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001-es BibID:	BIBFORM048543
035-os BibID:	PMID:8886410 WOS:A1996VG29800017
Első szerző:	Szállási Árpád (pathológus)
Cím:	The stimulation of capsaicin-sensitive neurones in a vanilloid receptor-mediated fashion by pungent terpenoids possessing an unsaturated 1,4-dialdehyde moiety / A. Szallasi, M. Jonassohn, G. Ács, T. Bíró, P. Ács, P. M. Blumberg, O. Sterner
Dátum:	1996
ISSN:	0007-1188
Megjegyzések:	1. The irritant fungal terpenoid isovelleral caused protective eye-wiping movements in the rat upon intraocular instillation and showed cross-tachyphylaxis with capsaicin, the pungent principle in hot pepper. 2. Isovelleral induced a dose-dependent calcium uptake by rat dorsal root ganglion neurones cultured in vitro with an EC 50 of 95 nM, which was fully inhibited by the competitive vanilloid receptor antagonist capsazepine. 3. Isovelleral inhibited specific binding of [ 3H]-resiniferatoxin (RTX), an ultrapotent capsaicin analogue, to rat trigeminal ganglion or spinal cord preparations with an IC 50 of 5.2 ?M; in experiments in which the concentration of [ 3H]-RTX was varied, isovelleral changed both the apparent affinity (from 16 pM to 37 pM) and the co-operativity index (from 2.1 to 1.5), but not the B(max). 4. The affinity of isovelleral for inducing calcium uptake or inhibiting RTX binding was in very good agreement with the threshold dose (2.2, nmol) at which it provoked pungency on the human tongue. 5. For a series of 14 terpenoids with an unsaturated 1,4-dialdehyde, a good correlation was found between pungency on the human tongue and affinity for vanilloid receptors on the rat spinal cord. 6. The results suggest that isovelleral-like compounds produce their irritant effect by interacting with vanilloid receptors on capsaicin-sensitive sensory neurones. Since these pungent diterpenes are structurally distinct from the known classes of vanilloids, these data provide new insights into structure-activity relations and may afford new opportunities for the development of drugs targeting capsaicin-sensitive pathways.
Tárgyszavak:	Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:	British Journal of Pharmacology. - 119 : 2 (1996), p. 283-290. -
További szerzők:	Jonassohn, Mikael Ács Gábor Bíró Tamás (1968-) (élettanász) Ács P. Blumberg, Peter M. Sterner, Olov
Internet cím:	Szerző által megadott URL Intézményi repozitóriumban (DEA) tárolt változat
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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.
Internet cím:	Szerző által megadott URL DOI Intézményi repozitóriumban (DEA) tárolt változat
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