Pre- and postsynaptic muscarinic receptors in surgical samples from human cerebral cortex.

The present study was carried out using fresh surgical material from human cerebral cortex of patients who were not medicated with atropine or other drugs known to affect the cholinergic system. The concentration of [3H]L-quinuclidinyl benzilate binding sites was 0.45 /+- 0.05 pmol/mg protein and the Kd-value of the receptor-[3H]L-QNB-complex was 0.038 /+- 0.005 nM. Agonist binding was studied by varying the concentration of carbamylcholine (10(-8) to 10(-2) M) in the presence of a constant concentration (0.2nM) of [3H]L-quinuclidinyl benzilate. The data revealed the existence of two populations of binding sites for carbamylcholine with different affinities and capacities. Presynaptic muscarinic receptors were studied in slices of the cerebral cortex, which were loaded with [3H]choline. The muscarinic antagonist, atropine (10(-6) and 10(-7) M) acting at the presynaptic muscarinic receptors enhanced the release of [3H] acetylcholine. It was also shown that muscarinic stimulation leads to elevation of cyclic GMP levels in the human cerebral cortical slices.