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• W2306231640 endingPage "1072" @default.
• W2306231640 startingPage "1064" @default.
• W2306231640 abstract "The CB1 cannabinoid receptor antagonist SR 141716A abolished the inhibition of Ca²⁺ currents by the agonist WIN 55,212–2. However, SR 141716A alone increased Ca²⁺ currents, with an EC₅₀ of 32 nm, in neurons that had been microinjected with CB1 cRNA. For an antagonist to elicit an effect, some receptors must be tonically active. Evidence for tonically active CB1 receptors was seen as enhanced tonic inhibition of Ca²⁺currents. Preincubation with anandamide failed to enhance the effect of SR 141716A, indicating that anandamide did not cause receptor activity. Under Ca²⁺-free conditions designed to block the Ca²⁺-dependent formation of anandamide and<i>sn</i>-2-arachidonylglycerol, SR 141716A again increased the Ca²⁺ current. The Ca²⁺ current was tonically inhibited in neurons expressing the mutant K192A receptor, which has no affinity for anandamide, demonstrating that this receptor is also tonically active. SR 141716A had no effect on the Ca²⁺current in these neurons, but SR 141716A could still antagonize the effect of WIN 55,212–2. Thus, the K192 site is critical for the inverse agonist activity of SR 141716A. SR 141716A appeared to become a neutral antagonist at the K192A mutant receptor. Native cannabinoid receptors were studied in male rat major pelvic ganglion neurons, where it was found that WIN 55,212–2 inhibited and SR 141716A increased Ca²⁺ currents. Taken together, our results demonstrate that a population of native and cloned CB1 cannabinoid receptors can exist in a tonically active state that can be reversed by SR 141716A, which acts as an inverse agonist." @default.
• W2306231640 created "2016-06-24" @default.
• W2306231640 creator A5004649890 @default.
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• W2306231640 date "1998-12-01" @default.
• W2306231640 modified "2023-09-25" @default.
• W2306231640 title "SR 141716A Acts as an Inverse Agonist to Increase Neuronal Voltage-Dependent Ca²⁺Currents by Reversal of Tonic CB1 Cannabinoid Receptor Activity" @default.
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• W2306231640 doi "https://doi.org/10.1124/mol.54.6.1064" @default.
• W2306231640 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/9855635" @default.
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