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The cannabinoid receptor agonist CP-55,940 and ethyl arachidonate interfere with [3H]batrachotoxinin A 20 α-benzoate binding to sodium channels and inhibit sodium channel function by Yin Duan; Chengyong Liao; Saurabh Jain; Russell A. Nicholson is a Environmental Science article available to read on EtoBox.
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3 H]Batrachotoxinin binding Sodium channel Cannabinoid-1 receptors Synaptoneurosomes Membrane potential Mouse brain Recent investigations in our laboratory showed that voltage-gated sodium channels (VGSCs) in brain are sensitive to inhibition by various synthetic cannabinoids and endocannabinoids. The present experiments examined the effects of the cannabinoid-1 (CB1) receptor agonist CP-55,940 and ethyl arachidonate on [ 3 H] batrachotoxinin A 20 α-benzoate ([ 3 H]BTX-B]) binding and VGSC-dependent depolarization of the nerve membrane in synaptoneurosomes isolated from mouse whole brain. CP-55,940 acted as a full inhibitor of [ 3 H]BTX-B binding and its IC 50 was established at 22.3 μM. At its maximum effect concentration, ethyl arachidonate achieved partial (approximately 70%) inhibition and was less effective than CP-55,940 as an inhibitor of binding (IC 50 = 262.7 μM). The potent CB1 receptor antagonist AM251 (2 μM) had no significant effect on the displacement of [ 3 H]BTX-B by either compound (P N 0.05). Scatchard analyses showed that CP-55,940 and ethyl arachidonate reduce the binding of [ 3 H]BTX-B by lowering its B max but ethyl arachidonate also increased the K d of radio
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- Author
- Yin Duan; Chengyong Liao; Saurabh Jain; Russell A. Nicholson
- Publisher
- Elsevier Science; Elsevier ; Elsevier BV (ISSN 1532-0456)
- Published
- 2008
- Language
- EN
- Field
- Environmental Science (Physical Sciences)