Medicinal Chemistry Encyclopedia

 

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Data Lock. At a predetermined time and date, in a clinical trial (in accordance with the trial protocol) when the sponsor agrees they will not submit anymore patient data to support their NDA  (New Drug Application). This date and time is called Data Lock.

 

Data and Safety Monitoring Board (DSMB) board comprised of researchers who periodically review data from blinded, placebo-controlled trials. The researchers should be independent of the trials they are monitoring. A DSMB board has the authority to stop a trial if the toxicities are found or if the treatment is proved beneficial. These boards are also known as Independent Data-Monitoring Committee.

 

De novo design is the design of bioactive compounds by incremental construction of a ligand model within a model of the receptor or enzyme active site, the structure of which is known from X-ray or nuclear magnetic resonance (NMR) data.

 

Desensitization of a receptor mediated response, refers to the termination or diminution of the response despite continued or repeated application of the ligand.

 

Dipole results in molecules that carry no net charge yet, have a permanent charge separation due to the differences in the electronegativity of the atoms that compose it. Dipole moment is a vector that quantifies the resulting magnitude and direction of the charge asymmetry in a dipole.

 

Dispersion Forces (London Forces) are forces induced between neutral molecules by induced dipole-induced dipole interactions. These forces fall off very rapidly with distance, but can be significant in molecules in close proximity.

 

Dipole-Dipole Interactions are electrostatic interactions that occur when molecules with permanent dipoles interact.

 

Distomer is the enantiomer of a chiral compound that is the less potent for a particular action. This definition does not excude the possibility of other effect or side effect of the distomer (See also Eutomer).

 

Docking studies are molecular modeling studies aiming at finding a proper fit between a ligand and its binding site.

 

Dose-Escalation is a preliminary study in a clinical trial in which the amount of the drug is either periodically increased or increased with each new trial arm that is added. Used to determine how a drug is tolerated in people. Clinical Trial.

 

Double-blind study is a clinical study of potential and marketed drugs, where neither the investigators nor the subjects know which subjects will be treated with the active principle and which ones will receive a placebo.

 

Double prodrug (or pro-prodrug) is a biologically inactive molecule, which is transformed in vivo in two steps (enzymatically and/or chemically) to the active species.

 

Drug is any substance presented for treating, curing or preventing disease in human beings or in animals. A drug may also be used for making a medical diagnosis or for restoring, correcting, or modifying physiological functions (e.g., the contraceptive pill).

 

Drug disposition refers to all processes involved in the absorption, distribution metabolism and excretion of drugs in a living organism.

 

Drug-Drug Interaction refers to the effects that occur when two or more drugs are used together. Such effects include changes of absorption in the digestive tract, changes in rate of the drugs. breakdown in the liver, new or enhanced side effects and changes in the drugs. activity.

 

Drug latentiation is the chemical modification of a biologically active compound to form a new compound, which in vivo will liberate the parent compound. Drug latentiation is synonymous with prodrug design.

 

Drug targeting is a strategy aiming at the delivery of a compound to a particular tissue of the body.

 

Dual action drug is a compound which combines two desired different pharmacological actions at a similarly efficacious dose.

 

Dyspepsia refers to a digestive upset, which may include flatulence, heartburn, nausea or vomiting.

 

Dysphagia relates to difficulty in swallowing.

 

Dysplasia is abnormal changes or growth of cells and tissues.

 

Dyspnea is shortness of breath or difficulty in breathing.

 

Edema is the swelling caused by an abnormal accumulation of fluid in body tissues.

 

Efficacy describes the relative intensity with which agonists vary in the response they produce even when they occupy the same number of receptors and with the same affinity. Efficacy is the property that enables drugs to produce responses. It is convenient to differentiate the properties of drugs into two groups, those that cause them to associate with the receptors (affinity) and those that produce stimulus (Efficacy). This term is often used to characterize the level of maximal responses induced by agonists. In fact, not all agonists of a receptor are capable of inducing identical levels of maximal responses. Maximal response depends on the efficiency of receptor coupling, i.e., from the cascade of events, which, from the binding of the drug to the receptor, leads to the observed biological effect.

 

Electrophoresis is a phenomenon that results from the application of an electric field causing a relative motion of the surface and diffuse layer; the solvent is stationary and the particles move. The particles must be large enough to have a double layer associated with them. The velocity of the particles with respect to the field strength is the electrophoretic mobility.

 

Elimination is the process achieving the reduction of the concentration of a xenobiotic including its metabolism.

 

Endocytosis is the process of internalization of cell surface receptors or receptor ligand complexes. Typically, receptor or receptor ligand internalization is followed by dissociation and sorting in the endosome. The step is either followed by degradation in the lysosome or by recycling to the cell surface.

 

Enzyme is a macromolecule, usually a protein, which functions as a (bio) catalyst by increasing the reaction rate. In general, an enzyme catalyzes only one reaction type (reaction selectivity) and operates on only one type of substrate (substrate selectivity). Substrate molecules are transformed at the same site (regioselectivity) and only one or preferentially one of chiral a substrate or of a racemate is transformed (enantioselectivity[special form of stereoselectivity]).

 

Enzyme induction is the process whereby an (inducible) enzyme is synthesized in response to a specific inducer molecule. The inducer molecule (often a substrate that needs the catalytic activity of the inducible enzyme for its metabolism) combines with a repressor and thereby prevents the blocking of an operator by the repressor leading to the translation of the gene for the enzyme.

 

Enzyme repression is the mode by which the synthesis of an enzyme is prevented by repressor molecules. In many cases, the end product of a synthesis chain (e.g., an amino acid) acts as a feedback corepressor by combining with an intracellular aporepressor protein, so that this complex is able to block the function of an operator. As a result, the whole operation is prevented from being transcribed into mRNA, and the expression of all enzymes necessary for the synthesis of the end product enzyme is abolished.

 

Eosinophil is a type of granulocyte (see) thought to play a role in fighting parasites producing allergic reactions. Its name comes from these cells. absorption of the red dye eosin.

 

Erythrocyte is a red blood cell. The primary function of erythrocytes is to carry oxygen to cells.

 

Eudismic ratio is the potency of the eutomer relative to that of the distomer.

 

Eutomer is the enantiomer of a chiral compound that is the more potent for a particular action.

 

Expanded Access refers to the FDA procedures (compassionate use, parallel track and treatment IND see) that distribute experimental drugs to patients who are failing on currently available treatments for their condition and also are unable to participate in ongoing clinical trials.