The post NOREPINEPHRINE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>(R)-4-(2-amino-1-hydroxyethyl)benzene-1,2-diol.
Norepinephrine is a nonselective adrenergic agonist. [1]
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 169.18g/mol |
2 | Physical appearance | Present in colorless microcrystal form |
3 | Melting point | 217°C |
4 | Solubility | Very soluble in alkali and dilute HCL, slightly soluble in water, ethanol and diethyl ether. |
5 | Presence of ring | Benzene ring present |
6 | Number of chiral centers | 1 |
R1 substitution:
R2 substitution:
R3 substitution on the aromatic ring:
i. Catechol reacts with chloroacetic acid and POCl3 to give 4-chloroacetylcatechol.
ii. Norepinephrine is then obtained from 4-chloroacetylcatechol.
The drug used for the treatment of:
Some of the common side effects of norepinephrine are pain, burning, irritation, discoloration of skin, headaches, blurred visions, trouble breathing, no or little urination, blue nails and lips, uneven heart rate, numbness, weakness and cold feeling.
Q.1 What can be the correct IUPAC nomenclature of Norepinephrine?
a) (R)-4-(1-Hydroxy-2-(methylamino)ethyl)benzene-1,2-diol
b) (R)-4-(2-amino-1-hydroxyethyl)benzene-1,2-diol
c) (R)-3-[-1-hydroxy-2-(methylamino)ethyl]phenol
d) (R)-4-(2-amino-1-phenyl)benzene-1,2-diol
Q.2 Which amongst the following statements is/are incorrect related to the SAR of Norepinephrine?
I. Primary or secondary aliphatic amine separated by two carbons from a substituted benzene ring is essential for the high agonist activity
II. The hydroxyl substituted carbon must be in the L configuration for the maximal direct activity
III. When R1 is increased in size, activity of alpha receptors increases and activity of the beta receptors decreases.
IV. Activity of both alpha and beta receptors is minimum when R1 is methyl group.
a) I, II, III & IV
b) II, III & IV
c) II & IV
d) II & III
Q.3 Norepinephrine-
a) Acts on α-adrenergic receptors and functions as peripheral vaasoconstrictor
b) Acts on α-adrenergic receptors and functions as inotropic stimulator of the heart, and dilator of the coronary arteries.
c) Acts on ß-adrenergic receptors and functions as peripheral vasoconstrictor.
d) Both a) and b)
Q.4 The drug Norepinephrine is mainly used for?
a) Low blood pressure
b) High blood pressure
c) Myelomas
d) Prostate cancer
Q.5 Match the drugs with the correct classification.
i. Norepinephrine | A. Purine antagonist |
ii. Nafarelin | B. GnRH analogue |
iii. Etoposide | C. Non selective adrenergic agonist |
iv. Fludarabine | D. Epipodophyllotoxin |
a) i-C, ii-D, iii-B, iv-A
b) i-A, ii-D, iii-C, iv-B
c) i-C, ii-B, iii-D, iv-A
d) i-D, ii-C, iii-A, iv-B
Q.6 How many statements below are correct with respect to the side effects of the drug norepinephirine?
a) 1
b) 2
c) 3
d) 4
Q.7 The type of ring system found in norepinephrine?
a) Benzene
b) Naphthalene
c) Oxazophosphorine
d) No ring present
1-b
2-d
3-a
4-a
5-c
6-d
7-a
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