PCL201H1 Lecture Notes - Lecture 30: Hypotension, Fatty Acid Amide Hydrolase, Relative Risk

5 views2 pages
14 Sep 2016
School
Course
Professor

For unlimited access to Class Notes, a Class+ subscription is required.

PCL201
Winter 2014
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
It works
Selectivity (increases benefit:risk ratio, yohimbine)
Suitable PK
Safety
Cannabinoids
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
endocannabinoids
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.
Unlock document

This preview shows half of the first page of the document.
Unlock all 2 pages and 3 million more documents.

Already have an account? Log in

Get access

Grade+
$10 USD/m
Billed $120 USD annually
Homework Help
Class Notes
Textbook Notes
40 Verified Answers
Study Guides
1 Booster Class
Class+
$8 USD/m
Billed $96 USD annually
Homework Help
Class Notes
Textbook Notes
30 Verified Answers
Study Guides
1 Booster Class