PHRM20001 Lecture 2 Drug Targets

Question	Answer
Nifedipine	- Blocks Calcium Channels - Reduces blood vessel constriciton - Reduces Blood Pressure
Fluoxitine	- Blocks 5-HT reuptake - Prolongs effects of 5-HT
Aspirin	- Inhibits Cyclo-Oxygenase (COX) - Reduces inflammatory response - Binds covalently
L-Dopa	- Increases synthesis of Dopamine
Morphine	- Activates opioid receptors for pain relief
Naloxone	- Opioid receptor antagonist - Used for heroin overdoses
Ionotropic Receptors	Agonists bind and directly regulate the opening of the ion channel
Metabotropic Receptors	Agonist binding causes series of intracellular events to indirectly produce effects
Nicotinic Receptors	Located on skeletal muscle, and at the preganglionic junction of Para and Sympa neurons. Ach binds and causes Sodium Channels to open
Kinase-Linked Receptors	Agonist binding causes the activation of the cytoplasmic domain that has Kinase Activity
Cytoplasmic Receptors	Receptors for lipid-soluble agonists Agonist-receptor binds and enters the nucleus Regulates gene expression e.g. Glucocorticoid Receptors
G-Protein Coupled Receptors	Largest receptor family Linked to an effector protein by a G-protein e.g. Muscarinic Receptors
GPCR: Adenylate Cyclase	Produces cAMP which has activation activity in the cell
GPCR: Phospholipase C	Catalyzes PIP2 into Inositol Triphosphate and DAG Increases intracellular Calcium levels in the cell Used by Beta Adrenoceptors and Alpha1

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	Created by Dan McArthur about 8 years ago