Detection of cannabinoid receptors by photoaffinity labelling.

Abstract:

:A novel [125I]-labelled photoaffinity ligand designed to detect cannabinoid binding sites has been used in mouse brain preparations and in cultured S49 mouse lymphoma cells. The ligand, 2-iodo-5'-azido-delta 8-THC, shows a high affinity for sites in both brain (Kd = 5.60 pM) and whole cell (Kd = 9.38 pM) systems. Photolabelling studies with brain samples revealed the existence of four ligand-protein adducts, of estimated molecular weights 85.5, 62.1, 30.0 and 25.5 kDa, that were diminished by prior exposure to 8 microM THC. A similar study with S49 cells gave adducts with apparent molecular weights of 62.1, 34.4, 16.9 and 13.5 kDa. The ligand produces a typical cannabinoid cataleptic response in mice suggesting that possibly one or more of the binding sites may be involved in some of the receptor mediated actions of THC.

authors

Burstein SH,Audette CA,Charalambous A,Doyle SA,Guo Y,Hunter SA,Makriyannis A

doi

10.1016/0006-291x(91)90951-3

subject

Has Abstract

pub_date

1991-04-15 00:00:00

pages

492-7

issue

1

eissn

0006-291X

issn

1090-2104

pii

0006-291X(91)90951-3

journal_volume

176

pub_type

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