Abstract

In vitro competition binding experiments with the selective 3 muscarinic antagonists AF-DX 116 and pirenzepine (PZ) vs H-N-methylscopolamine as radioligand revealed a characteristic distribution of muscarinic receptor subtypes in different regions of rat brain. Based on non linear least squares analysis, the binding data were compatible with the presence of three different subtypes: the M 1 receptor (high affinity for PZ), the cardiac M 2 receptor (high affinity for AF-DX 116) and the glandular M 2 receptor (low affinity for PZ and AF-DX 116). The highest proportion of M 1 receptors was found in the hippocampus, whilst the cerebellum and the hypothalamus were the regions with the largest fraction of the cardiac M 2 and glandular M 2 receptors, respectively. In certain brain areas, depending on the relative proportions of the subtypes, flat binding curves were seen for AF-DX 116 and PZ. Based on these data, an approximate distribution pattern of the subtypes in the various brain regions is presented.

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