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Aribit (Aripiprazole) tablets. Aripiprazole, sold under the brand names Abilify and Aristada, among others, is an atypical antipsychotic. [8] It is primarily used in the treatment of schizophrenia and bipolar disorder; [8] other uses include as an add-on treatment in major depressive disorder and obsessive–compulsive disorder (OCD), tic disorders, and irritability associated with autism. [8]
Aripiprazole lauroxil. Aripiprazole lauroxil, sold under the brand name Aristada, is a long-acting injectable atypical antipsychotic that was developed by Alkermes. [3][4][5] It is an N-acyloxymethyl prodrug of aripiprazole that is administered via intramuscular injection once every four to eight weeks for the treatment of schizophrenia. [3][4 ...
Unlike antagonist antipsychotics, which require only 65% to 70% D2 receptor occupancy to be effective, aripiprazole receptor binding at effective antipsychotic doses is 90% to 95%. Since aripiprazole has an intrinsic activity of approximately 30% (i.e., when it binds, it stimulates the D2 receptor to about 30% of the effect of dopamine binding ...
EC 50 is a measure of concentration, expressed in molar units (M), where 1 M is equivalent to 1 mol / L. The EC 50 of a graded dose response curve therefore represents the concentration of a compound where 50% of its maximal effect is observed. [4] The EC 50 of a quantal dose response curve represents the concentration of a compound where 50% ...
In competitive inhibition, an inhibitor that resembles the normal substrate binds to the enzyme, usually at the active site, and prevents the substrate from binding. [8] At any given moment, the enzyme may be bound to the inhibitor, the substrate, or neither, but it cannot bind both at the same time. During competitive inhibition, the inhibitor ...
In biochemistry and pharmacology, the Hill equation refers to two closely related equations that reflect the binding of ligands to macromolecules, as a function of the ligand concentration. A ligand is "a substance that forms a complex with a biomolecule to serve a biological purpose" (ligand definition), and a macromolecule is a very large ...
In general, molecular binding is an interaction between molecules that results in a stable physical association between those molecules. Cooperative binding occurs in a molecular binding system where two or more ligand molecules can bind to a receptor molecule. Binding can be considered "cooperative" if the actual binding of the first molecule ...
In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist. A neutral antagonist has no activity in the absence of an agonist or inverse agonist but can block the activity of either; [ 1 ] they are in fact sometimes called blockers (examples ...