Estrogen and progesterone modulate [35S]GTPgammaS binding to nociceptin receptors.

Neuroendocrinology
Arnulfo Quesada, Paul Micevych

Abstract

Sex steroids modulate reproduction by altering the response of steroid-activated opioid circuits in the hypothalamus and limbic system, by inducing release of endogenous opioids and activation of their cognate receptors. Many studies have concentrated on steroid regulation of exogenous opioid peptides, but steroids also have important actions on opioid receptors inducing receptor trafficking. Opioid receptors are G protein-coupled receptors and their activation catalyzes the exchange of GTP for GDP initiating intracellular signaling cascades. Kinetics of G protein activation were studied using [(35)S]GTPgammaS binding. Catalytic amplification, the number of G proteins activated per occupied receptor, was used as a measure of receptor/transducer amplification. The present study examined whether estrogen and progesterone treatment altered the kinetics of nociceptin opioid receptor (ORL1) in plasma membranes from the medial preoptic area and mediobasal hypothalamus. These hypothalamic regions are important in the gonadal steroid hormone regulation of sexual receptivity. In the mediobasal hypothalamus, estrogen increased ORL1 (B(max)) receptor number 2-fold and maximal GTPgammaS binding (E(max)) 3.9-fold. Subsequent progesterone tr...Continue Reading

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Citations

Oct 2, 2009·Peptides·Richard J Bodnar
Sep 17, 2011·Birth Defects Research. Part B, Developmental and Reproductive Toxicology·Brian P EnrightStephan J Kopytek
Sep 12, 2019·Developmental Neurobiology·Thorsten M KranzEliot A Brenowitz

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