Elimination of Na+ and GTP regulation of alpha 2-adrenoceptor-agonist interactions in rat kidney membranes by 4,4'-diisothiocyano-2,2'-stilbene disulfonic acid (DIDS).
Pretreatment of rat kidney membranes with 4,4'-diisothiocyano-2,2'-stilbene disulfonic acid (DIDS) did not affect the Bmax but reduced the affinity of the receptors for antagonist by less than 2-fold. However, such treatment reduced the affinity of the receptors for agonist by several fold by preventing the formation of agonist-receptor-Gi-protein complex. The modulatory effects of GTP and Na+ on alpha 2-adrenoceptor-agonist interactions were also abolished. These results suggest that DIDS acts at multiple sites on alpha 2-adrenoceptor-adenylate cyclase complex.
D017878:4,4'-Diisothiocyanostilbene-2,2'-Disulfonic Acid; D012856:4-Acetamido-4'-isothiocyanatostilbene-2,2'-disulfonic Acid / Q000031:analogs & derivatives / Q000494:pharmacology*; D000316:Adrenergic alpha-Agonists / Q000378:metabolism*; D000818:Animals; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D004837:Epinephrine / Q000494:pharmacology; D006160:Guanosine Triphosphate / Q000502:physiology*; D066298:In Vitro Techniques; D007668:Kidney / Q000187:drug effects / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects / Q000378:metabolism*; D012964:Sodium / Q000502:physiology*; D013267:Stilbenes / Q000494:pharmacology*; D015016:Yohimbine / Q000037:antagonists & inhibitors / Q000378:metabolism
D000316:Adrenergic alpha-Agonists; D011942:Receptors, Adrenergic, alpha; D013267:Stilbenes; D012856:4-Acetamido-4'-isothiocyanatostilbene-2,2'-disulfonic Acid; D015016:Yohimbine; D006160:Guanosine Triphosphate; D012964:Sodium; D017878:4,4'-Diisothiocyanostilbene-2,2'-Disulfonic Acid; D004837:Epinephrine