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The Hill equation is useful for determining the degree of cooperativity of the ligand (s) binding to the enzyme or receptor. The Hill coefficient provides a way to quantify the degree of interaction between ligand binding sites. [5] The Hill equation (for response) is important in the construction of dose-response curves.
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]
The first description of cooperative binding to a multi-site protein was developed by A.V. Hill. [4] Drawing on observations of oxygen binding to hemoglobin and the idea that cooperativity arose from the aggregation of hemoglobin molecules, each one binding one oxygen molecule, Hill suggested a phenomenological equation that has since been named after him:
The binding affinity is the concentration needed to occupy 50% of the sites; the lower this value is the easier it is for the ligand to occupy the binding site. The binding of the ligand to the receptor at equilibrium follows the same kinetics as an enzyme at steady-state ( Michaelis–Menten equation ) without the conversion of the bound ...
Half maximal inhibitory concentration (IC50) is a measure of the potency of a substance in inhibiting a specific biological or biochemical function. IC 50 is a quantitative measure that indicates how much of a particular inhibitory substance (e.g. drug) is needed to inhibit, in vitro, a given biological process or biological component by 50% ...
Partial agonist. In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic effects—when both a full agonist and partial agonist are present, the partial ...
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 ...
By Bhanvi Satija and Michael Erman (Reuters) -The U.S. FDA approved Bristol Myers Squibb's schizophrenia drug on Thursday, providing patients with a treatment option that reduces symptoms of the ...