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Home >> Industrial and Microbial Biotechnology >>Drug Discovery and Drug Designing >> Drug Designing through Blocking Hormone Receptors

Drug designing through blocking hormone receptors

Drugs have also been produced through a study of receptor molecules that are responsible for the disease, followed by identification of chemicals that will block. such receptors. Utilizing this strategy, atleast two drugs were developed by Dr. James Black (of UK), who shared with Drs. G. Elion and G. Hitchings (of USA), the 1988 Nobel Prize for Medicine. These two medicines are briefly described in the following text.

Propranolol.

This drug is widely used for treating heart disease and high blood pressure. Heart diseases result due to the presence (in excess) of hormones norepinephrine and epinephrine, due to their role in contraction and relaxation of cardiac muscles. These hormones act through two receptors α and β. The drug Propranolol is a blocker of receptor β and relaxes the heart muscles. It has been shown that the drug not only cures the heart diseases but reduces the death rate of heart disease survivors by 25%. The drug is also used for treatments of angina pectoris and high blood pressure. Obviously by blocking the receptor β, the drug inhibits the activity of hormones which act through a receptor molecule.

Cimetidine.

This drug is anti-ulcer and is used for treatment if ulcers. Ulcers result from acid production due to histamine release in the stomach and therefore attempts were made to treat these ulcers through anti-histamines that were earlier used to combat respiratory allergies. These antihistamines proved ineffective for ulcer treatment and James Black attributed this to use of receptors that were different in stomach lining and respiratory tract. He was able to characterize histamine receptor of stomach lining and called it H2 receptor, which is blocked by the drug Cimetidine, thus leading to healing of ulcers by preventing acid production due to blocking of histamine receptor. Therefore cimetidin markerd the beginning of a new era in ulcer treatment, since earlier ulcers, that did not heal had to be removed surgically.

 

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