Opioid Receptor Activator

Helianorphin-19 is a potent and selective κ-opioid receptor (KOR) activator with a K_i of 21 nM and an EC₅₀ of 45 nM. Helianorphin-19 exhibits strong KOR-specific peripheral analgesic activity in a mouse model of chronic visceral pain.

Cyclosomatostatin TFA is a non-selective somatostatin receptor antagonist that blocks SSTR1-5-mediated signaling. Cyclosomatostatin TFA decreases the ALDH⁺ stem cell population and sphere formation without affecting cell viability, and reduces cell proliferation. Cyclosomatostatin TFA activates opioid receptors. Cyclosomatostatin TFA can be used for research on arthritis and colorectal cancer.

M119 (NSC 119910) is a Gβγ subunit and PLCβ3 inhibitor with selective activity toward μ-opioid receptor-related pathways. M119 selectively inhibits Gβγ-dependent PLCβ3 activation, reduces inositol phosphate production, and enhances μ-opioid receptor-mediated antinociception. M119 attenuates acute μ-opioid receptor agonist-induced antinociceptive tolerance and physical dependence in mice. M119 can be used for pain-related research.

Bromadoline maleate is an opioid analgesic selective for the μ-opioid receptor, exhibiting analgesic activity in various biological fluids. Bromadoline maleate has been successfully quantified alongside its N-demethylated metabolites in human and canine samples.

Ro-48-6791 is a compound that may have the activity of activating opioid receptors. Computational studies have found that it may bind to and activate opioid receptors, and may mediate or increase their related physiological effects and side effects.

(±)-Leucine (Standard) is the analytical standard of (±)-Leucine. This product is intended for research and analytical applications. (±)-Leucine (DL-Leucine), an isomer of Leucine, chemosterilant and dietary additive. (±)-Leucine inhibits growth of Escherichia coli HfrH by 92.08%.

Sinomenine hydrochloride (Standard) is the analytical standard of Sinomenine hydrochloride. This product is intended for research and analytical applications. Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.

BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC₅₀ of 101 nM and a pEC₅₀ of 6.99. BAM-12P is a ligand for CXCR7 with an EC₅₀ of 175 nM.

Azo-enkephalin is an endorphin analog with significant analgesic activity. Azo-enkephalin can be used in the development of opioid analgesics.

1-Naphthyl U-47700 is an α-isomer. 1-Naphthyl U-47700 is a racemic mixtures of the trans-isomers [R,R and S,S]. 1-Naphthyl U-47700 activates MOR in a concentration-dependent manner (EC₅₀ > 23 μM).