1answer.
Ask question
Login Signup
Ask question
All categories
  • English
  • Mathematics
  • Social Studies
  • Business
  • History
  • Health
  • Geography
  • Biology
  • Physics
  • Chemistry
  • Computers and Technology
  • Arts
  • World Languages
  • Spanish
  • French
  • German
  • Advanced Placement (AP)
  • SAT
  • Medicine
  • Law
  • Engineering
Nesterboy [21]
3 years ago
14

Based on the definitions of pharmacophore and privileged structure, outline essential structural features a 1,4-dihyrdopyridine

must possess for effective Ca2+ channel blocking capability. (ex. functional groups, presence of electron-donating or electron-withdrawing moieties) 2. Why are the products of today's lab (dimethyl 1,4-dihydro-2,6-dimethylpyridine-3,5-dicarboxylate and diethyl 1,4-dihydro-2,6-dimethylpyridine-3,5-dicarboxylate) ineffective in this regard?
Biology
1 answer:
stiv31 [10]3 years ago
6 0

Answer:

Explanation:

Pharmacophore (pharmacology) - The molecular framework responsible for a drug's biological activity. According to IUPAC — A pharmacophore is the ensemble of steric and electronic features that is necessary to ensure the optimal supramolecular interactions with a specific biological target structure and to trigger (or to block) its biological response.

Privileged structures are defined as molecular frameworks which are able of providing useful ligands for more than one type of receptor or enzyme target by judicious structural modifications.

1) The 1,4-dihydropyridine ring is present in many biologically important molecules that acts as an important scaffold for cardiovascular drug - a calcium antagonists and although it is technically not considered as a pharmacophore, it is considered as a privileged structure.

1,4-Dihydropyridine (DHP), belongs to the class of calcium antagonist that inhibits the influx of extracellular Ca+2 through the L-type voltage-dependent calcium channels.

A positional substitution in the 4-position is feasible in the heterocyclic ring which in turn culminates in various calcium channel antagonist activities and this heterocyclic ring is the common feature for various pharmacological activities such as anti-inflammatory activity, analgesic activity,

antihypertensive, antianginal, antitumor, antitubercular activity and antithrombotic .

Position on the heterocyclic ring binds to the L-type channel and also to N-type channel on membranes.

2.) The bioisosteres are not a suitable bioisostere for the traditional C-4 aryl or heteroaryl substitution which is necessary for calcium ion blockage thereby inhibiting it to function with the mechanism shared above.

You might be interested in
What are the adaptations of bottle-nosed dolphins that allows them to thrive in the marine biome?.
3241004551 [841]

Answer:

Thermoregulation

Explanation:

  1. Decreased surface-to-volume ratio. The dolphin's fusiform body shape and reduced limb size decrease the amount of surface area exposed to the external environment.
  2. Increased insulation. Dolphins deposit most of their body fat into a thick layer of blubber.
  3. Heat exchange system.

5 0
2 years ago
A crayfish’s swimmerets are used only for swimming.<br> a. True<br> b. False
marta [7]
Its false because lobsters have swimmerets as well and they dont use them only for swimming
6 0
3 years ago
An individual sustained a closed head injury in a rock climbing accident. In the ER the RN elevates the head of the bed at 30 de
mote1985 [20]

Answer:

Answered below

Explanation:

Head injuries may be penetrating head injury or closed head injury.

A major concern for health professionals regarding intracranial injuries resulting from closed head traumas, is the management of intracranial pressure. Elevated intracranial pressure have negative effects on the brain and immediate management of raised intracranial pressure is important to avoid cerebral edema, intracranial hematoma, brain herniation and even death.

The usual procedures in the management of head injury include elevating the head to about 30 degrees. This position promotes cerebral venous drainage and decreases intracranial venous pressure and intracranial pressure as well.

This is helpful because when the patient is left in the horizontal position, the intracranial pressure becomes significantly higher and the have fatal consequences.

8 0
3 years ago
Which of the following would be true of heterochromatin but not of euchromatin?
Tanya [424]

I would choose the option D.

D. It remains tightly coiled at the G1 phase.

6 0
3 years ago
Which component of blood helps fight disease?
Pavlova-9 [17]
White blood cells fight disease
3 0
3 years ago
Read 2 more answers
Other questions:
  • 4. What are some of the hazards that domestic pets like dogs and cats can experience in regard to poisons? How are pets exposed
    5·1 answer
  • How do animal-like protists differ from plant-like protists?
    13·1 answer
  • How does semen travel to the egg?
    10·1 answer
  • How would the parasympathetic system help balance the sympathetic system?
    8·1 answer
  • Determine the genotypes of the parents if the father is blood type A the mother is blood type B the daughter is blood type O one
    13·1 answer
  • What type of unhealthful air population occurs when ozone near the ground mixes with other polluting gases?
    6·1 answer
  • What protects cells from the particles outside
    9·1 answer
  • Water reacts with sodium metal to produce sodium hydroxide and hydrogen
    14·1 answer
  • In a loudspeaker, ............... energy is converted into sound energy.
    10·1 answer
  • Study the cladogram. Which two organisms have dry skin? gorilla and shark shark and lizard lizard and tiger tiger and lamprey.
    12·1 answer
Add answer
Login
Not registered? Fast signup
Signup
Login Signup
Ask question!