A novel 3-(4,5-diphenyl-1,3-oxazol-2-yl)propanal oxime compound is a potent Transient Receptor Potential Ankyrin 1 and Vanilloid 1 (TRPA1 and V1) receptor antagonist
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- 作者：M. Payritsa ; b ; &dagger ; ; payrits.maja@gmail.com" class="auth_mail" title="E-mail the corresponding author ; É ; . Sá ; ghya ; b ; &dagger ; ; saghyeva@gmail.com" class="auth_mail" title="E-mail the corresponding author ; P. Má ; tyusd ; matyus.peter@pharma.semmelweis-univ.hu" class="auth_mail" title="E-mail the corresponding author ; A. Czompad ; czompa.andrea@pharma.semmelweis-univ.hu" class="auth_mail" title="E-mail the corresponding author ; R. Ludmerczkid ; ludmerczki.robert@pharma.semmelweis-univ.hu" class="auth_mail" title="E-mail the corresponding author ; R. Demed ; deme.ruth@pharma.semmelweis-univ.hu" class="auth_mail" title="E-mail the corresponding author ; Z. Sá ; ndora ; zoltan.sandor@aok.pte.hu" class="auth_mail" title="E-mail the corresponding author ; Zs. Helyesa ; b ; c ; &Dagger ; ; zsuzsanna.helyes@aok.pte.hu" class="auth_mail" title="E-mail the corresponding author ; É ; . Szőkea ; b ; c ; &Dagger ; ; eva.szoke@aok.pte.hu" class="auth_mail" title="E-mail the corresponding author
- 关键词：AITC ; allyl-isothiocyanate ; CGRP ; calcitonin gene-related peptide ; CHO ; Chinese hamster ovary cell line ; COX ; cyclooxygenase ; CZP ; capsazepine ; D-MEM ; Dulbecco&rsquo ; s-Modified Eagle Medium ; DMSO ; dimethyl sulfoxide ; ECS ; extracellular solution ; LJP 1207 ; N&prime ; -(2-Phenylallyl)hydrazine hydrochloride ; NGF ; nerve growth factor ; PBS ; phosphate-buffered solution ; SSAO ; semicarbazide-sensitive amine-oxidase ; SZV-1287 ; 3-(4 ; 5-diphenyl-1 ; 3-oxazol-2-yl)propanal oxim ; TG ; trigeminal ganglion ; TRPV1 ; T
- 刊名：Neuroscience
- 出版年：2016
- 出版时间：2 June 2016
- 年：2016
- 卷：324
- 期：Complete
- 页码：151-162
- 全文大小：861 K
文摘
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SZV-1287 is a new 3-(4,5-diphenyl-1,3-oxazol-2-yl)propanal oxime SSAO inhibitor.
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Structure of oxime derivatives described as TRPA1 antagonists is similar to SZV1287.
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SZV-1287 exerts inhibition on both TRPA1 and TRPV1 activation in TRG neurons.
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SZV-1287 inhibits the TRPA1, but not the TRPV1 activation on sensory nerve endings.
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SZV-1287 inhibits the TRPA1 and TRPV1 activation in receptor-expressing cell lines.