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• W2094348512 abstract "The present study shows that [3H]4-DAMP binds specifically, saturably, and with high affinity to muscarinic receptor sites in the rat brain. In homogenates of hippocampus, cerebral cortex, striatum, and thalamus, [3H]4-DAMP appears to bind two sub-populations of muscarinic sites: one class of high-affinity, low capacity sites (Kd < 1 nM; Bmax = 45–152 fmol/mg protein) and a second class of lower-affinity, high capacity sites (Kd > 50 nM; Bmax = 263–929 fmol/mg protein). In cerebellar homogenates, the Bmax of [3H]4-DAMP binding sites was 20 ± 2 and 141 ± 21 fmol/mg protein for the high- and the lower-affinity site, respectively. The ligand selectivity profile for [3H]4-DAMP binding to its sites was similar for both the high- and lower-affinity sites; atropine = (—)QNB = 4-DAMP » pirenzepine > AF-DX 116, although pirenzepine was more potent (16-fold) at the lower- than at the high-affinity sites. The autoradiographic distribution of [3H]4-DAMP sites revealed a discrete pattern of labeling in the rat brain, with the highest densities of [3H]4-DAMP sites present in the CA1 sub-field of Ammon's horn of the hippocampus, the dentate gyrus, the olfactory tubercle, the external plexiform layer of the olfactory bulb and layers I–II of the frontoparietal cortex. Although the distribution of [3H]pirenzepine sites was similar to that of [3H]4-DAMP sites in many brain regions, significant distinctions were apparent. Thus, both the ligand selectivity pattern of [3H]4-DAMP binding and the autoradiographic distribution of sites suggest that although the high-affinity [3H]4-DAMP sites may consist primarily of muscarinic-M3 receptors, the lower-affinity [3H]4-DAMP sites may be composed of a large proportion of muscarinic-M1 receptors." @default.
• W2094348512 created "2016-06-24" @default.
• W2094348512 creator A5016280147 @default.
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• W2094348512 date "1991-11-01" @default.
• W2094348512 modified "2023-09-27" @default.
• W2094348512 title "Heterogeneous binding of [3H]4-DAMP to muscarinic cholinergic sites in the rat brain: Evidence from membrane binding and autoradiographic studies" @default.
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• W2094348512 doi "https://doi.org/10.1002/syn.890090303" @default.
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