Schild equationIn pharmacology, Schild regression analysis, based upon the Schild equation, both named for Heinz Otto Schild, are tools for studying the effects of agonists and antagonists on the response caused by the receptor or on ligand-receptor binding. Dose-response curves can be constructed to describe response or ligand-receptor complex formation as a function of the ligand concentration. Antagonists make it harder to form these complexes by inhibiting interactions of the ligand with its receptor.
MuscimolMuscimol (also known as agarin or pantherine) is one of the principal psychoactive constituents of Amanita muscaria and related species of mushroom. Muscimol is a potent and selective orthosteric agonist for the GABAA receptors and displays sedative-hypnotic, depressant and hallucinogenic psychoactivity. This colorless or white solid is classified as an isoxazole. Muscimol went under clinical trial phase I for epilepsy, but the trial was discontinued. Muscimol is one of the psychoactive compounds responsible for the effects of Amanita muscaria intoxication.
Desensitization (medicine)In medicine, desensitization is a method to reduce or eliminate an organism's negative reaction to a substance or stimulus. In pharmacology, drug desensitization refers to two related concepts. First, desensitization may be equivalent to drug tolerance and refers to subjects' reactions (positive or negative) to a drug reducing following its repeated use. This is a macroscopic, organism-level effect and differs from the second meaning of desensitization, which refers to a biochemical effect where individual receptors become less responsive after repeated application of an agonist.
AutoreceptorAn autoreceptor is a type of receptor located in the membranes of nerve cells. It serves as part of a negative feedback loop in signal transduction. It is only sensitive to the neurotransmitters or hormones released by the neuron on which the autoreceptor sits. Similarly, a heteroreceptor is sensitive to neurotransmitters and hormones that are not released by the cell on which it sits. A given receptor can act as either an autoreceptor or a heteroreceptor, depending upon the type of transmitter released by the cell on which it is embedded.
Indirect agonistIn pharmacology, an indirect agonist or indirect-acting agonist is a substance that enhances the release or action of an endogenous neurotransmitter but has no specific agonist activity at the neurotransmitter receptor itself. Indirect agonists work through varying mechanisms to achieve their effects, including transporter blockade, induction of transmitter release, and inhibition of transmitter breakdown. Reuptake inhibition Cocaine is a monoamine transporter blocker and, thus, an indirect agonist of dopamine receptors.
Space-filling modelIn chemistry, a space-filling model, also known as a calotte model, is a type of three-dimensional (3D) molecular model where the atoms are represented by spheres whose radii are proportional to the radii of the atoms and whose center-to-center distances are proportional to the distances between the atomic nuclei, all in the same scale. Atoms of different chemical elements are usually represented by spheres of different colors.
