An Agonist Response To An Antagonist

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Abstract: An antagonist is a drug that blocks the response to an agonist drug. An agonist is a drug that elicits a response when it is administered to a tissue. The aim of the investigation was to compare the actions that the agonist, carbachol and antagonist, atropine has at muscarinic receptors on rat ileum. A concentration-response curve was determined with a cumulative concentration of agonist, expressed as a sigmoidal curve with an sub-maximal response (EC70) value of 5.5x10-6 M. As the agonist concentration increased to 5x10-6 M, the magnitude of the tissue response increased. This was approximately linear between 20% and 80% of the maximum response. The percentage reduction from the EC70 was determined in the presence of the antagonist, …show more content…

Gut baths can be used to produce quantitative responses and convert those responses to chemical or electrical stimulations by the use of an isometric transducer and these stimulations are shows on a computer. Agonists are compounds that produce a response when administered to a particular tissue. The response that are recorded are directly proportional to the concentration of drug administered. Antagonists are compounds that interact with a set of receptors and form a complex, but no response is elicited. When an effective concentration of the antagonist is administered, this complex prevents the agonist from binding to the receptor and can therefore reduce the agonist response (Dale et al., 2012). The agonist, carbachol and antagonist, atropine are used to show the different responses that is has on a rat ileum. Carbachol is a cholinergic agonist as it binds to muscarinic and nicotinic receptors for acetylcholine and stimulates them, causing a smooth muscle contraction. It is not absorbed well in the gastrointestinal tract and does not cross the blood-brain barrier. Atropine is non-selective muscarinic receptor antagonist and is absorbed well in the gastrointestinal tract. It is a reversible competitive antagonist of the muscarinic acetylcholine receptors and blocks the effects of carbachol, the agonist occupancy at a given agonist concentration is reduced as the receptor can only accommodate one molecule at a time (Dale et al., 2012). The aim of …show more content…

A two centimeter piece of rat ileum was cut and placed in a Krebs-Henseleit physiological saline in a petri dish and was kept oxygenated. A needle was threaded with cotton at one end of the ileum and three knots were done to form a small loop. A needle was threaded on the other end of the ileum, a knot was done and two equal lengths of cotton were left. The first loop formed was hooked at the bottom of the tissue holder and lowered into the organ bath. The two equal lengths of cotton were then tied to the hook at the bottom of the isometric transducer and the tension was adjusted to 0.5g. The tissue was rinsed several times and let to equilibrate for 15 minutes. The program LabChart 7 was used to record the trace. A carbachol solution (1x10-2 M) was diluted to concentrations of 5x10-3, 5x10-4, 5x10-5 and 5x10-6. An atropine solution (1x10-3 M) was diluted to concentrations of 5x10-4, 5x10-5, 5x10-6 and 5x10-7. In order to construct an agonist concentration response curve, carbachol concentrations were added to the gut bath in a cumulatively dosing regime (Table 1). After a single concentration was added and a response has elicited, the second dosage was only added once the response reaches a plateau. Once the maximum contraction of the tissue was observed, the tissue was rinsed and allowed to recover. These results obtained (the response in grams) were used to calculate the maximum response

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