About inverse agonism, true is:
Ans. b (Binds to the same receptor binding-site as an agonist for that receptor but exerts the opposite pharmacological effect). (Ref. KDT, Pharmacology, 6th ed., p 41)# Receptor agonists, antagonists and inverse agonists bind to the same receptor types:DefinitionAgonistsincrease the inhibitory transmitter GABA potencyInverse agonistsdecrease GABA potencyAntagonistsblock action of agonists and antagonists# An inverse agonist is an agent which binds to the same receptor binding-site as an agonist for that receptor but exerts the opposite pharmacological effect. Inverse agonists are effective against certain types of receptors (e.g. certain histamine receptors/GABA receptors) which have intrinsic activity without the acting of a ligand upon them (also referred to as 'constitutive activity'.)# One particular example is R015-4513 which the inverse agonist of the benzodiazepine class of drugs.# Gabapentin acts by facilitation of GABA mediated CT channel opening. It does not block GABA receptors. Substances called Beta carboline which also bend this receptor cause stimulation anxiety, increased muscle tone and convulsions. They are inverse agonists of benzodiazepine receptors.
Action on the target receptors is similar to that of agonist
Binds to the same receptor binding-site as an agonist for that receptor but exerts the opposite pharmacological effect
Effective against receptors having intrinsic activity without acting of a ligand upon them
None
General Pharmacology