Modulation of Guanosine-5-O-(3-[³⁵S]thio)triphosphate ([³⁵S]GTP--S) Binding by Opioid Agonists and Antagonists

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In this Subject: Animal Culture ,&nbsp; Pharmacology ,&nbsp; <a title="Veterinary Medicine" href="/content/subcat?j_subject=219&j_availability=">Veterinary Medicine
By this author: Xu, Heng ;&nbsp; Rothman, Richard B.

Authors: Xu, Heng; Rothman, Richard B.

Source: Reviews in Analgesia, Volume 7, Number 1, 2003 , pp. 83-96(14)

Publisher: Cognizant Communication Corporation

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Abstract:

The development of the [³⁵S]GTP- ggr

-S binding assay has proven to be a valuable tool for studying opioid receptor mechanisms. In addition to being useful for medicinal chemistry applications, where it is important to determine if a compound is an agonist or an antagonist, this assay has provided new insights into the mechanisms of opioid tolerance and dependence. Importantly, this assay can provide a new dimension to structure–activity studies. The main purpose of this article is to review the recent work in our laboratory that used the [³⁵S]GTP- ggr

-S binding assay to advance our understanding of the four parameters associated with ligand–receptor interaction: potency, efficacy, intrinsic efficacy, and binding affinity, as well as molecular mechanisms associated with opioid tolerance and dependence. A major finding to emerge from our research is that the structure–activity of intrinsic efficacy is different from the typically studied structure–activity of binding affinity. The relative ease of determining the intrinsic efficacy of a compound with the [³⁵S]GTP- ggr