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Receptor theory is the application of receptor models to explain drug behavior. [1] Pharmacological receptor models preceded accurate knowledge of receptors by many years. [2] John Newport Langley and Paul Ehrlich introduced the concept that receptors can mediate drug action at the beginning of the 20th century.
For instance, an agonist will stabilize the active form of a pharmacological receptor. Phenomenologically, it looks as if the agonist provokes the conformational transition. One crucial feature of the model is the dissociation between the binding function (the fraction of protein bound to the regulator), and the state function (the fraction of ...
The fraction of bound receptors is known as occupancy. The relationship between occupancy and pharmacological response is usually non-linear. This explains the so-called receptor reserve phenomenon i.e. the concentration producing 50% occupancy is typically higher than the concentration producing 50% of maximum response. More precisely ...
Receptors of a particular type are linked to specific cellular biochemical pathways that correspond to the signal. While numerous receptors are found in most cells, each receptor will only bind with ligands of a particular structure. This has been analogously compared to how locks will only accept specifically shaped keys. When a ligand binds ...
A threshold model or linear no-threshold model may be more appropriate, depending on the circumstances. A recent critique of these models as they apply to endocrine disruptors argues for a substantial revision of testing and toxicological models at low doses because of observed non- monotonicity , i.e. U-shaped dose/response curves.
Binding curves showing the characteristically sigmoidal curves generated by using the Hill equation to model cooperative binding. Each curve corresponds to a different Hill coefficient, labeled to the curve's right. The vertical axis displays the proportion of the total number of receptors that have been bound by a ligand.
Beta blockers exert their pharmacological effect, decreased heart rate, by binding to and competitively antagonising a type of receptor called beta adrenoceptors. [1]In pharmacology, the term mechanism of action (MOA) refers to the specific biochemical interaction through which a drug substance produces its pharmacological effect. [2]
Major receptor types studied in pharmacology include G protein coupled receptors, ligand gated ion channels and receptor tyrosine kinases. Network pharmacology is a subfield of pharmacology that combines principles from pharmacology, systems biology, and network analysis to study the complex interactions between drugs and targets (e.g ...