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118) In the present study, we modified carboxylic acid group of ibuprofen, one of non-steroidal anti-inflammatory drugs, based on the common structure of transient receptor potential vanilloid type 1 antagonists which are considered as new candidates for analgesic drugs, and synthesized several derivatives of ibuprofen.
* Evaluation of anti-inflammatory and analgesic effects of synthesized derivatives of ibuprofen.
- Inflammatory and pain are major areas for drug discovery. Current analgesic drugs often cause a number of side-effects. In the present study, we modified carboxylic acid group of ibuprofen, one of non-steroidal anti-inflammatory drugs, based on the common structure of transient receptor potential vanilloid type 1 antagonists which are considered as new candidates for analgesic drugs, and synthesized several derivatives of ibuprofen. Comprehensive evaluations of the pharmacological properties of these compounds were investigated. Compound 17 showed weak cyclooxygenase inhibition and exhibited strong transient receptor potential vanilloid type 1 antagonistic activity. It was found to be capable of blocking noxious thermal nociception and capsaicin-induced nociception in mice. Besides, 17 showed less ulcerogenic action than ibuprofen did and had no hyperthermia side-effect compared with common transient receptor potential vanilloid type 1 antagonists. Therefore, it suggested that 17 could be used as a safe alternative analgesic candidate for pain treatment.
=>1.酸っぱい, 2.辛辣な, 3.酸, 4.《俗語》麻薬, LSD
Overview of noun acid
The noun acid has 2 senses (first 1 from tagged texts)
1. (4) acid -- (any of various water-soluble compounds having a sour taste and capable of turning
litmus red and reacting with a base to form a salt)
2. acid, back breaker, battery-acid, dose, dot, Elvis, loony toons, Lucy in the sky with diamonds,
pane, superman, window pane, Zen -- (street name for lysergic acid diethylamide)
Overview of adj acid
The adj acid has 3 senses (first 1 from tagged texts)
1. (1) acerb, acerbic, acid, acrid, bitter, blistering, caustic, sulfurous, sulphurous, virulent,
vitriolic -- (harsh or corrosive in tone; "an acerbic tone piercing otherwise flowery prose"; "a
barrage of acid comments"; "her acrid remarks make her many enemies"; "bitter words"; "blistering
criticism"; "caustic jokes about political assassination, talk-show hosts and medical ethics"; "a
sulfurous denunciation"; "a vitriolic critique")
2. acidic, acid, acidulent, acidulous -- (being sour to the taste)
3. acid -- (having the characteristics of an acid; "an acid reaction")
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