The post NALORPHINE Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>17-allyl-7,8-didehydro-4,5α-epoxymorphinan-3,6α-diol.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 311.4 g/mol |
2 | Physical appearance | Crystals from diethyl ether |
3 | Melting point | 208.5°C |
4 | Solubility | Slightly soluble in water; sparingly soluble in ether |
5 | Octanol/water partition coefficient | 1.86 |
6 | Presence of ring | Piperidine, cyclohexene, tetrahydrofuran, phenyl |
7 | Number of chiral centers | 5 |
Nalorphine acts on to opioid receptors:
i. On mu-receptors it shows antagonistic effects
ii. On kappa receptors, it shows high-efficacy agonistic effects.
SAR for opiates can be summarized as follows:
i. Heroin is processed with cyanogens bromide to give N-cyano derivative.
ii. The N-cyano derivative is hen hydrolyzed by a solution of hydrochloric acid to transform into N-demethylated morphine which is also called as normorphine.
iii. The secondary amine group of normorphine undergoes alkylation with allylbromide to give the desired nalorphine.[1]
Nalorphine is used for:
Side effects Nalorphine are:
Q.1 What can be the correct IUPAC nomenclature of Nalorphine?
a) 17-allyl-7,8-didehydro-4,5α-epoxymorphinan-3,6ß-diol
b) N-phenyl-N-[1-(2-phenylethyl)piperidin-4-yl]propanamide
c) N-[1-(2-phenylethyl)piperidin-4-yl]propanamide
d) 17-allyl-7,8-didehydro-4,5α-epoxymorphinan-3,6α-diol
Q.2 Which amongst the following statements is/are incorrect related to the SAR of opiates?
I. On replacement of the methyl group from tertiary nitrogen by hydrogen atom, activity increases.
II. On replacement of N-CH3 by NCH2CH2Ph, activity decreases by 14 times.
III. When the methyl group of tertiary nitrogen replaced by N-allyl/methallyl/propyl, the compound so formed acts like the Drug antagonist
a) I, II
b) I, II, III
c) III
d) I
Q.3 Nalorphine can be synthesized from alkylation of ___________ by allylbromide?
a) Morphine
b) Normorphine
c) Codeine
d) Pentazocine
Q.4 Side effects of drug Nalorphine is/are?
a) Anxiety
b) Hallucinations
c) Confusions
d) All of the above
Q.5 Match the following drugs with their correct molecular weight.
i. Nalorphine | A. 311.4 gm/mol |
ii. Phenacemide | B. 184.49 gm/mol |
iii. Loxapine | C. 178.19 gm/mol |
iv. Enflurane | D. 327.8 gm/mol |
a) i-A, ii-D, iii-C, iv-B
b) i-B, ii-A, iii-D, iv-C
c) i-A, ii-C, iii-D, iv-B
d) i-D, ii-C, iii-A, iv-B
Q.6 An example of drug from class Mixed-opioid antagonist is?
a) Gabapentin
b) Nalorphine
c) Levallorphan
d) Secobarbital
Q.7 The type of ring system found in the structure of Nalorphine is?
a) Piperidine
b) Furan
c) Cyclohexane
d) All of the above
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ANSWERS
1-d
2-a
3-b
4-d
5-c
6-b
7-d
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