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]]>(RS)-1-[4-(2-Methoxyethyl)phenoxy]-3-[(propan-2-yl)amino]propan-2-ol.
Metoprolol is a selective ß1-adrenergic antagonist
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 237.36 g/mol |
2 | Physical appearance | Solid |
3 | Melting point | 120°C |
4 | Solubility | Water solubility is 0.06M |
5 | Octanol/water partition coefficient | 2.15 |
6 | Presence of ring | Benzene |
7 | Number of chiral centers | 1 |
i. Reaction of 4-(2-methoxyethyl)phenol and epichlorohydrin in aqueous alkaline condition produces epoxide.
ii. It is distilled under high vacuum for purification.
iii. Epoxide is then treated with isopropylamine in isopropyl alcohol at reflux to yield metoprolol. [3]
Metoprolol is used for treatment of:
Side effects of metoprolol are:
Q.1 Match the following with correct SAR of the drug metoprolol-
i. Increasing side chain length | A. Prevents appropriate binding of the required functional groups to the same receptors side. |
ii. Aryloxypropanolamines are | B. Stimulates appropriate binding of the required functional groups to the same receptors side |
C. Less potent than aryloxyethanolamines | |
D. More potent than aryoxyethanolamines |
a) i-A, ii-C
b) i-A, ii-D
c) i-B, ii-C
d) i-B, ii-D
Q.2 Correct sequence for the True/False for correct IUPAC names of the drug can be?
a) TFFT
b) TFTF
c) TTFF
d) TTFT
Q.3 Number of chiral centers present in the structure of metoprolol?
a) 0
b) 1
c) 2
d) 3
Q.4 Mechanism of action of metoprolol is based on?
a) Blocking of α1-adrenergic receptors
b) α1-adrenergic agonism
c) ß1-adrenergic antagonism
d) None of these
Q.5 Which amongst the following is not a therapeutic use of drug metoprolol?
a) Angina
b) Hypertension
c) Heart failure
d) Ocular hypertension
Q.6 Which of the following drug and their classification are correct?
I. Metipranolol: nonselective ß-adrenergic antagonist
II. Metoprolol: selective ß1-adrenergic antagonist
III. Amphetamine: nonselective α-adrenergic agonist
IV. Clonidine: Mixed acting sympathomimetics
a) I, III
b) I, II
c) II, III, IV
d) I, II, III, IV
Q.7 What chemical compound can be reacted with isopropylamine in isopropyl alcohol to produce metoprolol?
a) Epoxide
b) Benzene
c) Hydroquinone
d) Epichlorohydrine
1-b
2-a
3-b
4-c
5-d
6-b
7-a
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