Question

Given what you know about the pharmacophore of morphine (ie draw the new compound) that will convert the compound from an agonist (morphine) to an antagonist (your experimental compound).

Answer 1

Morphine, C17H19NO3,:

It is the most bounteous of opium's 24 alkaloids, representing 9 to 14% of opium-concentrate by mass. Named after the Roman lord of dreams, Morpheus, who likewise turned into the divine force of sleep, the medication morphine, fittingly enough, numbs torment, changes mind-set and prompts rest. Less prominent and less specified impacts incorporate queasiness, regurgitating and diminished gastrointestinal motility. (It's an incredible constipator, and in Guerin's work of art, Isis is maybe presenting to Morpheus a purgative.) Morphine and its related engineered subordinates, known as opioids, are so far magnificent at dulling incessant or alleged "moderate" torment, however lamentably they are all physically addictive. Amid the American Civil War, 400 000 fighters got to be dependent on morphine.Both morphine and its hydrated frame, C17H19NO3.H2O, are sparingly solvent in water. In five liters of water, just a single gram of the hydrate will break down. Thus, pharmaceutical organizations create sulfate and hydrochloride salts of the medication, both of which are more than 300 times more water-solvent than its parent particle. While the pH of a soaked morphine hydrate arrangement is 8.5, the salts are acidic. Since they get from a solid corrosive however powerless base, they are both at about pH = 5; consequently,in maufacturing stage,the morphine salts are blended with little measures of NaOH to make them reasonable for infusion,

The three dimensional structure of morphine is interesting. It comprises of five rings, three of which are around in a similar plane. The other two rings, including the nitrogen one, are each at right edges to the next trio.

Opioid analgesics, including morphine, codeine, levorphanol, heroin and basically less comparative medications, for example, meperidine all have a fragrant ring and a quaternary carbon iota connected to a tertiary amine amass by two other carbon iotas. This is known as the morphine manage, however it ought to be called attention to that the majority of the opioids beneath additionally have a methyl aggregate joined to a nitrogen molecule.

All the more imperatively and unexpectedly, going astray from the morphine govern has prompted to the production of much more grounded opioids, for example, fentanyl and its ester-subsidiary, carfentynyl. These particles have tertiary carbons and for every situation the molecule is not connected to a sweet-smelling bunch.

Substitute morphine's methyl amass with a propenyl gathering, and you make nalorphine, a rival which counters morphine's belongings. Likewise, hydromorphone, a ketone form of morphine five times more effective than its parent particle turns into the rival hydromorphone by a similar substitution of a CH3 with a CH2CH=CH2 aggregate. All the more for the most part, morphine's b-phenylethylamine unit (basically what I simply portrayed less the quaternary carbon iota) is additionally found at the last part of enkephalin particles. Enkephalins are littler adaptations of endorphins, which are created actually in the cerebrum, pituitary and different tissues, where they act particularly like opium's particles.

Morphine follows up on a particular receptor of nerve cells. All the more particularly numerous such receptors are found in the spinal line's substantia gelatinosa, an area where torment signs are initially prepared. The engineering of the morphine receptor is the thing that manages the morphine run the show. There is a level part that ties to the sweet-smelling ring, a hole that draws in the two carbon particles and an anionic site that obliges the tertiary nitrogen molecule. Whenever morphine or another agonist ties to the receptor, the cell film's fondness for sodium particle changes. This in the long run lessens the arrival of neurotransmitters from the influenced neurons. Specialists found out about morphine's method of activity by applying it and different sedatives within the sight of opponents, Na+ liking was reestablished and intestinal constrictions which had dropped steeply shot up once more.