogenous metabolite Disease Research Fields Source Classification	Opioid Receptor Endogenous Metabolite
Dynorphin A (1-8) is a ligand with preference for the **κ-opioid receptor, and its IC₅₀** value against human placental κ-opioid receptor is 330 nM. Dynorphin A (1-8) mediates neuroprotective effects by inhibiting oxidative stress, suppressing apoptosis, and competitively displacing the binding of κ partial agonists. Dynorphin A (1-8) is the dominant opioid peptide in human placental villi and tissue extracts; it undergoes rapid hydrolysis and can enter the central nervous system via intranasal administration. Dynorphin A (1-8) can be used in studies related to ischemic stroke .

HY-100845

Salvinorin A Divinorin A	Terpenoids Labiatae Diterpenoids Plants Vachellia nilotica (L.) P. J. H. Hurter & Mabb. Source Classification	Opioid Receptor
Salvinorin A is a potent, unique and short-acting high efficacy kappa-opioid receptor (KOPr) agonist with K_i value of 4.3 nm. Salvinorin A is a non-nitrogenous neoclerodane isolated from Salvia divinorum.

HY-B0188AR

Mianserin hydrochloride (Standard) Org GB 94 (Standard)	Alkaloids Structural Classification Leguminosae Other Alkaloids Crotalaria pallida Ait. Plants Source Classification	Reference Standards Histamine Receptor Opioid Receptor ERK p38 MAPK
Mianserin hydrochloride (Org GB 94) (Standard) is the analytical standard of Mianserin hydrochloride. This product is intended for research and analytical applications. Mianserin hydrochloride is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate **κ-opioid receptor** and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy .

HY-N0164R

Matrine (Standard) Matridin-15-one (Standard); Vegard (Standard); α-Matrine (Standard)	Alkaloids Piperidine Alkaloids Structural Classification Leguminosae Sophora flavescens Aiton Plants Source Classification	PINK1/Parkin Reference Standards Opioid Receptor Autophagy Mitophagy Ferroptosis Apoptosis
Matrine (Standard) is the analytical standard of Matrine. This product is intended for research and analytical applications. Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .

Cat. No.	Nom du produit	Chemical Structure

HY-B0188S

Mianserin-d3

Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .

HY-17609S1

Difelikefalin-d5 hydrochloride
Difelikefalin-d₅ (CR-845-d₅) hydrochloride is the deuterium labeled Difelikefalin (HY-17609). Difelikefalin (CR-845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .

HY-B0188AS

Mianserin-d3 hydrochloride

Mianserin-d₃ hydrochloride is the deuterium labeled Mianserin. Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .

HY-123689S1

Samidorphan-d5

Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioid receptors. Samidorphan is a μ-opioid receptor antagonist and a partial agonist at k-opioid and δ-opioid receptors. Samidorphan acts primarily as an opioid receptor antagonist in vivo .

HY-17609S

Difelikefalin-d5
Difelikefalin-d₅ (CR-845-d₅) is deuterium labeled Difelikefalin. Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .

HY-W654256

Matrine-d3

Matrine-d₃ (Matridin-d₃) is a deuterium labeled Matrine (HY-N0164). Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .

HY-123689S

Samidorphan-d4

Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).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-106605S

Flumezapine-d8 hydrochloride

Flumezapine-d₈ (LY 120363-d₈) hydrochloride is deuterated labeled Flumezapine hydrochloride. Flumezapine hydrochloride is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine hydrochloride does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine hydrochloride inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine hydrochloride can be used in antipsychotic research.

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