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MK-801 inhibition of nicotinic acetylcholine receptor channels

โœ Scribed by Mariano Amador; John A. Dani

Publisher
John Wiley and Sons
Year
1991
Tongue
English
Weight
908 KB
Volume
7
Category
Article
ISSN
0887-4476

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โœฆ Synopsis

MK-801 is a potent inhibitor of the NMDA subtype of glutamate receptors. Single-channel and macroscopic currents indicate that MK-801 also inhibits nicotinic acetylcholine receptors (nAChRs). MK-801 does not significantly increase desensitization of the nAChRs or compete for the ACh binding site. Although there is a slight inhibition of the closed nAChR, the main action of MK-801 is to enter and block the open channel. The voltage dependence for block is consistent with a single binding site within the channel that is 50% of the way through the membrane field. The IC,, for block is 3 pM at -70 mV for currents induced by 0.5 pM ACh. The data from both single-channel and macroscopic currents can be used to estimate a & (0) of 7 pM, which is about 40 times higher than the &(O) for MK-801 binding to the NMDA receptor. The relative potency of tricyclic compounds like MK-801 for various neurotransmitter systems points out that the pharmacologic action of these drugs could involve complicated interactions in vivo.

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