Receptors as a drug target Unit- 1 general pharmacology (pc- 520) Priyansha singh m.s. pharm- pharmacology & toxicology (pc2021-14/226) Niper guwahati
introduction Drugs produce their therapeutic effects by producing biochemical / physical changes : in the target tissues of the host or the organisms which invade the host . These changes are due to physical and chemical properties of drug and the action on the drug targets namely ; ▪ Receptors ▪ Enzymes ▪ Carrier molecules ▪ Ion channels
introduction To get drug action, it is essential that:- 1 . Sufficient concentration of drug reaches the site of action 2. Remains there for a sufficient duration 3. The tissue is susceptible for drug action Magnitude of drug action is proportional to the concentration of drug at the site of action. Receptor mechanism is very important to understand the action and effect of a drug.
receptors component of a cell or organism which interacts with a drug and initiates the chain of biochemical events thus leading to the drug’s observed effects They have specific binding sites that are definite in size and shape Most are present on or near the membrane . Some lie in the enzymes or genes protein (polypeptide) in nature
History of receptors Langley and Ehrlich introduced concept of receptor Langley (1852 – 1925) Studied the effects of atropine against pilocarpine induced salivation in cats Postulated that there was a receptive substance in the nerve ending or gland cell with which both atropine and pilocarpine are capable of forming compounds. Ehrlich (1854 – 1915) observed that, certain dyestuffs acted selectively, staining some cells more deeply or in a different way from other cells suggested that drugs with selective actions on particular cells could be developed Introduced the term “receptor”
Some important terms related to receptors
Concept of cell signalling Process in which cells sense the extracellular stimuli through membranous or intracellular receptors , transduce the signals via intracellular molecules - Regulate the biological function of the cells.