Course: 15FALL-CHEM371 x uno.mrooms3.net/plugi c Duno.mrooms3.net/pluginfile.php
ID: 51393 • Letter: C
Question
Course: 15FALL-CHEM371 x uno.mrooms3.net/plugi c Duno.mrooms3.net/pluginfile.php/1040919/mod_resource/content/2/CHEM3710H1-F2015.pdf C Chegg.com o.mrooms3.net/pluginf x Problem 1 Briefly describe the difference between and IND application and a NDA. Problem 2 Define the following terms a) Orphan disease d) druggable e) dossier b) Orphan receptor c) Data-mining Problem 3 Anandamide is the endogonous ligand of the cannabinoid system and intimately involved in cell signaling associated with pain and inflamation. Elevated levels of anandamide are believed to have therapeutic value for the treatment of eating and sleep disorders as well as pain relief. Propose "druggable" targets that woud be useful in treating: a) sleep disorders, b) Inflamatory bowel disease. Breifly explain your target(s) selection Anadamide Cell Signalling CB1 Receptor (central nevous system) Cannabinoid Receptors CB2 Receptor (peripheral nervous system, gastrointestinal system) cox-2 enzyme rostaglandin ain inflammation) anandamide FAAH enzyme cox-1 enzyme arachardonic acid_COX-2enzyme p arach ardonic acid prostagandin (pain, inflammation) MGL enzyme FAAH enzyme cox-2 enzyme prostaglandn (oain, inflammation) glyceryl esters 2-arachidonoylgly cerolp Problem 4 All of the drug candidates listed below failed to make it to the market. Indicate point in the drug discovery/development pipeline that the drug candidates probably failed a) A cholesterol lowering drug candidate was found to lead to a high incidence of breast tumors in -d» TO .111 3:44 PM 9/7/2015Explanation / Answer
The drug Anandamide is a neurotransmitter of cannabinoid system and it can affect both CNS and PNS. The PNS has CB2 cannabinoid receptors for Anandamide binding and CNS has CB1 cannabinoid receptors.
The Anandamide binds to these receptors and involved in the regulation of pleasure and neural generation. From the given the Anandamide signalling pathway, it can inactivate COX-enzymes (both 1 and 2), which are responsible for production of prostaglandins. These prostaglandins cause the pain and inflammation.
So, the probable target for sleep disorders is CB2 cannabinoid receptors. This is because sleep disorder, like Peripheral Neuropathy occur due to anomalies in PNS. Inflammatory bowel syndrome is caused due to inflammatory prostaglandins; therefore the probable target for inflammatory bowel syndrome is FAAH enzyme and COX enzymes.