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Endocannabinodergic neuromodulators?

emotion cognition endocannabinoid

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#1 Ruth

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Posted 05 December 2017 - 09:22 AM


Any idea of a Endocannabinoid neuro-modulator(i.e. AEA 2-AG reuptake, receptor density/upregulation...)? https://en.wikipedia.../wiki/Org_27569 "Org 27569 is a drug which acts as a potent and selective positive allosteric modulator of the cannabinoid CB1 receptor. Studies in vitro suggest that it binds to a regulatory site on the CB1 receptor target, causing a conformational change that increases the binding affinity of CB1 agonists such as CP 55,940, while decreasing the binding affinity of CB1 antagonists or inverse agonists such as rimonabant. However while Org 27569 increases the ability of CB1 agonists to bind to the receptor, it decreases their efficacy at stimulating second messenger signalling once bound, and so in practice behaves as an insurmountable antagonist of CB1 receptor function.[1]"

Allosteric modulators of CB1/2 with a CB agonist which isn't blocked by the receptor modulator is the future of (endo)-cannabinoidergic neuromedicine

Edited by Ruth, 05 December 2017 - 09:29 AM.






Also tagged with one or more of these keywords: emotion, cognition, endocannabinoid

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