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1.

001-es BibID:BIBFORM039245
Első szerző:Ács Géza (traumatológus)
Cím:Differential activation and desensitization of sensory neurons by resiniferatoxin / Acs, G., Biro, T., Acs, P., Modarres, S., Blumberg, P. M.
Dátum:1997
ISSN:0270-6474
Megjegyzések:Recently, with use of rat dorsal root ganglion (DRG) neurons we have been able to dissociate the binding affinities of vanilloids from their potencies to induce Ca-45 uptake, which suggests the existence of distinct classes of the vanilloid receptor (Acs et al., 1996). In the present study, we have demonstrated that the ultrapotent capsaicin analog resiniferatoxin (RTX) desensitized rat DRG neurons to the subsequent induction of Ca-45 uptake by capsaicin and RTX with affinity and cooperativity similar to that found for [H-3]RTX binding, contrasting with a similar to 10-fold weaker potency and lack of cooperativity to induce Ca-45 uptake. Likewise, the competitive antagonist capsazepine inhibited RTX-induced desensitization with potency similar to that for inhibition of specific [H-3]RTX binding, whereas the potency of capsazepine was similar to 10-fold higher for inhibiting RTX-induced Ca-45 uptake. Finally, the noncompetitive antagonist ruthenium red inhibited both the RTX-induced desensitization and Ca-45 uptake but showed similar to 60-fold selectivity for inhibiting RTX-induced desensitization. The RTX-induced desensitization was not associated with loss of specific [H-3]RTX binding, suggesting lack of gross cell toxicity. In contrast to RTX, capsaicin caused desensitization with a potency corresponding to that for Ca-45 uptake and did so in a noncooperative manner. Unlike the RTX-induced desensitization, the desensitization by capsaicin was blocked by ruthenium red only at doses that blocked Ca-45 uptake and depended on external calcium, Our findings provide further support for the existence of vanilloid receptor subtypes on DRG neurons with distinct pharmacology and distinct patterns of desensitization.
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:Journal of Neuroscience. - 17 : 14 (1997), p. 5622-5628. -
További szerzők:Bíró Tamás (1968-) (élettanász) Ács Péter Modarres, Shayan Blumberg, Peter M.
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2.

001-es BibID:BIBFORM039246
Első szerző:Bíró Tamás (élettanász)
Cím:Recent advances in understanding of vanilloid receptors : a therapeutic target for treatment of pain and inflammation in skin / Biro, T., Acs, G., Acs, P., Modarres, S., Blumberg, P. M.
Dátum:1997
Megjegyzések:C-fiber sensory afferent neurons, which contain neuropeptides such as calcitonin-gene related peptide and substance P, mediate a wide variety of physiologic responses, including chemogenic pain, thermoregulation, and neurogenic inflammation. Capsaicin, the pungent constituent in red pepper, functions to activate and then, at higher doses and longer times, desensitize this class of neurons, This latter response provides the basis for the therapeutic application of capsaicin, A major advance in the field has been the identification of resiniferatoxin, a phorbol-related diterpene, as an analog of capsaicin that is ultrapotent but with differential selectivity, In particular, resiniferatoxin is only similar in potency for induction of pain but is much more effective for desensitization, Structure-activity analysis in whole animal experiments provides further evidence for dissociation of biologic endpoints, strongly arguing for the existence of vanilloid receptor subclasses, Using resiniferatoxin, we have been able to define specific, high-affinity receptors for capsaicin both in animal models such as rats and in man, Of great importance, the pharmacologic characterization in cultured dorsal root ganglion cells of the high-affinity resiniferatoxin-binding site and of tile physiologic response believed to be directly coupled to the receptor, viz, calcium uptake, differed in structure-activity and in cooperativity. We conclude that multiple high-affinity vanilloid receptor subclasses mediate vanilloid response; moreover, the resiniferatoxin-selective subclass of vanilloid receptors is not the voltage-independent, cation-nonselective ion channel as previously believed, Optimization of ligands for the individual vanilloid receptor subclasses should revolutionize this therapeutic area.
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:Journal of Investigative Dermatology Symposium Proceedings. - 2 : 1 (1997), p. 56-60. -
További szerzők:Ács Géza (1939-) (traumatológus) Ács Péter Modarres, Shayan Blumberg, Peter M.
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3.

001-es BibID:BIBFORM039266
Első szerző:Bíró Tamás (élettanász)
Cím:Characterization of functional vanilloid receptors expressed by mast cells / Biro, T., Maurer, M., Modarres, S., Lewin, N. E., Brodie, C., Acs, G., Acs, P., Paus, R., Blumberg, P. M.
Dátum:1998
ISSN:0006-4971
Megjegyzések:Capsaicin and its ultrapotent analog resiniferatoxin (RTX) act through specific vanilloid receptors on sensory neurons. The C-type receptor is coupled to Ca-45 uptake, whereas the R-type is detectable by [H-3]RTX binding. We describe here specific vanilloid responses in murine mast cells (MCs). In the MC lines and in bone marrow-derived mast cells. capsaicin and RTX induced Ca-45 uptake similarly to that observed for cultured rat dorsal root ganglion neurons (DRGs). This response was antagonized by the antagonists capsazepine and ruthenium red. As in DRGs, pretreatment of MCs with capsaicin or RTX induced desensitization to subsequent stimulation of Ca-45 uptake. The potency for desensitization by RTX in the MCs corresponded to that for Ca-45 uptake, whereas in DRGs it occurred at significantly lower concentrations corresponding to that for the high-affinity [H-3]RTX binding site. Consistent with this difference, in MCs we were unable to detect [H-3]RTX binding. Vanilloids were noncytotoxic to the MCs, in contrast to the DRGs. Although vanilloids did not cause degranulation in MCs, in the P815 clone capsaicin evoked selective interleukin-4 release. We conclude that certain MCs possess vanilloid receptors, but only the C-type that functions as a channel. Our finding that MCs can respond directly to capsaicin necessitates a reevaluation of the in vivo pathway of inflammation in response to vanilloids. This is a US government work. There are no restrictions on its use.
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:Blood. - 91 : 4 (1998), p. 1332-1340. -
További szerzők:Maurer, Marcus Modarres, Shayan Lewin, Nancy E. Brodie, Chaya Ács Géza (1939-) (traumatológus) Ács Péter Paus, Ralf Blumberg, Peter M.
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4.

001-es BibID:BIBFORM039235
035-os BibID:PMID:9602075
Első szerző:Bíró Tamás (élettanász)
Cím:Specific vanilloid responses in C6 rat glioma cells / Tamás Bíró, Chaya Brodie, Shayan Modarres, Nancy E. Lewin, Péter Ács, Peter M. Blumberg
Dátum:1998
ISSN:0169-328X
Megjegyzések:Capsaicin and its ultrapotent analog resiniferatoxin (RTX) act through specific vanilloid receptors on sensory neurons. Here, we describe specific vanilloid responses in rat C6 glioma cells. Capsaicin and RTX stimulated 45Ca uptake in a similar fashion to that found for cultured rat dorsal root ganglion neurons (DRGs); this response was antagonized by the antagonists capsazepine and ruthenium red. As in DRGs, pretreatment of C6 cells with capsaicin or RTX produced desensitization to subsequent stimulation of 45Ca uptake. The potency for desensitization by RTX in the C6 cells corresponded to that for 45Ca uptake, whereas in DRGs it occurred at significantly lower concentrations corresponding to that for the high affinity [3H]RTX binding site. Consistent with this difference, in C6 cells we were unable to detect [3H]RTX binding. These characteristics suggest the presence of C-type but not R-type vanilloid receptors on C6 cells. After 2 day treatment, capsaicin but not RTX inhibited the proliferation and altered the differentiation of the cells and produced apoptosis. In the long term experiments, capsazepine, instead of antagonizing the effect of capsaicin, acted as an agonist. Moreover, capsazepine displayed these effects with higher potency than that of capsaicin. The different potencies and structure activity relations suggest a distinct mechanism for these long-term vanilloid effects. Our finding that C6 cells can respond directly to capsaicin necessitates a reevaluation of the in vivo pathway of response to vanilloids, and highlights the importance of the neuron-glial network.
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
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Megjelenés:Molecular Brain Research. - 56 : 1-2 (1998), p. 89-98. -
További szerzők:Brodie, Chaya Modarres, Shayan Lewin, Nancy E. Ács Péter Blumberg, Peter M.
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5.

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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6.

001-es BibID:BIBFORM016044
Első szerző:Szállási Árpád (pathológus)
Cím:Resiniferatoxin-type phorboid vanilloids display capsaicin-like selectivity at native vanilloid receptors on rat DRG neurons and at the cloned vanilloid receptor VR1 / A. Szallasi, T. Szabo, T. Biro, S. Modarres, P. M. Blumberg, E. Krause
Dátum:1999
ISSN:0007-1188
Tárgyszavak:Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
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Megjelenés:British Journal Of Pharmacology. - 128 : 2 (1999), p. 428-434. -
További szerzők:Szabó Tamás (1968-) (gyermekgyógyász) Bíró Tamás (1968-) (élettanász) Modarres, Shayan Blumberg, Peter M. Krause, E.
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7.

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
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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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