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Virginia Commonwealth University

Theses/Dissertations

2020

CB1

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In Vivo Effects Of The Cb1 Allosteric Modulator Ldk1258, A Structural Analog Of Org-27569, Mohammed A. Mustafa Jan 2020

In Vivo Effects Of The Cb1 Allosteric Modulator Ldk1258, A Structural Analog Of Org-27569, Mohammed A. Mustafa

Theses and Dissertations

CB1 receptor allosteric modulators are an area of growing interest for their potential novel therapeutic actions. In the present study, we examined LDK1258 in a series of pharmacological in vivo tests sensitive to CB1 receptor stimulation. In the tetrad assay, LDK1258 produced significant decreases in locomotor activity and body temperature measures but did not produce either antinociception as measured in the tail-withdrawal assay or catalepsy as assessed in the bar test. These same effects were observed in both CB1 (-/-) and (+/+) mice. Moreover, LDK1258 failed to shift the dose-response curves of two orthosteric CB1 receptor agonists in the triad …