Discussion of two agonies BU006 and BU007

Discussion of two agonies

According to the aim of the experiment, the two agonists, BU006 and BU007, were compared in the process of determining the most potent among them in activating the bladder muscarinic receptors. As shown the potency test carried for the two drugs, it was realized that BU007 was more potent than BU006. The analysis of the two drugs acme to a conclusion based on the findings that the EC50 of BU006 and that of BC007 were 125ug/25ml and 40 ug /25ml respectively. In the same way, their percentage measurements of the receptor occupancy required in the production of half the total response of both the drugs were 35.33% and 8.04% respectively. According to the results, considering also that the percentage measures for their receptors to produce total response were found to be 97.76% and 95.63% respectively, it meant that lesser receptors are required for BC007 in order to produce maximum response.

According to Mehdia et all. (2011), it is true to conclude that the extra receptors are treated as spare or reserve receptors. Okamoto et al. (2002) also affirms that BU006 seemed to bind 97.76% of the receptors to reach maximum response, meaning 2.24% are the reserve receptors. In comparison to the BU007, that needed to be bound with 95.63% to attain maximum response, left only 4.375 reserve receptors. Despite the fact that same receptor type of a drug has the same affinity, the number of receptors present and different qualities of the pathways may affect the affinity (Mehdia et al. 2011).

As a measure of potency of a drug, EC50 determines the connection between response and affinity of a particular drug on particular tissue. According to Choppin (2002), lower EC50 reflects more potency of the drug; hence low concentration was required in the production of half the total response. Choppin (2002) also illustrated that the difference in the EC50 of the same drug were attributed difference in the number of receptors, different second messenger pathways, as well as different breakdown rate of a drug on other tissues. Okamoto et al. (2002) also indicated that in the event of a piece of a very reactive gall bladder with high receptor density becomes exposed to BU006 or BU007, EC50 remained the same since receptors exceeded the required number to activate maximum response.

Okamoto et al. (2002) affirms that EC50 decreased, when drugs were broken down in a particular tissues, since less drug were required to activate sufficient receptors to produce EC50. The best way therefore to determine the breakdown of the drug in the tissues, is by considering the level of EC50 of the drug before and after the enzyme inhibitors are added. More concentration of EC50 would be required to attain half the total response, thereby changing the EC50 curve to the right. Failure to break down the drug in particular sites however made the EC50 curve to be constant. It was also found out that breaking down the drug by enzymes shifted the EC50 curve to the left since enzymes were inhibited, and less concentration of the drug are required for half achievement of maximum response ( Choppin 2002).

Lack of efficiency in the use of the computer programmes that measure contractile response, and errors in preparation of the bicarbonate solutions are some of the human mistakes that have brought inconsistencies of data. However, in the end, the experiment made a general conclusion that BU007 drug was more potent than BU006 because BU007 attained a lower EC50.