What is the mechanism of action of triptans?
Mechanism of action. Their action is attributed to their agonist effects on serotonin 5-HT1B and 5-HT1D receptors in blood vessels (causing their constriction) and nerve endings in the brain, and subsequent inhibition of pro-inflammatory neuropeptide release, including CGRP and substance P.
How is phenacetin prepared?
Phenacetin may be synthesized as an example of the Williamson ether synthesis: ethyl iodide, paracetamol, and anhydrous potassium carbonate are heated in 2-butanone to give the crude product, which is recrystallized from water.
How is lidocaine synthesized?
Lidocaine, 2-(diethylamino)-N-(2,6-dimethylphenyl)acetamide (2.2. 2), is synthesized from 2,6-dimethylaniline upon reaction with chloroacetic acid chloride, which gives α-chloro-2,6-dimethylacetanilide (2.1. 1), and its subsequent reaction with diethylamine [11].
How do triptans cause vasoconstriction?
In conclusion, triptans induce vasoconstriction in arteries and veins from the thoracic wall, most likely by activation of 5-HT1B receptors.
How does ibuprofen inhibit prostaglandin synthesis?
Nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used for their anti-inflammatory, analgesic, and antipyretic effects. NSAIDs generally work by blocking the production of prostaglandins (PGs) through the inhibition of two cyclooxygenase enzymes.
What is the purpose of phenacetin?
Phenacetin was the first NSAID and fever reducer to go on the market. It acts as an analgesic at the spinal cord as well as a negative inotrope at the heart. It can be used to treat subacute rheumatoid arthritis, intercostal neuralgia, and ataxias. Metabolised in the body to paracetamol.
What three roles does diethyl amine serve in the synthesis of lidocaine?
Diethyl amine serves three roles in this reaction: (a) as a nucleophile to displace chloride anion from –CH2Cl in the α-chloro-2, 6-dimethylacetanilide by an SN2 type reaction; (b) as a base to absorb the HCl that is formed in the nucleophilic substitution reaction leading to Lidocaine; and (c) as a solvent for the …
Do triptans dilate or constrict blood vessels?
Triptans constrict extracerebral, but no intracerebral arteries, in healthy volunteers and migraine patients. The vasoconstrictor action of sumatriptan on extracerebral arteries could be relevant to relief migraine pain.
Do triptans constrict all blood vessels?
5-HT2A, 5-HT1B, and 5-HT1D receptor mRNA levels were detected by real-time PCR in all blood vessels studied. In conclusion, triptans induce vasoconstriction in arteries and veins from the thoracic wall, most likely by activation of 5-HT1B receptors.
How do NSAIDs work on prostaglandins?
NSAIDs block a specific enzyme called cyclooxygenase (or COX) used by the body to make prostaglandins. By reducing production of prostaglandins, NSAIDs help relieve the discomfort of fever and reduce inflammation and the associated pain.
How do prostaglandin inhibitors work?
The prostaglandin synthase inhibitors such as indomethacin, aspirin, naproxen, and fenoprofen decrease uterine contractions by inhibiting activity of the cyclo-oxygenase enzyme that converts arachidonic acid to the various prostaglandins.
What is synthesis of amides?
Synthesis of amides. Amines are efficiently acylated by both cyclic and acyclic anhydrides in aqueous medium with sodium dodecyl sulfate (SDS) – without use of acidic or basic reagents. Various amines and anhydrides were reacted with equal ease. Chemoselective acylation in the presence of phenols and thiols has been achieved.
How to synthesize N-(hetero) arylamide using amine activation?
A method for N – (hetero)arylamide synthesis based on rarely explored amine activation, rather than classical acid activation, shows a broad scope including challenging amides. The activated amines are easily prepared using a three-component reaction with commercial reagents.
How do you make N-acyl amidines from nitroalkene derivatives?
A mild, metal-free, multicomponent reaction provides N -acyl amidines from nitroalkene derivatives, dibromo amides, and amines via formation of an initial α,α-dibromonitroalkane intermediate that can undergo C-C bond cleavage.
How do you make amidine from terminal alkynes?
A silver-catalyzed, one-pot, four-component reaction of terminal alkynes, TMSN 3, sodium sulfinate, and sulfonyl azide provides amidines. A possible cascade reaction mechanism consists of alkyne hydroazidation, sulfonyl radical addition, 1,3-dipolar cycloaddition of TMSN 3, and retro-1,3-dipolar cycloaddition.