Drug Action 2 Exam 2 Practice

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• In drug design, what does CADD stand for?
• Phase 4 timing: Phase 4 occurs after which event and before which?
• Acetylcholine is primarily found in which locations?
• Aspartic acid 311 participates in which type of interaction in the muscarinic binding site?
• Structure-activity relationship in medicinal chemistry is best described as
• Which of the following is a listed use of muscarinic selective agonists?
• Nicotinic receptors are found in autonomic ganglia and at the neuromuscular endplate, and they are also present in which gland?
• What is done in Phase 4 of drug development?
• What is an example of sequential blocking?
• In the discovery stages, which step follows Define Lead?
• Can you increase or decrease the distance of the ethylene bridge in acetylcholine?
• Which statement best defines the structure-activity relationship?
• How are hits extracted from plants or animals?
• In what year was diacetylmorphine (heroin) introduced as a safer pain reliever?
• What compounds serve as precursors in the synthesis of choline?
• What percentage of compounds that show suitable biological activity go through clinical trials and reach the market?
• What is the crystal structure of HIV protease?
• Which of the following is NOT listed as an example of a synthetic drug?
• Which physiological effect is associated with muscarinic receptor activation in the heart?
• What percentage of hits are of animal origin?
• Nicotinic selective agonists are best described as targeting which receptors?
• What do muscarinic M2 receptors do?
• Which phases may not be undergone by all drugs?
• Which muscarinic receptor subtype is associated with increased salivary gland secretion?
• What is the primary focus of Phase 4?
• What is done in the preclinical stage of drug development?
• What percentage of hits are of herbal (plant) origin?
• Tetrodotoxin is a selective blocker of which ion channels?
• What is done in phase 2 of drug development?
• Which databases are used in computer-aided drug design?
• Which two enzymes are responsible for hydrolyzing acetylcholine in the body?
• Which of the following is NOT one of the three recommended actions when starting a new research project?
• What is high-throughput screening?
• Bethanechol enantiomers?
• Which function is associated with central neuronal nicotinic receptors?
• In screening hit origins, which origin contributes the largest share?
• Carbachol is primarily used for which condition?
• What step in the folic acid synthesis process do sulfonamides and PAS block?
• What distance between the acetyl O and N of acetylcholine supports activation of nicotinic receptors?
• Which modification increases acetylcholine's stability to gastric acid and esterases?
• Which of the following is a step in the drug discovery process?
• What do muscarinic M3 receptors do?
• What best describes lead optimization in drug discovery?
• Which of the following statements about the uses of muscarinic receptor agonists is true?
• What percentage of hits are of mineral origin?
• What are some natural products/body substances obtained from plants?
• Identify the concept that links a compound's chemical features to its potency across a family of related molecules.
• In Phase 2, what is determined to evaluate safety margin?
• Which drug is available orally as a capsule for xerostomia associated with Sjogren's syndrome?
• What can you do to increase the selectivity of acetylcholine for nicotinic receptors?
• Which term describes the ability to acetylcholine to activate multiple receptors?
• Which statement about methacholine is true?
• Which strategy is used to address shortcomings of a lead compound?
• Which substitution would still be an active agonist albeit weaker when nitrogen is replaced with a heteroatom (as described above)?
• What is possible using data generated in lead optimization?
• Which modification leads to Methacholine's intermediate half-life?
• Which percentage of hits are of synthetic origin?
• Cyclosporine A is an immunosuppressant obtained from which source?
• In methacholine, which statement about enantiomers is true?
• Important to remember about pilocarpine?
• What was the first commercially available semisynthetic morphine derivative?
• Where are nicotinic receptors found?
• What storage instruction would you give a patient taking pilocarpine?
• Which is stronger, ionic or H-bonding?
• Nicotinic selective agonists are used in the treatment of which condition?
• Which modification increases nicotinic receptor selectivity?
• Which compound has the longest half-life among Acetylcholine, Carbachol, and Methacholine?
• What occurs with alpha-methyl substitution of acetylcholine?
• In the muscarinic binding site, which amino acid participates in van der Waals interactions?
• Ritonavir boosting: In a fixed-dose combination approved in 2000, ritonavir is used to boost the bioavailability of which protease inhibitor?
• What percentage of hits are biotechnology (macromolecules) origin?
• What is the typical time from conception to approval of a new drug?
• What is done in Phase 5 of drug development?
• What is acetylcholine degraded by?
• Bethanechol receptor selectivity?
• Which approach is used to optimize cholinergic agonists by increasing receptor selectivity?
• Which muscarinic receptor subtypes are associated with facilitating dopamine release?
• Replacing 1, 2, or all 3 methyl groups on the nitrogen of acetylcholine with hydrogen atoms would result in:
• Which parameter sets are applied to hits during drug discovery screening?
• Cevimeline hydrochloride is?
• In computer-aided drug design, what do SBDD and LBDD stand for?
• What are product line extensions?
• Cevimeline hydrochloride availability and use?
• What is an example of target-centered drug design?
• Which step describes the release of acetylcholine from the presynaptic nerve?
• What was the target in the drug design that created Ritonavir?
• What happens if Lipinski's Rule of Five is not met?
• In 1853, Henry Wellcome attempted to convert morphine into what?
• Which statement best describes the relative durations of drug discovery and drug development?
• What are the products of acetylcholine hydrolysis by acetylcholinesterase?
• What is the effect of increasing shield size on acetylcholine's stability and activity?
• What step in the folic acid synthesis process does trimethoprim block?
• Which of the following describes carbachol's qualities?
• Tryptophan participates in which type of interaction in the muscarinic binding site?
• Where is butyrylcholinesterase located in the body?
• Which of the following could lead to termination during lead optimization related to DNA risk?
• How potent is the R enantiomer of beta-methyl substitution of acetylcholine (methacholine) compared to the S enantiomer?
• Bethanechol clinical use after surgery?
• Which statement best describes acetylcholine hydrolysis?
• Which statement about Phase 1 is correct?
• Cevimeline hydrochloride works by activating which receptor to stimulate salivary secretion?
• Asparagine 617 participates in which type of interaction in the muscarinic binding site?
• Which of the following is an example of a natural product obtained from marine sources?
• What are the different phases of drug development?
• Which property makes bethanechol suitable for oral administration?
• Pilocarpine is what?
• Which approach is used to identify lead compounds efficiently and at reasonable cost in early drug discovery?
• The step blocked by sulfonamides and PAS is which step?
• What distance between the acetyl O and N of acetylcholine supports activation of muscarinic receptors?
• Which structural feature is essential to maintain cholinergic activity in acetylcholine analogs?
• Which drugs utilize the theory of antimetabolites?
• Which statement best reflects the nature of a lead compound?
• Which atom in acetylcholine acts as a hydrogen bond acceptor in muscarinic receptor binding?
• What do muscarinic M1 receptors do?
• What moieties are essential to acetylcholine?
• In what year was ritonavir approved for marketing by the FDA?
• When starting a new research project, which of the following is recommended?
• Carbachol's receptor activation profile is best described as:
• Which tissues contain nicotinic receptor subtypes?
• Where are muscarinic receptors found?
• What percentage of new compounds investigated may show suitable biological activity?
• In the context of screening, which best describes hits?
• How long does drug discovery usually take?
• P-aminosalicylic acid (PAS) stands for what?
• Which compound is an example of an antimetabolite drug?
• Pilocarpine indications?
• In drug discovery terminology, what are hits?
• Replacing the quaternary nitrogen in acetylcholine with arsenic, phosphorus, or sulfur would result in:
• Which of the following substitutions would still yield an active cholinergic agonist albeit weaker?
• In the muscarinic binding site, which amino acid participates in hydrogen bonding?
• What is done in phase 3 of drug development?
• What is medicinal chemistry concerned with?
• Which statement correctly describes a quality of acetylcholine?
• Which methyl acts as a steric shield to protect the ester group in methacholine?
• Elongating the methyl group to an ethyl group on the ester of acetylcholine would result in what?
• Which statement best describes acetylcholine degradation and recycling?
• What enzyme resynthesizes acetylcholine?
• Which amino acids are involved in the degradation of acetylcholine?
• Choline esters of aromatic or higher molecular weight acids serve as what?
• What was diacetylmorphine (heroin) introduced as?
• How long does drug development take?
• What do muscarinic receptors control?
• What significant regulatory action occurred in 2000 regarding ritonavir?
• According to Lipinski's Rule of Five, an orally active drug should fulfill at least how many of the listed criteria?
• What is acetylcholine broken down into?
• What important function do nicotinic receptors in skeletal muscles control?
• Which step comes immediately after preclinical testing?
• What are two types of computer-aided drug design (CADD)?
• What is the role of the IND in clinical development?
• Replacing all three methyl groups on the nitrogen of acetylcholine with larger alkyl groups would result in:
• What did Henry Wellcome do in 1853?
• In the plant/animal extraction process, what term describes chemically modifying a natural product to create an active ingredient?
• To increase muscarinic receptor selectivity of acetylcholine, which modification is suggested?
• Carbachol's property of being resistant to hydrolysis and non-selective means:
• What is the theory of antimetabolites based on?
• Which drug is described as a natural alkaloid muscarinic agonist?
• In the muscarinic binding site, which amino acid participates in ionic bonding?
• What are some natural products/body substances obtained from microorganisms?
• When does a drug typically receive FDA approval in the drug development process?
• Which receptor type is activated at the neuromuscular junction?
• Which methods are used for synthesis of synthetic hits?
• Which receptor type mediates secretion of catecholamines in the peripheral nervous system?
• What percentage of hits are of micro-organism and fungi origin?
• Where is butyrylcholinesterase primarily located?
• Which step occurs immediately before human clinical trials in the drug development timeline?
• Which natural product comes from animal sources?
• What is the typical estimated cost of bringing a new drug from conception to approval?
• Which drug is used to stimulate GI motility after surgery?
• What was the first antibiotic?
• How should pilocarpine be stored?
• Where is acetylcholine found in the body?
• Generic drug products are defined as?
• Penicillin is an example of which therapeutic category?
• Which modification contributes to Carbachol's longer half-life compared to acetylcholine?
• By inhibiting acetylcholinesterase, what effect occurs?
• What is the MOA of sulfonamides?
• Specialty drug products are defined as?
• Which two cholinesterases are present in humans?
• Which drug groups compete with PABA for receptor binding?
• What event marks the submission of a formal application for drug approval to the FDA?
• What happens immediately after ACh binds to postsynaptic receptor?
• Early drug discovery typically identifies what?
• Which statement about muscarinic M1 receptor effects on dopamine and locomotion is true?
• Which carbon is methylated to increase muscarinic selectivity in acetylcholine derivatives?
• What happens to choline after acetylcholine is hydrolyzed?
• What serves as a precursor in the synthesis of acetyl-CoA?
• Which of the following is part of the discovery stages and strategies?
• Replacing one methyl group on the nitrogen of acetylcholine with an ethyl or propyl group would result in:
• Veber's parameters focus on which aspects to assess oral bioavailability?
• What would replacing one of the hydrogens on the urethane nitrogen with a methyl group result in?
• What are the different nicotinic receptor subtypes?
• What is done in phase 1 of drug development?
• What was the first drug used for treating cancer as alkylating agent?
• If you replace the nitrogen on acetylcholine with sulfur, what is the expected activity relative to acetylcholine?
• What is bethanechol best described as?
• What do muscarinic M4 receptors do?
• What are the two methods of acetylcholine hydrolysis?
• What important function do peripheral neuronal nicotinic receptors control?
• What is a lead compound?
• Which feature supports ionic interactions in the active conformation of acetylcholine?
• Which compound has the shortest half-life among Acetylcholine, Carbachol, and Methacholine?
• Which of the following is NOT a common reason to terminate at lead optimization?
• What would an AChE inhibitor act as?
• High-throughput screening is performed in which setting?
• What do muscarinic M5 receptors do?
• Which interaction occurs in the muscarinic receptor binding site related to methyl groups?
• What should occur at the end of lead optimization?
• In Phase 5, which populations might be studied?
• What is sequential blocking?
• What important function do central neuronal nicotinic receptors control?