Muscarinic receptor agonists

Eglen, RM and Watson, N (1996) Selective muscarinic receptor agonists and antagonists. Pharmacol. Toxicol. 78 59-78. 

Brown, J.H. and Taylor, P., Muscarinic receptor agonists and antagonists, in Goodman and Gilman s The Pharmacological Basis of Therapeutics, 9th ed., Hardman, J.G. and Limbird, L.E., Eds., McGraw-Hill, New York, 1996, chap. 7. 

Velazquez-Moctezuma, J., Gillin, J. C. Shiromani, P. J. (1989). Effect of specific Ml, M2 muscarinic receptor agonists on REM sleep generation. Brain Res. 503, 128-31. 

Muscarine, an alkaloid from certain species of mushrooms, is a muscarinic receptor agonist. The compound has toxicologic importance muscarine poisoning will produce all of the effects that are associated with an overdose of ACh (e.g., bronchocon strict ion, bradycardia, hypotension, excessive salivary and respiratory secretion, and sweating). Poisoning by muscarine is treated with atropine. 

Muscarinic Agonists. Another approach is to use a medication that directly activates subtypes of the acetylcholine receptors, namely, muscarinic receptor agonists. The muscarinic agonists used in the past have not been effective. This includes bethanecol, pilocarpine, and oxotremorine. This line of treatment, however, has not been entirely abandoned, and several medications are currently in testing. 

Muscarinic receptor agonists, such as carbachol and bethanechol, can improve intestinal motility, e.g. in the post operative state. Both drugs act with some... 

Pilocarpine is a naturally occurring cholinomimetic alkaloid that is structurally distinct from the choline esters. It is a tertiary amine that crosses membranes relatively easily. Therefore, it is rapidly absorbed by the cornea of the eye, and it can cross the blood-brain barrier. Pilocarpine is a pure muscarinic receptor agonist, and it is unaffected by cholinesterases. Muscarine is an alkaloid with no therapeutic use, but it can produce dangerous cholinomimetic stimulation following ingestion of some types of mushrooms (e.g., Inocybes). 

The protocol is used for the preparation of 25 kg of the aldehyde in Banyu, and applied to the synthesis of a muscarinic receptor agonist. It is noteworthy that halogen-metal exchange reactions with other metal reagents such as butyllithium or isopropylmagnesium bromide led to more complex mixtures. The Banyu protocol was applicable to similar monoformylation reactions of dibromoheteroarenes (Table 12). 

Zlotos, D. P., Bender, U., Holzgrabe, U. Muscarinic receptor agonists and antagonists, Exp. Opin. Ther. Patents 1999, 9, 1029-1053. 

Variable elimination is the name given to the process by which unhelpful or unnecessary variables are removed from a data set. One means by which a variable may be judged is from the information it contains. If the standard deviation of the variable is very small, then it does not contain much information and is thus not likely to be useful in the construction of models. Another common situation is that a variable may contain only a small number of different values, an extreme case being where the values are the same for all compounds in the set except one. If a variable such as this is used in the construction of a model then it may appear to be useful but is usually only serving to identify, and thus explain, the response value for that single compound. An example of this is shown in Table 7.2, which contains values of receptor binding and computed properties for a set of quinuclidine-based muscarinic receptor agonists (Saunders et al., 1990). For some of the compounds (6, 7, 8, and 12) the substitution pattern means that there is not, in fact, an... 

Bodick NC, Offen WW, Levey Al, Cutler NR, Gauthier SG, et al. 1997. Effects of xanomeline, a selective muscarinic receptor agonist, on cognitive function and behavioral symptoms in Alzheimer disease. Arch Neurol 54 465-473. 

Rasmussen T, Fink-Jensen A, Sauerberg P, Swedberg MD, Thomsen C, et al. 2001. The muscarinic receptor agonist... 

Shannon HE, Hart JC, Bymaster FP, Calligaro DO, DeLapp NW, et al. 1999. Muscarinic receptor agonists, like dopamine receptor antagonist antipsychotics, inhibit conditioned avoidance response in rats. J Pharmacol Exp Ther 290 901-907. 

Brown JH and Taylor P (1996) Muscarinic receptor agonists and antagonists. In Hardman JG and Limbird LE (eds.) Goodman and Gillman s Pharmacological Basis of Therapeutics, 9th edn., pp. 141-160. New York McGraw-Hill. 

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