Opioid Receptor Inhibitor

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.

(-)-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).

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.

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).

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.

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.

β-Chlornaltrexamine dihydrochloride (β-CNA dihydrochloride) is a potent long-term opioid receptor blocker. β-Chlornaltrexamine dihydrochloride can effectively block the inhibitory effect of κ opioid receptor agonists on dopamine release. β-Chlornaltrexamine dihydrochloride can be used to study the mechanism of pain perception.

Bisacodyl (Standard) is the analytical standard of Bisacodyl. This product is intended for research and analytical applications. 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.