(+)-( super(3)H)MK-801 binding sites in postmortem human brain

The pharmacological specificity and the regional distribution of the N-methyl-D-aspartate receptor-associated 5-methyl-10,11-dihydro-5H-dibenzo(a,d)cyclohepten-5,10-imine maleate (MK-801) binding sites in human postmortem brain tissue were determined by binding studies using (+)-( super(3)H)MK-801. Scatchard analysis revealed a high-affinity and a low-affinity binding site. The rank order pharmacological specificity and stereoselectivity of the high-(cortex) and low-(cerebellar) affinity binding sites were identical. However, all compounds tested showed greater potency at the high-affinity site in cortex. The results indicate that (+)-( super(3)H)MK-801 binding in human postmortem brain tissue shows pharmacological and regional specificity.