High-affinity agonist-receptor

A single residue, aspartate 95, in the S opioid receptor specifies high affinity agonist binding. J Biol Chem 1993 268 23055-23058. 

High-Affinity Niacin Receptor GPR109A Agonists... 

Ionotropic glutamate receptors mediate fast excitatory neurotransmission in practically all areas of the central nervous system (CNS). They are also critical for both the induction and expression of synaptic plasticity, and have been implicated in diverse pathological conditions, such as epilepsy, ischemic brain damage, anxiety, and addiction. There are three subtypes of ionotropic glutamate receptors that are named after their high-affinity agonists as a-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA), N-1nethyl-D-aspartate (NMDA), and kainate (KA) receptors (1). 

Table 6.1 Biogenic amine binding GPCR antitargets and side effects mediated by high-affinity agonists and antagonists of the respective receptor. ...

Newell JG, Dunn SMJ. 2002. Functional consequences of the loss of high affinity agonist binding to gamma-aminobutyric acid type A receptors. Implication for receptor desensitization. J Biol Chem 277 (24) 21423. 

Brown RWB, Collins AC, Lindstrom 1, Whiteaker P (2007) Nicotinic a5 subunit deletion locally reduces high-affinity agonist activation without altering receptor numbers. 1 Neurochem 103 204-215... 

Effect of Guanine Nucleotides on High Affinity Agonist Binding to Membrane and Solubilized Receptor Preparations... 

Hausdorff, W. P., Hnatowich, M., O Dowd, B. F., Caron, M. G., and Lefkowitz, R. J. 1990. A mutation of the beta 2-adrenergic receptor impairs agonist activation of adenylyl cyclase without affecting high affinity agonist binding. Distinct molecular determinants of the receptor are involved in physical coupling to and functional activation of Gs. J. Biol. Chem. 265 1388-1393. 

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