Altering cell function by changing mem potential, enzyme activity, gene expression by interacting with receptors. Act like synthetic hormones.
Drugs can be agonists - produce an effect
Drugs can be antagonists - preventing an effect. Desensitised.
Studies ion channels. Measures current over the channel. (insert photo)
One receptor complex at a time.
Binary quantification, open/closed.
Agonists open channel, Partial agonists not as effective as they cause opening with less frequency
Some channels that open independently, antagonist will not affect this?
Using well plates, 96, 384, 1536. 1 cell per well, add different pharmacological agent to each cell, test response.
Gave rise to Imatinib, Human abl kinase
Identified 1st molecule, librium by chance, first synthesis, then phenotypic observation. No molecular knowledge of receptor.
Glutamate gated ion receptor. (excitatory). Common in CNS. Common in worms/parasites.
Structure: Stacked pentamer of protein subunits.