Medicinal Chemistry with Dr. Al-Horani
Pharmacodynamics and Pharmacokinetics with Dr. Williams
A little bit of everything!
Medicinal Chemistry and Pharmacology with Dr. Sirohi
Know your SARs!
100
This amino acid is the biochemical precursor to the neurotransmitter Acetylcholine
What is L-Serine?
100
This type of ligand has affinity to a receptor, but does not elicit a response by the receptor, lacking efficacy.
What is an antagonist?
100
This term is the proportion given dosage of drug which reaches systemic circulation, represented by the letter F
What is bioavailability?
100
This division of the autonomic nervous system is responsible for the "Fight" response
What is the Sympathetic nervous system?
100
A methyl substituent on the alpha carbon of a cholinomimetic drug has increased selectivity toward this type of cholinergic receptor
What is nicotinic receptor selectivity?
200
This drug's ability to cross the Blood Brain Barrier and reach the central nervous system makes it a useful reversible AChE inhibitor in this disease state
What is Alzheimer's disease?
200
This is the Dose at which 50% of the population achieves the desired response
What is the ED50 or median effective dose?
200
Coactivators recruit this enzyme in order to acetylate histones
What is HAT?
200
This muscarinic cholinergic receptor subtype is widely expressed in the CNS, heart, and smooth muscle, and has an inhibitory cellular response.
What are M2 receptors?
200
This drug's methyl group on its beta carbon allows it to hold specificity toward this type of receptor
What is mAchR?
300
The pharmacophore of antimuscarinic drugs consists of these three essential characteristics
What is a positive nitrogen, a 2 to 6 atom spacer, and an unsubstituted ring?
300
This hyperpolarizing neurotransmitter has an inhibitory effect on neurons, and operates via a Ligand Gated Chloride ion channel
What is y amino butyric acid or GABA
300
Hemicholinium blocks this reuptake receptor
What is the CHT1 Choline reuptake receptor
300
This clinically used depolarizing muscular blocker has an extremely short duration of action (5-10 minutes)
What is succinylcholine?
300
Nicotinic agonists utilizes this type of substituted and unprotonated amine in order to cross the blood brain barrier
What are secondary and tertiary amines?
400
Cevimeline, a non-classical direct cholinomimetic, undergoes these two types of inactive metabolites by CYP450 hepatic enzymes
What are S and N-oxide metabolites?
400
This presystemic metabolism can cause certain drugs to be nearly completely destroyed after administration, prior to reaching the systemic circulation and the site of action
What is First Pass effect?
400
This alcohol based cholinesterase inhibitor is used as a diagnostic agent for Myasthenia Gravis
What is Edrophonium?
400
This side effect of depolarizing neuromuscular blockers is due to the faciculation (muscle twitches) prior to paralysis
What is Myalgia?
400
In regards to nicotinic receptor blockers, when the distance between the two Quaternary ammonium groups is greater than 10 carbons, it is considered this type of blocker
What is a neuromuscular blocker?
500
This drug is used in combination with atropine as an antidote to this class of drug
What is 2-PAM (pralidoxime) + Atropine?
500
This happens to the concentration of a drug that is metabolized by CYP450 when CYP450 is being induced
What is a decrease in drug concentration?
500
Darifenacin, an antimuscarinic drug commonly used in urinary disorders, has specificity toward this type of receptor
What is an M3 muscarinic receptor?
500
As it pertains to the mechanism of action of depolarizing neuromuscular blockers, this phase of the blockade is the result of desensitization despite repolarization
What is Phase II (2) blockade?
500
This is the chemical class of reversible AchE inhibitors (as seen above)
What are Aryl Carbamates?