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]]>7-Chloro-1,3-dihydro-3-hydroxy-1-methyl-5-phenyl-1,4-benzodiazepin-2-one
Temazepam is a benzodiazepine sedative-hypnotic.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 300.74 g/mol |
2 | Physical appearance | Solid |
3 | Melting point | 119-121°C |
4 | Octanol/water partition coefficient | 2.19 |
5 | Solubility | 164 mg/L |
6 | Presence of ring | Diazepine, benzene |
7 | Number of chiral centers | 1 |
i. Temazepam binds nonspecifically with benzodiazepine receptors BNZ1.
ii. It coupled with GABAA receptors and increases the GABA affinity for the GABA receptor.
iii. This results in opening of the chloride channel and thus, causes hyperpolarization of the cell membrane which prevents further excitation of the cell.
i. 7-chloro-5-phenyl-1,3-dihydro-3-hydroxy-1-methyl-5-phenyl-2H-1,4-benzodia- zepin-2-on-4-oxide undergoes methylation of the nitrogen of the amide group in the first position of the benzodiazepine ring by using dimethylsulfate to give 1-methyl-7-chloro-5-phenyl-1,3-dihydro-2H-1,4-benzodiazepin-2-on-4-oxide.
ii. The product undergoes acetylation using acetic anhydride to produce 1-methyl-3-acetoxy-7-chloro-5-phenyl-1,3-dihydro-2H-1, 4-benzodiazepin-2-one.
iii. Alkaline hydrolysis results in removal of acetyl group to give temazepam. [2]
Temazepam is used for:
Side effects of Temazepam are:
MCQ
Q.1 Match the following with correct SAR of the drug Temazepam-
i. Electronegative group at 7-position of the ring A | A. Increase in functional anxiolytic activity |
ii. Substitutions at 6, 8 or 9 position with electronegative group on ring A | B. Decreases the functional anxiolytic activity |
iii. When Heterocycles used as ring A | C. maximum activity is observed |
iv. When the proton accepting group is present on the 2-position of the ring B | D. Poor pharmacological activity |
a) i-D, ii-C, iii-A, iv-B
b) i-D, ii-B, iii-A, iv-C
c) i-B, ii-D, iii-C, iv-A
d) i-A, ii-B, iii-D, iv-C
Q.2 Correct sequence for the True/False for correct IUPAC names of the drug can be?
a) TFTF
b) TTFF
c) FTTF
d) FFTT
Q.3 Physical appearance of Temazepam is?
a) Red-brown crystalline powder
b) Solid
c) Green granular form
d) None of these
Q.4 Temazepam shows its mechanism of action through biding with which receptor?
a) BNZ1
b) Pain receptors
c) Light receptor
d) None of the above
Q.5 Which amongst the following is a therapeutic use of drug temazepam?
a) Sedative before surgery
b) Treatment of Insomnia
c) Treatment of cancer
d) All of the above
Q.6 Which of the following drug and their classification are correct?
I. Temazepam: Barbiturate sedative-hypnotic
II. Loxapenes: Benzazepenes
III. Thiothixene: Benzodiazepenes
IV. Haloperidole: Butyrophenone
a) I
b) I, III
c) II, IV
d) II, III
Q.7 Type of ring present in the structure of temazepam?
a) Diazepine
b) Triazole
c) Pyrimidine
d) Both a) and c)
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1-d
2-d
3-b
4-a
5-b
6-c
7-d
The post TEMAZEPAM Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
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