Abstract
1 The reaction of tritiated propylbenzilylcholine mustard ([3H]-PrBCM; N-2′-chloroethyl-N-[2″,3″-3H2] -propyl-2-aminoethylbenzilate) with homogenates of mammalian brain has been studied.
2 The uptake can be divided into an atropine-sensitive component of fixed capacity (380 pmol/g protein in the rat) and an atropine-insensitive part.
3 The atropine-sensitive portion is identified as muscarinic receptor by its insensitivity to nicotinic antagonists and anticholinesterases and its sensitivity to a range of muscarinic antagonists.
4 The uptake of [3H]-PrBCM is also inhibited by muscarinic agonists and there is reasonable quantitative agreement between the affinities of agonists estimated in this way and in intact tissues by physiological responses.
5 The fraction of [3H]-PrBCM uptake inhibited by muscarinic antagonists and agonists is the same.
6 The amount of receptor found in six mammalian species was inversely related to the size of the brain, but the rates of alkylation and the sensitivity to atropine were not dissimilar.
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Selected References
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- Burgen A. S., Hiley C. R., Young J. M. The binding of (3H)-propylbenzilycholine mustard by longitudinal muscle strips from guinea-pig small intestine. Br J Pharmacol. 1974 Jan;50(1):145–151. doi: 10.1111/j.1476-5381.1974.tb09602.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Curtis D. R., Crawford J. M. Central synaptic transmission--microelectrophoretic studies. Annu Rev Pharmacol. 1969;9:209–240. doi: 10.1146/annurev.pa.09.040169.001233. [DOI] [PubMed] [Google Scholar]
- Farrow J. T., O'Brien R. D. Binding of atropine and muscarone to rat brain fractions and its relation to the acetylcholine receptor. Mol Pharmacol. 1973 Jan;9(1):33–40. [PubMed] [Google Scholar]
- LOWRY O. H., ROSEBROUGH N. J., FARR A. L., RANDALL R. J. Protein measurement with the Folin phenol reagent. J Biol Chem. 1951 Nov;193(1):265–275. [PubMed] [Google Scholar]
- PATON W. D., RANG H. P. THE UPTAKE OF ATROPINE AND RELATED DRUGS BY INTESTINAL SMOOTH MUSCLE OF THE GUINEA-PIG IN RELATION TO ACETYLCHOLINE RECEPTORS. Proc R Soc Lond B Biol Sci. 1965 Aug 24;163:1–44. doi: 10.1098/rspb.1965.0058. [DOI] [PubMed] [Google Scholar]
- Parker R. B. Measurement of drug-receptor dissociation constants of muscarinic agonists on intestinal smooth muscle. J Pharmacol Exp Ther. 1972 Jan;180(1):62–70. [PubMed] [Google Scholar]
- TOWER D. B., ELLIOTT K. A. C. Activity of acetylcholine system in cerebral cortex of various unanesthetized mammals. Am J Physiol. 1952 Mar;168(3):747–759. doi: 10.1152/ajplegacy.1952.168.3.747. [DOI] [PubMed] [Google Scholar]
- Young J. M., Hiley R., Burgen A. S. Homologues of benzilylcholine mustard. J Pharm Pharmacol. 1972 Dec;24(12):950–954. doi: 10.1111/j.2042-7158.1972.tb08925.x. [DOI] [PubMed] [Google Scholar]