Drug-receptor Interactions
Know general characteristics of signal-transducing receptors:
Bind to a ligand (drug or endogenous molecule)
Participate in a signaling cascade
Distinguish from non-receptor-mediated drug action
Graded or Dose-Response effects (vs. all-or-none)
Understand “occupational theory” of drug action
Molecular basis (ligand-receptor interaction)
Mathematical description
Occupational theory: Response = Max Response * [D]/(Kd +[D])
Shapes of dose-response curves
Significance of Kd ligand dissociation constant half-max binding when [D] = Kd
Understand the difference between Potency and Efficacy
Know the general mechanism of drug-receptor interaction, and recognize dose-response curves for:
Agonists
Antagonists
Competitive
Non-competitive
Partial Agonists
Inverse Agonists
Biochemical Classification of Receptors: Know the general characteristics and mechanism of action for:
Membrane-bound receptors
G protein-coupled
Ligand-regulated ion channels
Tyrosine Kinase-linked
Guanyl cyclase-linked
(Know some specific examples of each type)
Cytosolic/nuclear “soluble” receptors
Understand basic mechanisms of receptor regulation
Desensitization, homologous or heterologous
Spare receptors
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OVERVIEW OF AUTONOMIC PHARMACOLOGY
PHARMACOLOGICAL (NOT ANATOMICAL) DIVISION OF PNS: Cholinergic vs. Adrenergic
Cholinergic: All preganglionic and parasympathetic postganglionic Acetylcholine is the neurotransmitter at ganglia, nmj, and muscarinic tissue synapses
Adrenergic: Postganglionic sympathetic neurons (most). Norepinephrine is the transmitter
Exceptions:
Cholinergic transmission in sympathetic system - all ganglia, adrenal medulla, sweat glands
(muscarinic)
Dopaminergic innervation in sympathetic system - renal blood vessels
Important steps of Neurotransmission: Synthesis, storage, release, recognition, and metabolism. Know where drugs can intervene,