Intrinsic activity and effects of guanyl-5'-yl imidodiphosphate, Gpp(NH)p on the affinity of partial agonists to the muscarinic receptor.
The effects of a GTP analogue, guanyl-5'-yl imidodiphosphate, Gpp(NH)p on the inhibition of [3H]3-quinuclidinyl benzilate (QNB) binding by some partial agonists were studied with a microsomal fraction of longitudinal muscle of guinea-pig ileum and compared with the intrinsic activity of the partial agonists which was estimated in the longitudinal muscle of guinea-pig ileum. There was a good correlation between the inhibitory effects of Gpp(NH)p on the affinity of the partial agonists to muscarinic receptors and their intrinsic activity.
D000818:Animals; D006160:Guanosine Triphosphate / Q000031:analogs & derivatives*; D006165:Guanylyl Imidodiphosphate / Q000494:pharmacology*; D006168:Guinea Pigs; D008297:Male; D009132:Muscles / Q000378:metabolism; D010276:Parasympatholytics / Q000378:metabolism*; D011813:Quinuclidinyl Benzilate / Q000378:metabolism; D011976:Receptors, Muscarinic / Q000187:drug effects / Q000378:metabolism*
D010276:Parasympatholytics; D011976:Receptors, Muscarinic; D006165:Guanylyl Imidodiphosphate; D011813:Quinuclidinyl Benzilate; D006160:Guanosine Triphosphate