Sebastian Lazareno

TL;DR: Functional studies confirm that brucine analogs are allosteric enhancers of ACh affinity at certain muscarinic receptor subtypes.

TL;DR: It is suggested that these atypical ligands either bind to the two known spatially separated allosteric sites on muscarinic receptors with positive cooperativity or their binding to the common allosterics site modulates receptor-receptor interactions such that homotropic positive cooperateativity within a dimer or higher oligomer is generated.

TL;DR: It is concluded that the structure-binding relationships of the amilorides at the alpha(1A)- and alpha(2A)-adrenergic receptors are different, and the interactions of the fiveAmiloride analogs, but not the parent amILoride, with the alpha (1A)-adren allergic receptor are compatible with the presence of two (but not one) allosteric sites, and is thus more complex than that found for the alpha

TL;DR: The dissociation data fitted well to an equation derived from the ternary complex allosteric model with amiloride analogue concentration and time as two independent variables and rules out the possibility that theAmilorides are acting in a nonspecific fashion.

TL;DR: It is hypothesized that long‐lasting adenosine‐receptor‐G protein complexes are present in the CHO membrane preparations, and the existence of these complexes may rationalize the observed kinetics and the increase in 3H‐antagonist binding produced by GTP.