Mu opioid receptor antagonist

Devine DP, Leone P, Wise RA. (1993). Mesolimbic dopamine neurotransmission is increased by administration of mu-opioid receptor antagonists. EurJ Pharmacol. 243(1) 55-64. 

Goodman AJ, Le Bourdonnec B, Dolle RE (2007) Mu opioid receptor antagonists recent developments. Chem Med Chem 2 1552-1557... 

McLaughlin JP, Sebastian A, Archer S, Bidlack JM (1997) 14 Beta-chlorocinnamoylamino derivatives of metopon long-term mu-opioid receptor antagonists. Eur J Pharmacol 320 121-129... 

The compound lobeline has been shown to have a high affinity for nicotinic acetylcholine receptors and inhibits the function of vesicular monoamine and dopamine transporters (Felpin and Lebreton 2004 Flammia et al. 1999 Reavill et al. 1990 Teng et al. 1998). In guinea pig brain homogenates, lobeline functioned as a mu opioid receptor antagonist (Miller et al. 2007). 

Viscusi E, et al. Peripherally acting mu-opioid receptor antagonists and postoperative ileus mechanisms of action and clinical applicability. Anesth Analg2009 108 1811-1822. 

Bot G, Blake A, Li S, Reisine T. Mutagenesis of a single amino acid in the rat mu opioid receptor discriminates the binding of full agonists from partial agonists and antagonists. J Neurochem 1998 70 358-365. 

Dooley, C. and Houghten, R. (Torrey Pines Institute for Molecular Studies) Novel mu opioid receptor ligands agonists and antagonists, W09640208 (1996) US5641861 (1997) US5919897 (1999). 

MODULATION OF THE MU OPIOID RECEPTOR BY DELTA-SELECTIVE ANTAGONISTS... 

Further studies in mouse vas deferens indicated that DPI-3290 is also active at mu opioid receptors. The intrinsic activity of DPI-3290 at mu opioid receptors was determined in the presence of the highly selective delta opioid receptor antagonist TIPP (H-Tyr-Tic-Phe-Phe-OH) (3 pM) and the selective kappa opioid receptor antagonist nor-BNI (15 nM). Under these conditions, DPI-3290 again caused concentration-dependent inhibition of muscle contraction with a corresponding IC50 value of 6.2 2.0 nM. Although far less potent at kappa opioid receptors in comparison to its intrinsic activity at mu... 

The body of literature concerning the functional roles of delta opioid receptors in the digestive tract is somewhat complicated by the results of studies that employed opioid agonists or antagonists with relatively poor selectivity for opioid receptor types (e.g., capable of interacting with both delta and mu opioid receptors within a narrow concentration range). Such ligands include... 

Interestingly, morphine is primarily considered to have selective effects on the mu opioid receptor for its analgesic effects however, there is also evidence that it possesses effects on delta or kappa opioid receptors and that crosstalk can occur between mu and delta opioid receptors [44]. To test the hypothesis that the cardioprotective effects of IPC and morphine were acting via a delta opioid receptor, Schultz et al. [45] administered the selective delta receptor antagonist naltrindole to rats prior to IPC or morphine infusion. In both instances, the cardioprotective effects of morphine and IPC were completely abolished at a dose of naltrindole that had no effect by itself on infarct size in nonpreconditioned rat hearts. These data clearly suggest that both IPC and morphine are exerting their cardioprotective effects via the delta opioid receptor in the intact rat heart. 

Moynihan H, Jales AR, Greedy BM, Broadbear JH, Purington L, Traynor JR, Woods JH, Lewis JW, Husbands SM (2009) 14( -0-Cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity. J Med Chem 52 1553-1557... 

Corbett AD, Kosterlitz HW (1986) Bremazocine is an agonist at kappa-opioid receptors and an antagonist at mu-opioid receptors in the guinea-pig myenteric plexus. Br J Pharmacol 89 245-249... 

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