Opioid Receptor Inhibitor

Harmane is a benzodiazepine receptor inhibitor (IC₅₀=7 μM), with IC₅₀ values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC₅₀ = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).

Bisacodyl is a stimulant laxative agent that works directly on the colon to produce a bowel movement. Bisacodyl increases the secretion of PGE₂ by direct activation of colon macrophages. PGE₂ acts as a paracrine factor and decreases the expression of AQP3 in the colon, which inhibits water transfer from the luminal to the vascular side and leads to a laxative effect.

SB-612111 hydrochloride hydrochloride is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (K_i=0.33 nM). SB-612111 hydrochloride exhibits selectivity for μ-,?κ- and?δ-receptors with K_i values of?57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model.

Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC₅₀ values of 0.8 nM, 110 nM, and 6500 nM, respectively. Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy.

(-)-U-50488 hydrochloride ((-)-Trans-(1S,2S)-U-50488 hydrochloride) is a selective kappa-opioid receptor (KOR) agonist (K_d=2.2 nM) over μ-opioid receptor (MOR) (K_d=430 nM). (-)-U-50488 hydrochloride is a more active enantiomer than (+) trans-(1R,2R) U-50488 (HY-15997A) or the (±) trans-racemic mixture U-50488 (HY-15997B). (-)-U-50488 hydrochloride has a potent and sustained anti-HIV effect in fected blood monocyte-derived macrophages (MDM).

Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioid receptor, with analgesic effect.

CCG258747 is a selective GRK2 inhibitor (IC₅₀ = 18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, > 5500, and > 550-fold, respectively). CCG258747 also blocks the internalization of the µ-opioid receptor (MOR). CCG258747 attenuates IgE mediated anaphylaxis by inhibiting GRK2 and FcεRI signaling pathway but activates mast cells via MRGPRX2 and MRGPRB2. CCG258747 can be used to study diseases related to overexpression of GRK2 (such as heart failure, opioid tolerance).

Harmane hydrochloride is a benzodiazepine receptor inhibitor (IC₅₀=7 μM), with IC₅₀ values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane hydrochloride inhibits the I1 imidazoline receptor (IC₅₀ = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane hydrochloride inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane hydrochloride can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).

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.

Gluten exorphin C is an opioid peptide derived from wheat gluten. Its IC₅₀ values are 40 μM and 13.5 μM for μ opioid and δ opioid activities in the GPI and MVD assays, respectively.

6-Hydroxyflavanone is a compound that can be isolated from the Muntingia calabura leaves. 6-Hydroxyflavanone targets cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), and opioid and GABA-A receptors that has anti-inflammatory and anti-neuropathic pain potential. 6-Hydroxyflavanone can be used for the research of diabetes.

Harman-¹³C₂,¹⁵N is ¹³C and ¹⁵N labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC₅₀=7 μM), with IC₅₀ values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC₅₀ values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC₅₀=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).

SB-612111 is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (K_i=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with K_i values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model.

Urotensin-II receptor antagonist-1 (compound 1) is a low oral bioavailability (F=0-3%, rat) selective human Urotensin II receptor antagonist, K_i=16 nM (test on HEK293 cells expressing recombinant human UT receptor). Urotensin-II receptor antagonist-1 inhibits cytochrome P450 (IC₅₀=0.75 μM, CYP2D6; 1.4 μM, CYP3A4), inhibits κ-opioid receptor (EC₅₀=3.2 μM), targets cardiac sodium channels (K_i=2.5 μM).

(-)-P7C3-S243 is an orally active, blood-brain barrier permeable neuroprotective agent. (-)-P7C3-S243 binds to μ-opioid Receptor and TSPO. (-)-P7C3-S243 inhibits the premature apoptosis death of newborn hippocampal neurons, protects mature nigral dopaminergic neurons, promotes neuronal survival and prevents cognitive impairment. (-)-P7C3-S243 ameliorates depression-like behaviors in rat models. (-)-P7C3-S243 is applicable to research related to Parkinson's disease and Alzheimer's disease.

Neuropeptide AF (human) is an endogenous antiopioid peptide.

rel-SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (K_i=0.33 nM). rel-SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with K_i values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. rel-SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model.

Akuammidine, isolated from the seeds of Picralima nitida, shows a preference for μ-opioid binding sites with K_i values of 0.6, 2.4 and 8.6 μM at μ-, σ- and κ-opioid binding sites, respectively. Akuammidine possesses anti-inflammatory and anti-asthmatic properties.

Sec-O-Glucosylhamaudol (Standard) is the analytical standard of Sec-O-Glucosylhamaudol. This product is intended for research and analytical applications. Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioid receptor, with analgesic effect.

Doxpicomine is an analgesic with potent activity, effective in treating severe postoperative pain.