Pumiliotoxin-C and synthetic analogues. A new class of nicotinic antagonists

• Published in: Molecular pharmacology Vol. 22; no. 3; pp. 565 - 573
• Main Authors: Warnick, J E, Jessup, P J, Overman, L E, Eldefrawi, M E, Nimit, Y, Daly, J W, Albuquerque, E X
• Format: Journal Article
• Language: English
• Published: United States American Society for Pharmacology and Experimental Therapeutics 01.11.1982
• Subjects: acetylcholine; Acetylcholinesterase - metabolism; Action Potentials - drug effects; Alkaloids - pharmacology; Animals; Anura; Dendrobatidae; Electric Organ - metabolism; Ganglionic Blockers - pharmacology; In Vitro Techniques; Membrane Potentials - drug effects; Muscle Contraction - drug effects; Muscle Denervation; Muscle, Smooth - drug effects; nerve transmission; neuromuscular junctions; Phrenic Nerve - drug effects; pumiliotoxin-C; Quinolines; rats; Torpedo

Pumiliotoxin-C (PTX-CI), a cis-decahydroquinoline alkaloid, and synthetic analogues inhibited directly and indirectly elicited twitches in rat phrenic nerve diaphragm preparations. At 40 microM the most potent analogue, 2,5-di-n-propyl-cis-decahydroquinoline (PTX-CII), reversibly blocked the indirec...