Mu-receptor binding in physiological media: comparison with isolated tissue data.

J A Carroll; L Miller; J S Shaw; C P Downes

doi:10.1016/0143-4179(84)90034-9

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Mu-receptor binding in physiological media: comparison with isolated tissue data.

J A Carroll·L Miller·J S Shaw·C P Downes

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Abstract

Mu-receptor affinities have been determined for a number of opioid drugs using a combination of isolated tissue and receptor binding techniques. The affinities of antagonists and partial agonists were determined by their ability to antagonise responses to [D-Ala2,MePhe4,Glyol5]enkephalin (GLYOL) on the rat vas deferens preparation. There was little correlation between these results and affinities measured by displacement of [3H]-GLYOL from guinea-pig brain membranes incubated in 50mM Tris buffer. By contrast, affinities measured by displacement of [3H]-naloxone from rat brain membranes incubated in a Krebs/HEPES buffer containing a non-hydrolysable analogue of GTP, agreed very closely with the isolated tissue data.

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Animals Brain Enkephalin, Ala(2)-MePhe(4)-Gly(5)-Enkephalins Guinea Pigs In Vitro Techniques Male Naloxone Narcotics Rats Receptors, Opioid Receptors, Opioid, mu Vas Deferens Comparative Study Journal Article

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J A Carroll, L Miller, J S Shaw, C P Downes. 1984. Mu-receptor binding in physiological media: comparison with isolated tissue data.. https://doi.org/10.1016/0143-4179(84)90034-9

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