Ontology highlight
ABSTRACT:
SUBMITTER: Enuo He
PROVIDER: BIOMD0000000082 | BioModels | 2006-09-26
REPOSITORIES: BioModels
Thomsen W J WJ Jacquez J A JA Neubig R R RR
Molecular pharmacology 19881201 6
The functional significance of high affinity agonist binding to receptors that interact with guanine nucleotide regulatory proteins has remained controversial. Preincubation of human platelet membranes with the full alpha 2-agonist UK 14,304 in the absence of GTP increases the potency of the agonist to inhibit adenylate cyclase in a pre-steady state (15-sec) assay. The EC50 after preincubation (6 +/- 1 nM) is within a factor of 2 of the high affinity Kd for [3H]UK 14,304 binding determined under ...[more]