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001-es BibID:BIBFORM048549
035-os BibID:PMID:9761427
Első szerző:Szállási Árpád (pathológus)
Cím:Dialdehyde sesquiterpenes and other terpenoids as vanilloids / Arpad Szallasi, Tamas Bíró, Shayan Modarres, Luigi Garlaschelli, Marlen Petersen, Andreas Klusch, Giovanni Vidari, Mikael Jonassohn, Salvatore De Rosa, Olov Sterner, Peter M. Blumberg, James E. Krause
Dátum:1998
ISSN:0014-2999
Megjegyzések:Selected naturally occurring unsaturated dialdehyde sesquiterpenes and related bioactive terpenoids were assayed for vanilloid-like activity. Out of the 25 compounds tested, eight inhibited completely the specific binding of [3H]resiniferatoxin by rat spinal cord membranes: binding affinities ranged from 0.6 ?M for cinnamodial to 19.0 ?M for hebelomic acid F. These values were comparable to the binding affinity of capsaicin (2.7 ?M). With the exception of four ligands, compounds that inhibited resiniferatoxin binding to rat spinal cord membranes were also pungent on the human tongue where they showed cross-tachyphylaxis with capsaicin. As expected from their reactive nature, these compounds possess additional sites of action, as reflected in the complex behavior of the stimulation of calcium influx by cinnamodial and cinnamosmolide at high concentrations. This observation might explain the unexpectedly weak membrane depolarization by cinnamodial compared to capsaicin. We conclude that a range of sesquiterpene dialdehydes and related terpenoids, both pungent and non-pungent, may function as vanilloids. These compounds may represent a new chemical lead for the development of vanilloid drugs, structurally unrelated to either capsaicin or resiniferatoxin.
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:European Journal Of Pharmacology. - 356 : 1 (1998), p. 81-89. -
További szerzők:Bíró Tamás (1968-) (élettanász) Modarres, Shayan Garlaschelli, Luigi Petersen, Marlen Klusch, Andreas Vidari, Giovanni Jonassohn, Mikael De Rosa, Salvatore Sterner, Olov Blumberg, Peter M. Krause, James E.
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