PMID: 3753655Jan 8, 1986Paper

Muscarinic cholinergic receptor subtypes in the human brain. II. Quantitative autoradiographic studies

Brain Research
R CortesJ M Palacios

Abstract

The distribution and characteristics of M1 and M2 muscarinic cholinergic receptors as defined by their affinity for the antagonist pirenzepine were studied in the human brain using in vitro quantitative autoradiographic techniques. The binding of N-[3H]methylscopolamine ([3H]NMS) to cortical and striatal microtome tissue sections was saturable and presented a Kd of 0.25 nM. The sensitivity of [3H]NMS-binding sites to 100 microM carbachol and 300 nM pirenzepine was analyzed in 30 brain areas. In selected brain regions, complete competition curves using carbachol, pirenzepine and atropine were analyzed. Finally, the regional distribution of M1 sites was studied using [3H]pirenzepine ([3H]PZ) as ligand. The binding of [3H]NMS to striatum, hippocampus and amygdala was very sensitive to pirenzepine but not to carbachol. The opposite situation was found in thalamus, hypothalamus, substantia innominata, pons and medulla, while intermediate sensitivity to both displacers was observed in different layers of the cortex and in the claustrum. Competition experiments showed that [3H]NMS binding was displaced with the same affinity by atropine in all the regions studied, while the IC50 of carbachol varied from 5 microM in the nucleus faciali...Continue Reading

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Citations

May 10, 2002·Hippocampus·Liang ZhaoHideo Tsukada
Jan 1, 1992·Journal of Neuroscience Research·A NordbergB Winblad
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Aug 13, 2005·Journal of Chemical Neuroanatomy·Fuencisla Pilar-CuéllarArsenio Fernández-López

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