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Opioid withdrawal

" in MedChemExpress (MCE) Product Catalog:

25

Inhibitors & Agonists

2

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • 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 .
    Norbinaltorphimine dihydrochloride
  • 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 .
    nor-Binaltorphimine
  • 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 .
    Lofexidine hydrochloride
  • 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 .
    Dapiprazole hydrochloride
  • 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 .
    CYM51010
  • 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 .
    Lofexidine
  • 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 .
    EG-2184
  • 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 .
    PF-04455242
  • 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 .
    Dapiprazole
  • 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 .
    MDAN-21
  • 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 .
    Lofexidine-d4 hydrochloride
  • 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 Ki 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) .
    Mu opioid receptor antagonist 4
  • 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 Ki 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) .
    Mu opioid receptor antagonist 2
  • HY-151811
    NAQ

    		Opioid Receptor Neurological Disease
    NAQ is a potent and selective μ opioid receptor partial agonist, with a Ki of 0.55 nM. NAQ shows selectivity for Mu opioid receptor over the δ receptor (Ki=132.50 nM) and the κ receptor (Ki=26.45 nM). NAQ can be used for the research of opioid withdrawal or dependence .
    NAQ
  • 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.
    Akuammine
  • 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 .
    Dapiprazole hydrochloride (Standard)
  • 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 Ki 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) .
    Mu opioid receptor antagonist 3
  • HY-117881
    CJ-15208

    		Opioid Receptor Neurological Disease
    CJ-15208 is a potent and selective κ-opioid receptor antagonist with significant opioid activity. CJ-15208 exhibited strong analgesic effects in the warm water tail withdrawal test in mice and was mediated through multiple opioid receptors. The stereoisomers of CJ-15208 exhibited different opioid activity characteristics, for example, one stereoisomer exhibited κ-opioid receptor antagonism, while the other exhibited δ-opioid receptor antagonism. All stereoisomers of CJ-15208 had no significant effects on respiration. The stereoisomers of CJ-15208 did not lead to the development of drug tolerance, which makes it potential in the further development of safe opioid analgesics .
    CJ-15208
  • HY-B1052R
    Lofexidine hydrochloride (Standard)

    Baq-168 (Standard); MDL-14042 (Standard)

    		 Adrenergic Receptor Reference Standards Neurological Disease Metabolic Disease
    Lofexidine (Baq-168) hydrochloride Standard is the analytical standard of Lofexidine hydrochloride (HY-B1052). This product is intended for research and analytical applications. 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 .
    Lofexidine hydrochloride (Standard)
  • HY-B1052S1
    Lofexidine-d4

    Baq-168 free base-d4; MDL-14042 free base-d4

    		 Isotope-Labeled Compounds Imidazoline Receptor Adrenergic Receptor Neurological Disease Metabolic Disease
    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 .
    Lofexidine-d4
  • 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 Kis of 0.25, 41.1, 1.30 nM, respectively[1]
    MOR modulator-1
  • HY-15691A
    PF-4455242 hydrochloride

    		Opioid Receptor mTOR Neurological Disease Metabolic Disease
    PF-4455242 hydrochloride is an orally bioavailable, blood-brain barrier-permeable κ-opioid receptor (KOR) inhibitor. PF-4455242 hydrochloride blocks in vivo effects induced by KOR and MOR agonists, and elicits KOR-independent outward currents in ventral tegmental area neurons. PF-4455242 hydrochloride promotes energy expenditure and activates the hypothalamic mTOR pathway. PF-4455242 hydrochloride attenuates stress-induced behavioral effects and produces antidepressant-like effects. PF-4455242 hydrochloride can be used in studies related to pain, depression, addictive disorders, and obesity induced by estrogen withdrawal .
    PF-4455242 hydrochloride
  • HY-181605
    MOR antagonist 2 hydrochloride

    		Opioid Receptor Neurological Disease
    MOR antagonist 2 hydrochloride is a blood-brain barrier-permeable μ-opioid receptor (MOR) antagonist, with an IC50 of 28.37 nM, an EC50 of 4.25 nM, and a Ki of 0.18 nM against MOR. MOR antagonist 2 hydrochloride stabilizes the inactive conformation of MOR to reduce receptor activation levels. MOR antagonist 2 hydrochloride antagonizes analgesic effects in the mouse warm-water tail-flick test. MOR antagonist 2 hydrochloride induces fewer opioid withdrawal symptoms (wet dog shakes, paw tremors) in mice with opioid withdrawal symptoms. MOR antagonist 2 hydrochloride can be used for the research of opioid use disorder .
    MOR antagonist 2 hydrochloride
  • HY-100903R
    Norbinaltorphimine dihydrochloride (Standard)

    nor-Binaltorphimine dihydrochloride (Standard); nor-BNI dihydrochloride (Standard)

    		 Opioid Receptor Reference Standards Neurological Disease
    Norbinaltorphimine dihydrochloride (Standard) is the analytical standard of Norbinaltorphimine dihydrochloride (HY-100903). This product is intended for research and analytical applications. 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 .
    Norbinaltorphimine dihydrochloride (Standard)
  • HY-104006R
    CYM51010 (Standard)

    		Reference Standards Opioid Receptor Neurological Disease
    CYM51010 (Standard) is the analytical standard of CYM51010 (HY-104006). This product is intended for research and analytical applications. 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 .
    CYM51010 (Standard)

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