Diazepam exhibits a full agonist profile at benzodiazepine receptors. The experi

Question

Diazepam exhibits a full agonist profile at benzodiazepine receptors. The experimental drug, EXP, was found to produce the dose response curve shown below. Draw the structure of diazepam. Describe the probable efficacy of EXP at benzodiazepine receptors. Using an Allosteric (two-state) model explain how EXP interacts with benzodiazepine receptors. The NMDA receptor is a specific type of ionotropic glutamate receptor NMDA (N-methyl-D-aspartatn) is the name of a selective agonist that binds to NMDA receptors but not to other glutamate receptors. Dizocilpine (Dz) has the following effect on the dose-response of NMDA.

Explanation / Answer

Problem 3:

a). Diazepam is an axiolytic drug that acts through GABA A (gamma amino butyric acid reeptors) receptors. They bind at allosteric site and facilitate the opening of GABA channles thus, allowing more actions mediated by GABA (an inhibitory neurotransmitter).

The structure of benzodiazepm is given below.

(b) From the given graph, we can say that diazepam is acting as true agonist and the experimenta drug (EXP) is acting as inverse agonist. Its efficacy towards benzodiazepam receptors is same as that of diazepam.

(c) An inverse agonist exhibits more affinity towards the receptor binding site similar to an agonist, but produces opposite effects to that of an agonist. In this case, EXP is an inverse agonist.

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