The Journal of General Physiology
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Published 1 June 2000. doi:10.1085/jgp.115.6.783
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© The Rockefeller University Press, 0022-1295/2000//783/ $5.00
Journal of General Physiology, Volume 115, Number 6, 2000

Original Article

Mechanism of Cgmp-Gated Channel Block by Intracellular Polyamines

Donglin Guoa and Zhe Lua

a Department of Physiology, University of Pennsylvania, Philadelphia, Pennsylvania 19104
University of Pennsylvania, Department of Physiology, D302A Richard Building, 3700 Hamilton Walk, Philadelphia, PA 19104.215-573-1940

zhelu{at}mail.med.upenn.edu

Polyamines block the retinal cyclic nucleotide-gated channel from both the intracellular and extracellular sides. The voltage-dependent mechanism by which intracellular polyamines inhibit the channel current is complex: as membrane voltage is increased in the presence of polyamines, current inhibition is not monotonic, but exhibits a pronounced damped undulation. To understand the blocking mechanism of intracellular polyamines, we systematically studied the endogenous polyamines as well as a series of derivatives. The complex channel-blocking behavior of polyamines can be accounted for by a minimal model whereby a given polyamine species (e.g., spermine) causes multiple blocked channel states. Each blocked state represents a channel occupied by a polyamine molecule with characteristic affinity and probability of traversing the pore, and exhibits a characteristic dependence on membrane voltage and cGMP concentration.

Key Words: retinal cyclic guanine monophosphate–gated channel • ion permeation • protonation • polyamine • diamine

© 2000 The Rockefeller University Press


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