Molecular regulation of opioid receptors.
Opioid actions are initiated at membrane receptors which couple to cellular effectors through G protein-mediated pathways. In the central nervous system opioids reduce neuronal activity through the inhibition of voltage-dependent Ca2+ channels, the activation of K+ channels and the inhibition of adenylyl cyclase. A significant clinical limitation to opioid therapy is the development of tolerance, a biological event that has been linked to agonist effects at the receptor level. Molecular studies on the consequences of opioid receptor regulation will provide a better understanding of the cellular mechanisms involved in the agonist-mediated events in tolerance development.
Blake
A D
AD
Department of Pharmacology, University of Pennsylvania, School of Medicine, Philadelphia 19104, USA.
Bot
G
G
Tallent
M
M
Law
S F
SF
Li
S
S
Freeman
J C
JC
Reisine
T
T
D000818:Animals; D006801:Humans; D011957:Receptors, Opioid / Q000378:metabolism*
D011957:Receptors, Opioid