Final Part 1 Flashcards
What is the principle cholinomimetic?
Acetylcholine
What enzyme creates acetyl choline by adding an acetyl group onto choline from Acetyl CoA?
Choline acetyltransferase
What is the limiting factor for choline acetyltransferase?
Choline
What enzyme inactivates ACh?
Acetylcholinesterase (AChE)
What amino acid must be attached to AChE to be activated?
Serine and Histidine
What process inactivates ACh?
Transesterification
What binds to AChE?
Serine and Histidine
What are the two types of cholinergic receptors?
Muscarinic and Nicotinic
What drug is selective to M1 receptors and was the only muscarinic antagonist to block gastric acid secretion and did not block other agents?
Pirenzapine
What do M1 receptors inhabit?
Neuronal tissue
Brain
presynaptic of autonimic ganglia
Exocrine glands
What disease is related to M1 receptors?
Alzheimer’s Disease
Memory and learning
Where are M2 receptors in the body?
Postganglionic membranes in ANS
Smooth Muscle
Heart
Exocrine Glands
What are M2 receptors known to do?
Decrease heart rate and contractility of the heart
Where are M3 receptors located in the body?
Brain
Smooth muscle and secretory glands
What do M3 receptors do?
Decrease neurotransmitter release
Contraction and secretion
Where are M4 receptors located?
Smooth muscle
Secretory glands
What do M4 receptors do?
Inhibit Calcium channels
Where are M5 receptors located?
Brain
Peripheral tissue
What are the two main requirements for SAR of Muscarinics?
Esteratic site
Anionic site
Accomodates the acetyl ester Oxygen through H bonding
Quat amine
What must at least two of the 4 side groups be on the quat amine of muscarinics?
CH3
What are the four classes of Cholinergis and anticholinergics?
Muscarinic agonist
Acetycholinesterase Inhibitors
Muscarinic agonists
Muscarinic antagonists
What is the pKa of a phenol?
9-10
Is a phenol acidic or basic?
Weakly acidic
What is the pKa of carboxylic acid?
2-5
