Opioid Receptor Regulation
The actions of opiates and opioid peptides upon nervous tissue are mediated by μ-, δ, and κ-opioid receptors and (in the case of σ-opioids) the PCP site of the NMD A receptor (for a review see Chap. 1). The three opioid receptors exhibit different ligand selectivities, strikingly different neuroanatomical patterns, distinct physiological and behavioral profiles, and differing sensitivities to naloxone (or naltrexone) antagonism. In the central nervous system (CNS) these receptors are activated by three classes of structurally related peptides, β-endorphin, the enkephalins, and the dynorphin-related peptides, encoded by three different genes. The observation that opiate analgesics produce tolerance and dependence suggests that opioid systems can undergo plastic changes. This chapter focuses on studies of the regulation of μ- and δ-opioid receptors. A particular emphasis is placed upon examination of mechanisms by which chronic treatment of opioid drugs quantitatively regulates opioid receptors in adult, embryonic, and neonatal brain.
KeywordsMethionine NMDA Alkaloid Neuroblastoma Haloperidol
Unable to display preview. Download preview PDF.
- Genazzani AR, Petraglia F, Giudetti R, Volpe A, Facchinetti F (1986) Neonatal β-endorphin secretion in babies passively addicted to opiates. Excerpta Med Int Congr Ser 369: 379–382Google Scholar
- Guitart X, Nestler EJ (1989) Identification of morphine and cyclic AMP-regulated phosphoproteins (MARPPs) in the locus coeruleus and other regions of rat brain. Regulation by acute and chronic morphine. J Neurosci 9: 4371–4387Google Scholar
- Guitart X, Hayward MD, Nisenbaum LK, Beitner-Johnson DB, Haycock JW, Nestler EJ (1990) Identification of MARPP-58, a morphine- and cyclic AMP- regulated phosphoprotein of 58kDa, as tyrosine hydroxylase: evidence for regulation of its expression by chronic morphine in the rat locus coeruleus. J Neurosci 10: 2649–2659PubMedGoogle Scholar
- Iyengar S, Rabii J (1982) Effect of prenatal exposure to morphine on the postnatal development of opiate receptors. Fed Proc 41: 1354–1357Google Scholar
- Klee WA, Lampert A, Nirenberg M (1976) Dual regulation of adenylate cyclase by endogenous opiate peptides. In: Kosterlitz HW (ed) Opiates and endogenous opioid peptides. Elsevier/North-Holland, New York, pp 153–159Google Scholar
- McDonald RL, Werz MA (1986) Dynorphin A decreases voltage-dependent calcium conductance of mouse dorsal root ganglion neurones. J Physiol (Lond) 377: 237–249Google Scholar
- Tsang D, Ng SC, Ho KP (1982) Kappa opioid receptor-mediated analgesia in the developing rat. Brain Res 394: 145–152Google Scholar
- Young WS, Kuhar MJ (1979) A new method for receptor autoradiography: [3H]opioid receptors in rat brain. Brain Res 179: 225–270Google Scholar