Results 61 to 70 of about 161 (74)

Varespladib (LY315920) neutralises phospholipase A2 mediated prothrombinase-inhibition induced by Bitis snake venoms

Comparative Biochemistry and Physiology Part C: Toxicology & Pharmacology, 2020
Anticoagulant toxicity is a common function of venoms produced by species within the Bitis genus. Potent inhibition of the prothrombinase complex is an identified mechanism of action for the dwarf species B. cornuta and B. xeropaga, along with some localities of B. atropos and B. caudalis.
Nicholas J. Youngman, Andrew A. Walker, Arno Naude, Kristian Coster, Eric Sundman, Bryan G. Fry   +5 more
semanticscholar   +5 more sources

Varespladib (LY315920) prevents neuromuscular blockage and myotoxicity induced by crotoxin on mouse neuromuscular preparations

Toxicon, 2021
Varespladib (LY315920) is a synthetic phospholipase A2 (PLA2) inhibitor that has been demonstrating antiophidic potential against snake venoms that present PLA2 neurotoxins. In this study, we evaluate the capacity of Varespladib to inhibit the neuromuscular effects of crotoxin (CTX), the main toxic component of Crotalus durissus terrificus snake venom,
Fernanda Valadares Maciel, Êmylle Karoline Ramos Pinto, Natália Muradas Valério Souza, Thales Augusto Gonçalves de Abreu, Paula Ladeira Ortolani, Consuelo Latorre Fortes-Dias, Walter Luís Garrido Cavalcante   +6 more
semanticscholar   +4 more sources

Varespladib (LY315920) inhibits neuromuscular blockade induced by Oxyuranus scutellatus venom in a nerve-muscle preparation

Toxicon, 2020
The phospholipase A2 (PLA2) inhibitors varespladib (LY315920) and its orally available derivative methyl-varespladib (LY333013) have been proposed as potential therapies for the treatment of snakebite envenomings in which toxicity depends on the action of PLA2s.
Isadora Caruso Fontana Oliveira, José Marı́a Gutiérrez, Matthew R. Lewin, Yoko Oshima‐Franco   +3 more
semanticscholar   +4 more sources

Varespladib (LY315920) rescues mice from rapidly lethal doses of venoms from five vipers, suggesting direct and indirect mechanisms for its therapeutic effect in a mouse model of snakebite envenomation

Toxicon, 2019
Matthew R. Lewin, Tommaso C. Bulfone
semanticscholar   +3 more sources

Varespladib (LY315920) effectively reverses experimental neuro-myotoxic effects in a pig model of lethal envenoming by Taipan (O. scutellatus) and Mojave rattlesnake (C. scutulatus)

Toxicon, 2020
Lyndi L. Gilliam, J.N. Gilliam, R.W. Carter, Stephen P. Samuel, José Marı́a Gutiérrez, David Williams, Y.V. Surovsteva, Tommaso C. Bulfone, Matthew R. Lewin   +8 more
semanticscholar   +3 more sources

Varespladib (LY315920) appears to be a very potent, broad-spectrum, inhibitor of snake venom PLA2s from six continents

Toxicon, 2016
Matthew R. Lewin, Stephen P. Samue, Janie Merkel, Philip E. Bickler   +3 more
semanticscholar   +3 more sources

Pharmacology of LY315920/S-5920, [[3-(Aminooxoacetyl)-2-ethyl-1-(phenylmethyl)-1 H-indol-4-yl]oxy]acetate, a Potent and Selective Secretory Phospholipase A2Inhibitor: A New Class of Anti-Inflammatory Drugs, SPI

The Journal of Pharmacology and Experimental Therapeutics, 1999
LY315920 is a potent, selective inhibitor of recombinant human, group IIA, nonpancreatic secretory PLA2 (sPLA2). In a chromogenic isolated enzyme assay, LY315920 inhibited sPLA2 activity with an IC50 of 9 +/- 1 nM or 7.3 x 10(-6) mole fraction, which approached the stiochiometric limit of this assay.
David W. Snyder, Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim, Donald G. Carlson, Niles Fox, Neal W. Roehm, Christopher T. Armstrong, C. Chang, Lawrence W. Hartley, Lea M. Johnson, Carlos Romero, Amy C. Smith, Min Song, Jerome H. Fleisch   +14 more
semanticscholar   +4 more sources

Myotoxin I from Bothrops moojeni co-crystallized with synthetic inhibitor Varespladib (LY315920)

, 2021
G.H.M. Salvador, Rafael J. Borges, Marcos R.M. Fontes   +2 more
openalex   +2 more sources

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The synthetic Varespladib molecule is a multi-functional inhibitor for PLA2 and PLA2-like ophidic toxins.

Biochimica et Biophysica Acta - General Subjects, 2021
BACKGROUND The treatment for snakebites is early administration of antivenom, which can be highly effective in inhibiting the systemic effects of snake venoms, but is less effective in the treatment of extra-circulatory and local effects.
Guilherme H. M. Salvador, R. Borges, B. Lomonte, M. Lewin, M. Fontes   +4 more
semanticscholar   +1 more source

Anticoagulant toxicity of black snake (Elapidae: Pseudechis) venoms: Potency, mechanisms, and antivenom efficacy.

Toxicology Letters, 2020
Pseudechis species (Australian black snakes) within the Elapidae family are rich in anticoagulant PLA2 toxins, with the exception of one species (P. porphyriacus) that possesses procoagulant mutated forms of the clotting enzyme Factor Xa.
C. Zdenek, Nicholas J. Youngman, Christoper Hay, James S. Dobson, N. Dunstan, L. Allen, Leontina Milanovic, B. Fry   +7 more
semanticscholar   +1 more source