PHA 4107 Lecture Notes - Lecture 17: Coniine, Tm1, Respiratory Arrest
12 Jul 2018
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Coniine: socrates died by drinking a cup of hemlock, hemlock contains coniine, symptoms, drowsiness, paresthesias, weakness, ataxia, nausea, profuse salivation and bradycardia -> tachycardia -> death due to respiratory arrest from paralysis of respiratory muscles and central depression. Type of drug receptor: drugs produce effects by interacting with cell receptors, by far, most ligands (drugs/neurotransmitters) bind to membrane proteins; some agents act directly on membrane lipids/dna. Tm1 close to tm7: t3 mediates drug-receptor interaction: effector molecule is guanine nucleotide binding protein (g protein) Ligand & voltage-gated ion channels: drugs also target these membrane transport proteins, voltage-gated ion channels do not have an endogenous ligand (as ligand- gates ion channels do) but open or close as a function of membrane voltage potential. Neurotransmitter transporters: 12-transmembrane domain proteins: transfer neurotransmitter molecules out of synapse and back into neuron, many drugs known as reuptake inhibitors target these transport proteins. Certain antineoplastic agents: lipids and phospholipids membrane receptors, eg.
