4234524
Description
Flashcards by Conrad Lewis, updated more than 1 year ago
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Created by Conrad Lewis
almost 10 years ago
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| Question | Answer |
| absorption | the movement of a drug from its site of administration to the bloodstream |
| active pharmaceutical ingredient (API) | the chemical in an administered drug that is responsible for its biological activity |
| adverse effect | an undesired effect of a drug |
| alkaloid | a molecule found in a natural source with a basic nitrogen and a level of structural complexity |
| allosteric site | a site on an enzyme or receptor that is not bound by a substrate or response-causing ligand. Noncompetitive inhibitors (enzymes) and noncompetitive antagonists (receptors) bind at allosteric sites. |
| alpha-helix (α-helix) | a type of secondary structure in which the protein backbone assumes a spiral conformation |
| amide linkage | the amide bond formed between individual amino acid residues in a protein backbone |
| analgesic | pain killer |
| analogues | compounds related to a lead and prepared in an attempt to optimize the desired properties of the lead |
| apparent volume of distribution (Vd) | a hypothetical volume of plasma that is required to contain a specified drug dose |
| area under curve (AUC) | the area beneath a Cp-time curve. AUC is a measure of drug exposure. |
| arsenicals | an early synthetic drug class that was used to treat syphillis and certainly protozoan infections |
| assay | a general term for testing the biological activity of a molecule. An assay may be performed either in vivo or in vitro. |
| beta-sheet (β-sheet) | a type of secondary structure in which the protein backbone assumes a fairly flat shape formed by a back-and-forth flow of the chain |
| binding energy | the free energy of binding between a drug and its target based on the dissociation equilibrium constant between the drug and target (K) |
| bioavailability (F) | the fraction of an drug dose that actually reaches the bloodstream from its site of administration |
| bioequivalence testing | an abbreviated clinical trial used by generic manufacturers to show that a generic product is biologically similar to an existing branded drug |
| bioisosteres | isosteres that specifically preserve electronic and hydrogen bonding characteristics when one group is exchanged with another |
| bolus | an amount of drug that is administered, typically intravenously, in a single burst |
| Caco-2 cells | a cell that is used in cell permeability assays |
| cell permeability | the ability of a molecule to passively cross cell membranes. High cell permeability indicates that a molecule will likely be well absorbed from the digestive system. |
| central compartment | blood plasma |
| Cheng-Prussoff equation | an equation that can convert an IC50 value to a Ki value |
| classical isosteres | isosteres that specifically preserve steric bulk when one group is exchanged with another |
| clearance (CL) | the removal of a drug from the bloodstream, normally by either excretion or metabolism. The variable CL has units of either mL/min or mL/min/kg. |
| combinatorial chemistry | a method, often automated, for making large collections of molecules using varied building blocks around a molecular scaffold |
| compartment model | a method for describing how a drug distributes into the various tissues of an organism |
| competitive inhibitor | an enzyme inhibitor that binds at the active site of an enzyme. Competitive inhibitors decrease the affinity of an enzyme for its substrate, and therefore increases Km. |
| composition of matter | a type of patent that covers new chemical substances, especially drugs |
| compound library | a collection of molecules that can be used to test for biological activity against a protein target |
| concensus scoring | the use of multiple scoring methods in an in silico screen to increase the relability of the resulting hits |
| cytochrome P-450 (CYP) | a superfamily of enzymes, mostly associated with the liver, that perform many oxidative metabolic reations on drugs |
| depolarization | the flow of ions across a cell membrane from the side with high concentration to the side with low concentration |
| desensitization | an abnormally low response to a drug, often because of downregulation of a receptor |
| directed combinatorial chemistry | the use of combinatorial chemistry to generate libraries focused upon the SAR around a lead |
| distribution | the transport of a drug to and from its site of action by the bloodstream |
| distribution phase | the time period during which an absorbed drug reaches its full volume of distribution |
| docking | the computer simulation of a molecule's binding to a target protein |
| downregulation | a decrease in receptor expression by a cell in response to a continuous, high-level stimulation of the receptor |
| drug-like | a description of a compound with a molecular weight between 400 and 500 g/mol and a lipophilicity (log P) of near 5 |
| drug product | the entire administered drug. For orally delivered drugs, the drug product includes the drug substance and all the binders, dyes, and fillers in the pill. |
| drug substance | the active material within a drug product |
| drug-target residence time | the half-life of a drug-receptor complex as it equilibrates between its bound and unbound state |
| elimination | any process that causes a decrease in the concentration of a drug in the bloodstream. Both metabolism and excretion are elimination processes. |
| elimination phase | the period of time after a drug has reached its full volume of distribution and is being cleared from the plasma |
| elimination rate constant (kel) | a rate constant that describes rate of elimination for a drug. Elimination rate constants normally correspond to first-order processes and have units of inverse time. |
| endogenous ligand | a ligand that is found naturally in the body |
| enzyme (E) | usually a protein, a biological catalyst that converts a substrate to a product |
| enzyme-substrate complex (E-S) | the aggregate substance formed by binding between an enzyme and its substrate |
| excretion | the removal of waste from the body. For drugs, excretion is normally associated with the generation of urine by the kidneys through the filtration of blood. |
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