There are four principle protein targets with which drugs can interact: enzymes (e.g. neostigmine and acetyl cholinesterase), membrane carriers (e.g. tricyclic antidepressants and catecholamine uptake-1), ion channels (e.g. nimodipine and voltage-gated Ca 2þ channels) and receptors. This article is concerned with the receptor and describes the dynamics of drug-receptor interaction, agonists, antagonists, partial agonists and inverse agonists, efficacy and potency. Key definitions are shown in Table 1.
b-Opioids mobilize Ca2 from intracellular stores in undifferentiated NG108-15 cells, but the mechanism involved remains unclear. Therefore, we examined the effect of [n-Pen2'5Jenkephalin on inositol 1,4,5-trisphosphate formation in these cells. [n-Pen2'5]enkephalin caused a dose-dependent (EC 50 = 3.1 nM) increase in
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