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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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001-es BibID:	BIBFORM016046
035-os BibID:	PMID:10217528
Első szerző:	Szállási Árpád (pathológus)
Cím:	A non-pungent triprenyl phenol of fungal origin, scutigeral, stimulates rat dorsal root ganglion neurons via interaction at vanilloid receptors / A. Szallasi, T. Biro, T. Szabo, S. Modarres, M. Petersen, A. Klusch, P. M. Blumberg, E. Krause, O. Sterner
Dátum:	1999
ISSN:	0007-1188
Megjegyzések:	1. A [3H]-resiniferatoxin (RTX) binding assay utilizing rat spinal cord membranes was employed to identify novel vanilloids in a collection of natural products of fungal origin. Of the five active compounds found (scutigeral, acetyl-scutigeral, ovinal, neogrifolin, and methyl-neogrifolin), scutigeral (Ki=19 microM), isolated from the edible mushroom Albatrellus ovinus, was selected for further characterization. 2. Scutigeral induced a dose-dependent 45Ca uptake by rat dorsal root ganglion neurons with an EC50 of 1.6 microM, which was fully inhibited by the competitive vanilloid receptor antagonist capsazepine (IC50=5.2 microM). 3. [3H]-RTX binding isotherms were shifted by scutigeral (10-80 microM) in a competitive manner. The Schild plot of the data had a slope of 0.8 and gave an apparent Kd estimate for scutigeral of 32 microM. 4. Although in the above assays scutigeral mimicked capsaicin, it was not pungent on the human tongue up to a dose of 100 nmol per tongue, nor did it provoke protective wiping movements in the rat (up to 100 microM) upon intraocular instillation. 5. In accord with being non-pungent, scutigeral (5 microM) did not elicit a measurable inward current in isolated rat dorsal root ganglion neurons under voltage-clamp conditions. It did, however, reduce the proportion of neurons (from 61 to 15%) that responded to a subsequent capsaicin (1 microM) challenge. In these neurons, scutigeral both delayed (from 27 to 72 s) and diminished (from 5.0 to 1.9 nA) the maximal current evoked by capsaicin. 6. In conclusion, scutigeral and its congeners form a new chemical class of vanilloids, the triprenyl phenols. Scutigeral promises to be a novel chemical lead for the development of orally active, non-pungent vanilloids.
Tárgyszavak:	Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban külföldön készült közlemény
Megjelenés:	British Journal Of Pharmacology. - 126 : 6 (1999), p. 1351-1358. -
További szerzők:	Bíró Tamás (1968-) (élettanász) Szabó Tamás (1968-) (gyermekgyógyász) Modarres, Shayan Petersen, M. Klusch, Andreas Blumberg, Peter M. Krause, E. Sterner, Olov
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