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βsubunits determine the time course of desensitization in ratα3 neuronal nicotinic acetylcholine receptors

✍ Scribed by Armand B. Cachelin; Rolf Jaggi

Publisher
Springer
Year
1991
Tongue
English
Weight
437 KB
Volume
419
Category
Article
ISSN
0031-6768

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✦ Synopsis

Standard two-electrode voltage-clamp techniques were used to investigate some of the pharmacological and functional properties of two types of rat neuronal nicotinic acetylcholine receptors expressed in Xenopus oocytes after pairwise injection of e3/74 or c~3/72 mRNAs. Currents of several gA amplitude were elicited by fast application of micromolar concentrations of either ace@choline (ACh) or ],l-dimethyl-4-piperazine (DMPP). The activation of either receptor type by DMPP showed cooperativity (Hill coefficient, n > 1.7) with a half-maximal activation concentration (ECso) of 15-30 pM. In e3/74 receptors, ACh displayed cooperativity (n = 1.8) but was less efficacious than DMPP, yet its ECso was about equal to that of DMPP. Finally, in c~3/~2 receptors, ACh was much less efficacious and had a much lower ECso. Desensitization induced by either DMPP or ACh was slow in ~3/74 nicotinic ACh receptors but was rapid and extensive in e3/72 receptors, causing a significant proportion of the response to wane within the first few seconds of agonist application.

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