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001-es BibID:	BIBFORM004104
Első szerző:	Marincsák Rita (fogszakorvos)
Cím:	The analgesic drug, tramadol, acts as an agonist of the transient receptor potential vanilloid-1 / Marincsák R., Tóth B.I., Czifra G., Szabó T., Kovács L., Bíró T.
Dátum:	2008
Megjegyzések:	Tramadol is an effective analgesic substance widely used in medical practice. Its therapeutic action have been mainly attributed to the activation of mu-opioid receptors as well as to the inhibition of neurotransmitter reuptake mechanisms and various voltage- and ligand-gated ion channels of the nociceptive system. As transient receptor potential vanilloid-1 (TRPV1, "the capsaicin receptor") has been shown to function as a central integrator molecule of pain sensation, our aim in the current study was to define the involvement of TRPV1 in the complex mechanism of action of tramadol. METHODS: To achieve these goals, we used single-cell Ca-imaging as well as fluorescent image plate reader assays on Chinese hamster ovary (CHO) cells heterologously over-expressing TRPV1. RESULTS: We found that (1) tramadol, similar to the well-known TRPV1 agonist, capsaicin, significantly increased [Ca(2+)](i) of TRPV1-CHO cells in a concentration-dependent fashion; (2) its effect was reversibly prevented by the TRPV1 antagonist capsazepine; (3) repeated application of tramadol resulted in marked tachyphylaxis; and (4) tramadol did not modify [Ca(2+)](i) in control (empty vector expressing) CHO cells. CONCLUSIONS: Collectively, these findings strongly support the intriguing and novel concept that tramadol acts as an agonist of TRPV1. Considering that activation of TRPV1 on sensory neurons is followed by a local release of vasoactive neuropeptides and a marked desensitization of the afferent fibers (hence termination of pain sensation), our findings may equally explain both the desired analgesic as well as the often-seen, yet "unexpected," local side effects (e.g., initiation of burning pain and erythema) of tramadol.
Tárgyszavak:	Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:	Anesthesia and Analgesia. - 106 : 6 (2008), p. 1890-1896. -
További szerzők:	Tóth István Balázs (1978-) (élettanász) Czifra Gabriella (1975-) (élettanász) Szabó Tamás (1968-) (gyermekgyógyász) Kovács László (1939-) (élettanász) Bíró Tamás (1968-) (élettanász)
Internet cím:	elektronikus változat elektronikus változat DOI
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