Cholinergic agonists centrally acting

An alkaloid of natural plant origin, pilocarpine is a direct-acting cholinergic agonist with a dominant action at both peripheral and central muscarinic sites. The cholinomimetic action of pilocarpine on smooth muscle muscarinic receptors generally results in contraction.The response of intraocular smooth muscle to pilocarpine is pupillary constriction, spasm of accommodation, and reduction of lOP. 

Physostigmine, the enantiomer of the naturally occurring alkaloid, has little effect on acetylcholinesterase in vitro (311,312) it is a weak centrally acting cholinergic agonist. Eseroline (248), the ester cleavage product of... 

The ideal agent for facilitating central cholinergic transmisson would act simultaneously as an antagonist at ACh autoreceptors and as an agonist at postsynaptic ACh-receptors.It has been suggestedl B that compounds, with this profile would be of therapeutic value in the... 

Nicotiana tabacum, and lobeline, present in the dried leaves and tops of the herb, Lobelia inflata (13). Both nicotine and lobeline act as agonists on a specific type of acetylcholine receptor, the nicotinic cholinergic receptor. In mammals, nicotinic cholinergic receptors mediate cholinergic neurotransmission in skeletal muscles, autonomic ganglia, and the central nervous system. At these sites nicotine s action has two phases, excitation and depression. Insect central nervous tissues are rich in nicotinic cholinergic receptors (cf. 14), but their role in behavior is not well understood. 

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