In vivo visualization of delta opioid receptors upon physiological activation uncovers a distinct internalization profile

J Neurosci. 2012 May 23;32(21):7301-10. doi: 10.1523/JNEUROSCI.0185-12.2012.

Abstract

G-protein-coupled receptors (GPCRs) mediate numerous physiological functions and represent prime therapeutic targets. Receptor trafficking upon agonist stimulation is critical for GPCR function, but examining this process in vivo remains a true challenge. Using knock-in mice expressing functional fluorescent delta opioid receptors under the control of the endogenous promoter, we visualized in vivo internalization of this native GPCR upon physiological stimulation. We developed a paradigm in which animals were made dependent on morphine in a drug-paired context. When re-exposed to this context in a drug-free state, mice showed context-dependent withdrawal signs and activation of the hippocampus. Receptor internalization was transiently detected in a subset of CA1 neurons, uncovering regionally restricted opioid peptide release. Importantly, a pool of surface receptors always remained, which contrasts with the in vivo profile previously established for exogenous drug-induced internalization. Therefore, a distinct response is observed at the receptor level upon a physiological or pharmacological stimulation. Altogether, direct in vivo GPCR visualization enables mapping receptor stimulation promoted by a behavioral challenge and represents a powerful approach to study endogenous GPCR physiology.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Enkephalin, Methionine / metabolism
  • Female
  • Gene Knock-In Techniques
  • Hippocampus / drug effects
  • Hippocampus / metabolism*
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Molecular Imaging
  • Morphine / pharmacology
  • Protein Transport*
  • Receptors, Opioid, delta / agonists
  • Receptors, Opioid, delta / genetics
  • Receptors, Opioid, delta / metabolism*
  • Substance Withdrawal Syndrome / metabolism

Substances

  • Receptors, Opioid, delta
  • Enkephalin, Methionine
  • Morphine