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Stereoselective muscarinic acetylcholine and opiate receptors in human phagocytic leukocytes

1980; Elsevier BV; Volume: 29; Issue: 10 Linguagem: Inglês

10.1016/0006-2952(80)90431-1

1873-2968

Anita Lopker, Leo G. Abood, Wayne Hoss, Fabian J. Lionetti,

Glycosylation and Glycoproteins Research

Human granulocytes and monocytes exhibited stereospecific, high-affinity binding to 3-quinuclidinyl benzilate (QNB) and dihydromorphine (DHM), specific ligands for the muscarinic cholinergic and opiate receptors respectively. The stereoselective muscarinic binding occurred in intact, viable cells as well as in cell fragments prepared by sonication. The apparent Kd for the muscarinic binding in granulocytes was 16 nM, and the number of binding sites per cell was on the order of 8 × 104, monocytes contained approximately 3 × 104 binding sites per cell with an apparent Kd of 20 nM. Studies in sonicated and in non-sonicated cell preparations indicate that the affinity of the l-isomer is approximately 10 times that of the d-isomer. Both cell types also exhibited stereospecific opiate binding with an apparent Kd of 10 nM for granulocytes and 8 nM for monocytes. The number of binding sites per cell was 3000 and 4000 respectively.