TY - JOUR
T1 - Properties of opiate receptor binding in rat brain
AU - Pert, C. B.
AU - Snyder, S. H.
PY - 1973
Y1 - 1973
N2 - [3H]Naloxone, a potent opiate antagonist, binds stereospecifically to opiate receptor sites in rat brain tissue. The binding is time, temperature, and pH dependent and saturable with respect to [3H]naloxone and tissue concentration. The [3H]naloxone receptor complex formation is bimolecular with a dissociation constant of 20 nM. 15 opiate agonists and antagonists compete for the same receptors, whose density is 30 pmol/g. Potencies of opiates and their antagonists in displacing [3H]naloxone binding parallel their pharmacological potencies.
AB - [3H]Naloxone, a potent opiate antagonist, binds stereospecifically to opiate receptor sites in rat brain tissue. The binding is time, temperature, and pH dependent and saturable with respect to [3H]naloxone and tissue concentration. The [3H]naloxone receptor complex formation is bimolecular with a dissociation constant of 20 nM. 15 opiate agonists and antagonists compete for the same receptors, whose density is 30 pmol/g. Potencies of opiates and their antagonists in displacing [3H]naloxone binding parallel their pharmacological potencies.
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U2 - 10.1073/pnas.70.8.2243
DO - 10.1073/pnas.70.8.2243
M3 - Article
C2 - 4525427
AN - SCOPUS:0008218273
SN - 0027-8424
VL - 70
SP - 2243
EP - 2247
JO - Proceedings of the National Academy of Sciences of the United States of America
JF - Proceedings of the National Academy of Sciences of the United States of America
IS - 8
ER -