Muscarinic receptor selectivities of 3-Quinuclidinyl 8-xanthenecarboxylate (QNX) in rat brain.
We have determined the binding of (R)-3-Quinuclidinyl 8-xanthenecarboxylate to muscarinic acetylcholine receptor preparations from rat cortex, hippocampus, caudate/putamen, thalamus, pons and colliculate bodies. The competition curves determined with [3H]quinuclidinyl benzilate as the radioligand are well described by a two site model with a difference in affinity between the two sites of 12-fold. The proportions of high affinity site vary from 100% in the caudate/putamen to 0% in the pons/medulla. The selectivities are different from those measured by pirenzepine and are consistent with QNX exhibiting similar affinity for the M1, M3, and M4 receptors with lower affinity for the M2 receptor. This assignment was confirmed by determining the affinities of QNX for the cloned receptor subtypes.
Gibson
R E
RE
Department of Radiology, George Washington University Medical Center, Washington, D.C. 20037.
Schneidau
T A
TA
Gitler
M
M
Zeeberg
B
B
Reba
R C
RC
D000818:Animals; D001921:Brain / Q000378:metabolism*; D010890:Pirenzepine / Q000378:metabolism; D011812:Quinuclidines / Q000378:metabolism*; D011813:Quinuclidinyl Benzilate / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D011976:Receptors, Muscarinic / Q000378:metabolism*; D014966:Xanthenes / Q000378:metabolism*
C087422:3-quinuclidinyl 8-xanthenecarboxylate; D011812:Quinuclidines; D011976:Receptors, Muscarinic; D014966:Xanthenes; D010890:Pirenzepine; D011813:Quinuclidinyl Benzilate