RHC 3024: Antiallergic Activity in vitro and Comparison with Disodium Cromoglycate and Other Antiallergic Agents

Khandwala, Atul; Coutts, Stephen M.; Dally-Meade, Vernetta; Jariwala, N.; Huang, Fu‐Chih

doi:10.1159/000233342

Cited by 9 publications

(14 citation statements)

References 14 publications

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“…In contrast, all the drugs displayed little or no inhibition of A23187-induced histamine release. Our results are in agree ment with those reported by many investiga tors (31)(32)(33)(34)(35). However, there are a few papers demonstrating that DSCG inhibits A23187 induced histamine release from rat mast cells (36,37).…”

Section: Discussionsupporting

confidence: 92%

Immunopharmacological Studies on TBX, a New Antiallergic Drug (2) Inhibitory Effects on Histamine Release from Peritoneal Mast Cells and Lung Fragments of Rats

Yanagihara

Kasai²,

Shida

1988

Japanese Journal of Pharmacology

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Section: Discussionsupporting

confidence: 92%

Immunopharmacological Studies on TBX, a New Antiallergic Drug (2) Inhibitory Effects on Histamine Release from Peritoneal Mast Cells and Lung Fragments of Rats

Yanagihara

Kasai²,

Shida

1988

Japanese Journal of Pharmacology

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“…A num ber of new orally effective 'DSCG-like' agents have been discovered and are in various stages of develop ment [5][6][7][8][9][10][11][12].…”

Section: Introductionmentioning

confidence: 99%

Antiallergic Activity Profiles in vitro of RHC 3164 and Related Compounds

Khandwala¹,

Dally-Meade²,

Jariwala³

et al. 1984

Int Arch Allergy Immunol

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RHC 3164 has been investigated for its antiallergic activities in 3 in vitro models of anaphylaxis. RHC 3164 was 6 times more potent than DSCG as an inhibitor of antigen-induced release of histamine (AIR) from rat mast cells (RMC) and had an activity profile identical to that of DSCG in the following respects: loss of inhibitory activity with increasing preincubation time, tachyphylactic properties, cross-tachyphylaxis to DSCG, and inability to inhibit nonimmunologic release of histamine. Neither RHC 3164 nor DSCG had any effect on immunologic release of histamine from human basophils or guinea pig lung slices. We conclude that RHC 3164 is a potent inhibitor of immunologic release of histamine from RMC with a mechanism of action similar to that of DSCG.

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“…We have previously reported (14,15] that DSCG (3 uM) routinely used as a positive control inhibited AIR by 45.2 ±5.2% (average ±SE, n = 304) and has an I50 value of 4.5 ±0.5 ¡.iM(average ± SE, n = 96). …”

Section: Inhibition O F Air From Rat Mast Cellsmentioning

confidence: 93%

“…The effects of test compounds on spontaneous (SR) and antigen-induced release of histamine (AIR) from passively sensitized rat mast cells were determined according to the procedure of Khandwala et al [14]. Washed peritoneal cells were passively sensi tized in vitro with rat anti-ovalbumin serum.…”

Section: Antigen-induced Release O F Histamine From Rat Mast Cells (Rmc)mentioning

confidence: 99%

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Antiallergic Activity Profiles in vitro of RHC 3164 and Related Compounds

Khandwala¹,

Inwegen²,

Coutts³

et al. 1984

Int Arch Allergy Immunol

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A series of 26 compounds belonging to the chemical class of (1,2,4)triazolo(4,3-a)-quinoxaline-1,4-diones have been investigated for their antiallergic activities in 3 in vitro models of anaphylaxis. Effects of these and other known antiallergic agents on cyclic nucleotide phosphodiesterases (cNUC-PDE) from purified rat mast cells have also been investigated. 18 compounds were potent (I₅₀ ≤ 45 μM) inhibitors of antigen-induced release of histamine (AIR) from rat mast cells (RMC), 3 compounds inhibited anti-IgE-induced release of histamine from human basophils (I₅₀ ≤ 25 μM) and none of the compounds significantly affected AIR from guinea pig lung slices. 13 of the compounds were more potent than theophylline as inhibitors of cyclic AMP-PDE and/or cyclic GMP-PDE from RMC. Parallel concentration-response curves for the inhibition of cyclic AMP-PDE and cyclic GMP-PDE indicated that these compounds probably interact with enzyme in the same manner. Paired regression analysis of the I₅₀ values for inhibition of AIR and cNUC-PDE from RMC by these compounds revealed no statistically significant correlation between the inhibition of AIR and inhibition of cyclic AMP-PDE or cyclic GMP-PDE. We conclude: (1) some of these compounds are potent inhibitors of immunologic release of histamine from RMC with an in vitro activity profile similar to that of DSCG, and (2) inhibition of cyclic AMP or cyclic GMP hydrolysis by cNUD-PDE by these compounds, DSCG, and 6 known antiallergic agents is not the biochemical mechanism by which they inhibit AIR from RMC.

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RHC 3024: Antiallergic Activity in vitro and Comparison with Disodium Cromoglycate and Other Antiallergic Agents

Cited by 9 publications

References 14 publications

Immunopharmacological Studies on TBX, a New Antiallergic Drug (2) Inhibitory Effects on Histamine Release from Peritoneal Mast Cells and Lung Fragments of Rats

Immunopharmacological Studies on TBX, a New Antiallergic Drug (2) Inhibitory Effects on Histamine Release from Peritoneal Mast Cells and Lung Fragments of Rats

Antiallergic Activity Profiles in vitro of RHC 3164 and Related Compounds

Antiallergic Activity Profiles in vitro of RHC 3164 and Related Compounds

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