Mu opiate receptor

Zadina JE, Martiri Schild S, Gerall AA, et al Endomorphins novel endogenous mu-opiate receptor agonists in regions of high mu-opiate receptor density. Ann N Y... 

Giimm MC, Ben-Baruch A, Taub DD, Howard OM, Resau JH, Wang JM (1998) Opiates transde-activate chemokine receptors delta and mu opiate receptor-mediated heterologous desensitization. J Exp Med 188(2) 317-325... 

Opiates produce more discreet inhibitory effects since they bind to and activate inhibitory opioid receptors which, due to their restricted distribution, cause less widespread effects than those of the barbiturates and alcohol. Activation of the opioid receptors leads to a decrease in release of other neurotransmitters (glutamate, NA, DA, 5-HT, ACh, many peptides, etc.) and direct hyperpolarisation of cells by opening of K+ channels and decreasing Ca + channel activity via predominant actions on the mu opiate receptor (see Chapter 12). 

Zadina JE, Hackler L, Ge LJ, Kastin AJ. A potent and selective endogenous agonist for the mu opiate receptor. Nature (London) 1997 386 499-502. 

Wang J, Johnson P, Persico Am Hawkins A, Griffin C, Uhl G. Human mu opiate receptor cDNA and genomic clones, pharmacological characterization and chromosomal assignment. FEBS Lett 1994 338 217-222. 

Moriwaki A, Wang J, Svingos A, van Bockstaele E, Cheng P, Pickel V, Uhl GR. Mu opiate receptor immunoreactiv-ity in rat central nervous system. Neuro-chem Res 1996 21 1315-1331. 

Leysen, J.E., Gommeren, W., Niemegeers, C.J. [3H]Sufentanil, a superior ligand for mu-opiate receptors binding properties and regional distribution in rat brain and spinal cord, Eur. J. Pharmacol. 1983, 87, 209-225. 

Bestervelt LL, Nolan CJ, Cai Y, et al. 1991. Altered rat brain mu opiate receptor number after exposure to 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) [Abstract 1192], The Toxicologist 11 08. 

The first peptide family of amphibian opiates was discovered in 1981 and named dermorphins [2,3], Until the discovery of mammalian endomor-phins by Zadina et al. [4], these peptides represented the most potent and selective mu opiate receptor agonists identified in living organisms. Nine years later, deltorphins were discovered in the amphibian skin. These peptides are still the most potent and selective delta opiate agonists available today [5]. 

Cadet P, Mantione KJ, Stefano GB. 2003. Molecular identification and functional expression of mu 3, a novel alternatively spliced variant of the human mu opiate receptor gene. J Immunol 170 5118-5123. 

Pasternak GW, Wood PJ. 1986. Multiple mu opiate receptors. Life Sci 38 1889-1898. 

Wang JB, Imai Y, Eppler CM, Gregor P, Spivak CE, et al. 1993. mu opiate receptor CDNA cloning and expression. Proc Natl Acad Sci USA 90 10230-10234. 

Smith DJ, Perrotti JM, Crisp T, Cabrtil MEY, Long JT, Scalzitti JM (1988) The mu opiate receptor is responsible for descending pain inhibition originating in the periaqueductal gray region of the rat brain. Eur J Pharmacol 156 47—54... 

Cadet P (2004) Mu opiate receptor subtypes. Med Sci Momt 10 MS28-MS32. 

Borowitz, J., Gunasekar, P., Isom, G. (1997). Hydrogen cyanide generation by mu opiate receptor activation Possible neuromodulatory role of endogenous cyanide. Brain Research, 768, 294-300. 

Sabin M, Bowen WD, Donoghue JP. 1992. Location of nicotinic and muscarinic cholinergic and mu-opiate receptors in rat cerebral neocortex Evidence from thalamic and cortical lesions. Brain Res 579 135-147. 

Tramadol has two basic modes of action mu opiate receptor binding and inhibition of norepinephrine and serotonin reuptake. It is indicated for the relief of moderate to moderately severe pain. ... 

Fig. 24. Patch and matrix striatal compartments are labeled with neurochemical markers. A) The patch compartment is labeled with 3H-naloxone binding to mu opiate receptors (white in the darkfield photomicrograph). B) The matrix compartment is labeled with calbindin-immunoreactivity, which labels spiny projection neurons that provide inputs to the substantia nigra pars reticulata. The correspondence between calbindin-poor zones (black arrows) and mu opiate binding sites (white arrows) is seen to occur in all regions of the striatum. Calbindin-immunoreactivity is relatively weak in the dorso-lateral striatum, which nonetheless contains opiate receptor patches.

Fig. 29. Coronal sections through the striatum showing mu-opiate receptor with 3H-naloxone binding of patches (A and B) and in adjacent sections spiny projection neurons labeled by in situ hybridization histochemistry with probes directed against substance P mRNA (A ) and enkephalin mRNA (B ). Substance P and enkephalin are expressed by different populations of spiny projection neurons, each comprising about half of the population and each evenly distributed in both patch and matrix compartments (arrows show patches in the corresponding sections). From Gerfen and Young (1987).

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