Peripheral-type benzodiazepine receptors: autoradiographic localization in whole-body sections of neonatal rats

J Pharmacol Exp Ther. 1985 May;233(2):517-26.


We have developed a procedure that allows the autoradiographic localization of benzodiazepine receptors in whole-body sections of neonatal rats. Central-type benzodiazepine receptors, visualized with [3H]methylclonazepam, are restricted to nervous tissue. In contrast, peripheral-type benzodiazepine receptors, visualized with [3H]Ro5-4864, occur widely, but with discrete localizations throughout the body. Peripheral-type benzodiazepine receptors are most concentrated in the adrenal cortex and the skin. Substantial levels of these receptors are also evident in the heart, the salivary glands, discrete regions of the kidney, the epithelium of the lung, the nasal and lingual epithelia, the lining of the pulmonary arteries, the thymus, the hair follicles of the vibrissae, the tooth buds and the bone marrow. Considerable binding of [3H]Ro5-4864 is observed in the brown fat pads, the liver and the spleen, but high levels of nonspecific binding preclude accurate evaluation of the actual specific binding in these organs. Only low levels of [3H]Ro5-4864 binding sites are found in the brain and they are virtually undetectable in the skeletal muscle, the eye, the inner ear and the gastrointestinal tract. High levels of peripheral-type benzodiazepine receptor appear present in tissues that derive their metabolic energy primarily from oxidative phosphorylation, whereas only low levels are present in tissues that can derive their metabolic energy largely from glycogenolysis. Association of these receptors with mitochondria and a possible role in modulation of energy metabolism is suggested further by the observation that the histochemically visualized distribution of cytochrome oxidase activity overlaps the autoradiographic pattern of [3H]Ro5-4864 binding sites.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Animals, Newborn
  • Autoradiography
  • Benzodiazepinones / metabolism
  • Rats
  • Rats, Inbred Strains
  • Receptors, GABA-A / analysis*
  • Receptors, GABA-A / metabolism
  • Tissue Distribution


  • Benzodiazepinones
  • Receptors, GABA-A
  • 4'-chlorodiazepam