The Binding of Antagonists to Brain Muscarinic Receptors
The equilibrium binding of muscarinic antagonists to a crude synaptosome fraction from rat cerebral cortex obeys the simple Langmuir isotherm. The affinity constants measured range from 10 5 to 10 10 M -1 and in all cases agree within a factor of 3 with the corresponding values derived from measurem...
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| Published in | Molecular pharmacology Vol. 14; no. 5; pp. 737 - 750 |
|---|---|
| Main Authors | , , , |
| Format | Journal Article |
| Language | English |
| Published |
United States
American Society for Pharmacology and Experimental Therapeutics
01.09.1978
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| Subjects | |
| Online Access | Get full text |
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| Abstract | The equilibrium binding of muscarinic antagonists to a crude synaptosome fraction from
rat cerebral cortex obeys the simple Langmuir isotherm. The affinity constants measured
range from 10 5 to 10 10 M -1 and in all cases agree within a factor of 3 with the corresponding
values derived from measurements of anticholinergic potency on smooth muscle. The
methodology which must be applied to obtain valid measurements of affinity constants
from in vitro studies using radiolabelled ligands is discussed. |
|---|---|
| AbstractList | The equilibrium binding of muscarinic antagonists to a crude synaptosome fraction from
rat cerebral cortex obeys the simple Langmuir isotherm. The affinity constants measured
range from 10 5 to 10 10 M -1 and in all cases agree within a factor of 3 with the corresponding
values derived from measurements of anticholinergic potency on smooth muscle. The
methodology which must be applied to obtain valid measurements of affinity constants
from in vitro studies using radiolabelled ligands is discussed. |
| Author | A. S. V. BURGEN E. C. HULME N. J. M. BIRDSALL P. MEHTA |
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| Snippet | The equilibrium binding of muscarinic antagonists to a crude synaptosome fraction from
rat cerebral cortex obeys the simple Langmuir isotherm. The affinity... |
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| SubjectTerms | Animals Atropine - metabolism Benzilates - metabolism Binding, Competitive Brain - metabolism Brain - ultrastructure In Vitro Techniques Kinetics Male Parasympatholytics - metabolism Rats Receptors, Cholinergic - metabolism Receptors, Muscarinic - metabolism Scopolamine Hydrobromide - metabolism Subcellular Fractions - metabolism Synaptosomes - metabolism |
| Title | The Binding of Antagonists to Brain Muscarinic Receptors |
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