Medicinal | Lec 5-8 Assessment | 12Q
Was developed by Bioisosteric modification
Has minimal CNS side effects
Has marked antiserotonin activity
sa potent second generation antihistamine
The 3-phenolic OH greatly enhanced activity
It is a ureceptor antagonist and k receptor agonist
It belongs to benzomorphans
It shows hallucinogenic side effect results from its binding to a non- opioid receptor
Au+ is attached to Sulfur
Au+ is easily converted to its oxidized form
Monovalent gold
Orally bioavailable
Carboxamide NH Contributes to increasing its acidity
4-hydroxy group is not essential for activity
It is an isostere of piroxicam
Pyridyl nitrogen contributes to enolate stabilization
Is a powerful agonist at the 3 types of opioid receptors
Its mirror image has a completely different pharmacological action
It is an active metabolite of an opioid drug
Has 2 stereocenters, only R,R isomer is an opioid agonist
Ri = CH3, R2 = H, R3= heteroaryl
R1= H, R2= H, Ra= heteroaryl
Ri = CH3, R2= CH3, Ra= heteroaryl
R, = H Rz= CH3, R3= heteroaryl
Which of the following is/are true about coxibs
All of the following are correct
The sulfamoyl or sulfonyl moiety provides target selectivity
Are class of selective COX-1 inhibitors
Show Gl side effects that hindered their potential clinical usefulness
Binds to delta receptors causing hallucination
Is a weak K agonist
Is a weak µ agonist
Has powerful analgesic activity with low risk of addiction
Belongs to biologic DMARDs
Is an interleukin-1 antagonist
Stabilizes mast cells
Decreases expression of B-cells and T-cells
5-fluoro substituent improved metabolic stability
Indene ring enhanced anti-inflammatory potency
Sulfinyl group decreased side effect and increased water solubility
2-CH3 group ensures trans like conformation
Ethylene diamine derivatives
Ethanolamine ethers
Propylamine analogs
Phenothiazine Derivatives
Binds weakly to all types of opioid receptors
Cannot bind to µ receptor
Its side effect results from its binding to a non-opioid receptor
s a powerful k agonist
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