Differential anti-inflammatory and analgesic effects by enantiomers of zaltoprofen in rodents

In the present study, we investigated the effect of zaltoprofen enantiomers on inflammation and pain and compared their effect with racemic zaltoprofen. S(+)-zaltoprofen potently inhibited the inflammatory response in carrageenan-induced paw edema model, whereas R(−)-zaltoprofen did not. Moreover, t...

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Veröffentlicht in:International immunopharmacology 2013-08, Vol.16 (4), p.457-460
Hauptverfasser: Cho, Ig Jun, Lee, Chang Woo, Lee, Myeong Youl, Kang, Moo Rim, Yun, Jieun, Oh, Soo Jin, Han, Sang-Bae, Lee, Kiho, Park, Song-Kyu, Kim, Hwan Mook, Jung, Sang-Hun, Kang, Jong Soon
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container_end_page 460
container_issue 4
container_start_page 457
container_title International immunopharmacology
container_volume 16
creator Cho, Ig Jun
Lee, Chang Woo
Lee, Myeong Youl
Kang, Moo Rim
Yun, Jieun
Oh, Soo Jin
Han, Sang-Bae
Lee, Kiho
Park, Song-Kyu
Kim, Hwan Mook
Jung, Sang-Hun
Kang, Jong Soon
description In the present study, we investigated the effect of zaltoprofen enantiomers on inflammation and pain and compared their effect with racemic zaltoprofen. S(+)-zaltoprofen potently inhibited the inflammatory response in carrageenan-induced paw edema model, whereas R(−)-zaltoprofen did not. Moreover, the anti-inflammatory effect of S(+)-zaltoprofen was stronger than that of racemic zaltoprofen, suggesting that S(+)-zaltoprofen is an active component of racemic zaltoprofen in terms of anti-inflammatory activity. In contrast, the results of acetic acid-induced writhing model demonstrated that no significant analgesic effect was observed by racemic zaltoprofen and zaltoprofen enantiomers at doses used in carrageenan-induced paw edema model. However, racemic zaltoprofen and zaltoprofen enantiomers all exerted an analgesic effect at higher doses, which is inconsistent with the result of carrageenan-induced paw edema model. Gastric ulcers induced by racemic zaltoprofen and zaltoprofen enantiomers were minimal. Taken together, these results suggest that S(+)-zaltoprofen is a potent and active anti-inflammatory component of racemic zaltoprofen, but both S(+)-zaltoprofen and R(−)-zaltoprofen might seem to contribute to the analgesic effect of racemic zaltoprofen. •S(+)-zaltoprofen is an active anti-inflammatory component of racemic zaltoprofen.•Both enantiomers of zaltoprofen contribute to the analgesic effect of racemate.•The effects of S(+)-zaltoprofen is more potent than the racemic zaltoprofen.•S(+)-zaltoprofen exerts minimal gastric damage.
doi_str_mv 10.1016/j.intimp.2013.05.008
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S(+)-zaltoprofen potently inhibited the inflammatory response in carrageenan-induced paw edema model, whereas R(−)-zaltoprofen did not. Moreover, the anti-inflammatory effect of S(+)-zaltoprofen was stronger than that of racemic zaltoprofen, suggesting that S(+)-zaltoprofen is an active component of racemic zaltoprofen in terms of anti-inflammatory activity. In contrast, the results of acetic acid-induced writhing model demonstrated that no significant analgesic effect was observed by racemic zaltoprofen and zaltoprofen enantiomers at doses used in carrageenan-induced paw edema model. However, racemic zaltoprofen and zaltoprofen enantiomers all exerted an analgesic effect at higher doses, which is inconsistent with the result of carrageenan-induced paw edema model. Gastric ulcers induced by racemic zaltoprofen and zaltoprofen enantiomers were minimal. Taken together, these results suggest that S(+)-zaltoprofen is a potent and active anti-inflammatory component of racemic zaltoprofen, but both S(+)-zaltoprofen and R(−)-zaltoprofen might seem to contribute to the analgesic effect of racemic zaltoprofen. •S(+)-zaltoprofen is an active anti-inflammatory component of racemic zaltoprofen.•Both enantiomers of zaltoprofen contribute to the analgesic effect of racemate.•The effects of S(+)-zaltoprofen is more potent than the racemic zaltoprofen.•S(+)-zaltoprofen exerts minimal gastric damage.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>23721690</pmid><doi>10.1016/j.intimp.2013.05.008</doi><tpages>4</tpages></addata></record>
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subjects Analgesic
Analgesics, Non-Narcotic - administration & dosage
Analgesics, Non-Narcotic - adverse effects
Analgesics, Non-Narcotic - chemistry
Analgesics, Non-Narcotic - therapeutic use
Animals
Anti-inflammatory
Anti-Inflammatory Agents, Non-Steroidal - administration & dosage
Anti-Inflammatory Agents, Non-Steroidal - adverse effects
Anti-Inflammatory Agents, Non-Steroidal - chemistry
Anti-Inflammatory Agents, Non-Steroidal - therapeutic use
Benzopyrans - administration & dosage
Benzopyrans - adverse effects
Benzopyrans - chemistry
Benzopyrans - therapeutic use
Disease Models, Animal
Dose-Response Relationship, Drug
Edema - drug therapy
Enantiomer
Male
Mice
Mice, Inbred ICR
Pain - drug therapy
Propionates - administration & dosage
Propionates - adverse effects
Propionates - chemistry
Propionates - therapeutic use
Rats
Rats, Sprague-Dawley
Stereoisomerism
Stomach Ulcer - chemically induced
Structure-Activity Relationship
Zaltoprofen
title Differential anti-inflammatory and analgesic effects by enantiomers of zaltoprofen in rodents
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