How to reset your cannabinoid receptors?

10 answers found

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.


In diseases for which cannabinoid receptors are protective, knowledge of the mechanisms of receptor up-regulation could be used to design therapies to regionally increase receptor expression and thus increase efficacy of an agonist.


However, new data, presented by Tam and colleagues in this issue of the JCI, demonstrate that selective blockade of peripheral cannabinoid receptors may be a novel successful therapeutic approach.


Studies using either the CB1 receptor antagonist and inverse agonist SR141716 or CB1-receptor-deficient mice suggest that numerous presynaptic cannabinoid receptors are tonically activated by endogenous cannabinoids and/or are constitutively active.


These data demonstrate that neurite remodeling is a newly discovered function of CB1 cannabinoid receptors.


Cannabinoid receptors thus have the potential to prevent other Gi/o-coupled receptors from transducing their biological signals.


These findings suggest two new signaling pathways for the cannabinoid receptors.


We suggest that the altered cannabinoid receptor expression is part of the adaptive changes underlying cannabinoid tolerance.


This effect is reversible within 3 days and is associated with a transient modification in the functional properties of cannabinoid receptors.


These results suggest that prolonged stimulation of cannabinoid receptors can transiently silence glutamatergic nerve terminals.

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