THE CENTRAL AND PERIPHERAL ACTIVITY OF ACETYLENIC AMINES RELATED TO OXOTREMORINE

Abstract

In 1961 Cho, Haslett & Jenden isolated and independently synthesized a metabolite, 1-(4-pyrrolidin-1'-ylbut-2-ynyl)pyrrolid-2-one (oxoTremorine), of Tremorine which was highly active in producing tremors, spasticity, hypokinesia and parasympathomimetic effects. The peripheral pharmacology of this compound was later studied in more detail by Cho, Haslett & Jenden (1962) and it was concluded that the peripheral effects could be explained solely in terms of stimulation of the postganglionic parasympathetic receptors. OxoTremorine inhibited cholinesterase only at high concentrations and it was devoid of nicotinic properties. N-C H2C.C-CH2-N oxoTremorine