PCL201H1 Lecture Notes - Lecture 30: Hypotension, Fatty Acid Amide Hydrolase, Relative Risk
14 Sep 2016
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Document Summary
Elements of drug discovery: stage 1: first vital steps. Molecular target: what molecule is responsible? (receptors, channels, transporters, enzymes, ligands) Biological system: a system to screen potential leads: stage 2: discover optimum molecule. Discover and compare pk profile with existing drugs: requirements for a new drug. Act on various cb receptors (there are also endogenous cb ligands) Also commercial benefit: used as a painkiller for over 5000 years, targets include modifying enzymes, uptake receptors, and metabolism of endocannabinoids. Anandamide arachidonic acid (enzyme = faah) 2-ag arachidonic acid (enzyme = mag lipase/faah) Only cb1 can affect cns and neurotransmitters. Agonists inhibit neurotransmitters decrease pain, increase appetite, elevate mood, impair memory, etc. Current therapeutic targets for cb agonists: suppression of nausea and pain, stimulate appetite. Possible therapeutic targets: ms, inflammatory pain, asthma, cancer, etc. Evidence from animal data, anecdotal data, (insufficient) clinical data: acute pain: mouse tail flick test.
