Select one compound (drug or toxicant) that targets one of the three receptor types(G-protein coupled receptor pathway, A receptor tyrosine kinase pathway, An ion channel pathway ) and discuss the following for the selected compound:
The name of the receptor involved
The type of ligand that the drug or toxicant presents:
Agonist, antagonist
Are there natural ligands that interact with the receptor? If so explain the interaction.
Provide a brief explanation of the mechanism of the cellular response upon ligand binding to the receptor (i.e what signal transduction mechanisms occur). Refer to Fig 6.3 on page 105 in Hacker for an example.
How does the cellular response translate into a physiological response? What are the intended target tissue(s)? Are there any reported examples for the drug/toxicant acting on an off-target site?
Have there been any toxicology studies that assessed the dose response relationship of the compound? Provide data on TD50, LD50 and TI if you were able to find it. If not available, please note that.
There are so many drugs and/or toxicants which inhibit either GPCR or tyrosine kinase or ion channels. For example atropine, morphine, salbutamol etc. bind to GPCR, tyrosine kinase inhibitor binds to receptor tyrosine kinase and there are many ion channel blockers which interact with ion channels.
Here we shall discuss about Calcium channel-blocker.
The name of the drug is Amlodipine.
Its an antagonist for calcium channel.
The natural ligand for this ion channel is calcium.
Mechanism of action of amlodipine is that when it binds to calcium channels present in heart, it blocks calcium influx into cardiac smooth muscle cell and vascular smooth muscles. Hence prevents their contraction.
This is used for relaxation of smooth muscle in vascular system and heart.
Thank you.
Select one compound (drug or toxicant) that targets one of the three receptor types(G-protein coupled receptor pathway, A receptor tyrosine kinase pathway, An ion channel pathway ) and discuss the fol...