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Lecture 30 – Cannabinoid Drug Discovery
Elements of drug discovery
o Stage 1: First Vital Steps
Therapeutic target: what disease are you treating?
Molecular target: what molecule is responsible? (receptors, channels,
transporters, enzymes, ligands)
Lead discovery: what drug (lead compound) will act on the molecular target?
Biological system: a system to screen potential leads
o Stage 2: Discover Optimum Molecule
Discover and compare PK profile with existing drugs
o Requirements for a new drug
Selectivity (increases benefit:risk ratio, yohimbine)
Act on various CB receptors (there are also endogenous CB ligands)
There are clinical applications for CBs
Also commercial benefit
o Used as a painkiller for over 5000 years
o Targets include modifying enzymes, uptake receptors, and metabolism of
Anandamide arachidonic acid (enzyme = FAAH)
2-AG arachidonic acid (enzyme = MAG lipase/FAAH)
Receptors: Human CB1 and CB2 receptors
Only CB1 can affect CNS and neurotransmitters
Agonists inhibit neurotransmitters decrease pain, increase appetite,
elevate mood, impair memory, etc.