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FK1706, a novel non-immunosuppressive immunophilin: neurotrophic activity and mechanism of action.
TLDR
Data suggest that FK1706 is a non-immunosuppressive immunophilin ligand with significant neurotrophic effects, putatively mediated via FKBP-52 and the Ras/Raf/MAPK signaling pathway, and therefore that Fk1706 may have therapeutic potential in a variety of neurological disorders. Expand
Neuroprotective Effects of a Novel Poly(ADP-Ribose) Polymerase-1 Inhibitor, 2-{3-[4-(4-Chlorophenyl)-1-piperazinyl] propyl}-4(3H)-quinazolinone (FR255595), in an in Vitro Model of Cell Death and in
TLDR
It is shown that prevention of PARP activation by FR255595 protects against both ROS-induced cells injury in vitro and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced nigrostriatal dopaminergic damage in an in vivo Parkinson's disease (PD) model, suggesting that the drug could be an attractive candidate for several neurodegenerative disorders, including PD. Expand
Resiniferatoxin antagonizes cisplatin-induced emesis in dogs and ferrets.
TLDR
The results suggest that resiniferatoxin-related vanilloids may be useful drugs against both acute and delayed emesis induced by cancer chemotherapy. Expand
Inhibition of arterial thrombosis by a protease-activated receptor 1 antagonist, FR171113, in the guinea pig.
TLDR
Observations indicate that FR171113 has desirable antiplatelet effects both in vitro and in vivo and that its in vivo antithrombotic activity is efficacious without causing a prolongation of bleeding time. Expand
A Novel and Potent Poly(ADP-Ribose) Polymerase-1 Inhibitor, FR247304 (5-Chloro-2-[3-(4-phenyl-3,6-dihydro-1(2H)-pyridinyl)propyl]-4(3H)-quinazolinone), Attenuates Neuronal Damage in in Vitro and in
TLDR
It is shown that prevention of PARP activation by FR247304 treatment protects against both reactive oxygen species-induced PC12 cell injury in vitro and ischemic brain injury in vivo and also suggests that FR 247304 or its derivatives could be attractive therapeutic candidates for stroke and neurodegenerative disease. Expand
Differential effects of FK506 and methotrexate on inflammatory cytokine levels in rat adjuvant-induced arthritis.
TLDR
FK506 is more effective than MTX in reducing elevated levels of inflammatory cytokines TNF-a, IL-1beta, and IL-6 in established stages of AIA, and inhibition of T cell activation results in a rapid reduction ofinflammatory cytokine levels even after the arthritis is established in AIA. Expand
Antiemetic activity of FK1052, a 5-HT3- and 5-HT4-receptor antagonist, in Suncus murinus and ferrets.
TLDR
The present study suggests that FK1052 may be useful against both acute and delayed emesis induced by cancer chemotherapy, and suggests that 5-HT4 receptors are at least partly involved in the mechanism of emesisinduced by copper sulfate. Expand
Inflammatory responses in cuff-induced atherosclerosis in rabbits.
TLDR
It is concluded that leukocytes play a major role in cuff-induced intimal thickening, and that their products cause endothelial denudation and SMC chemotaxis and Involvement of platelet aggregation in atherogenesis is also suggested. Expand
Pharmacological characteristics of a novel nonthiazolidinedione insulin sensitizer, FK614.
TLDR
It is suggested that FK614 improves insulin resistance in such animal models through activation of PPARgamma-mediated transcriptional activity and that it would be a new therapeutic candidate with potential for the treatment of type 2 diabetic patients. Expand
A review of the action of tacrolimus (FK506) on experimental models of rheumatoid arthritis
TLDR
The pharmacological action of tacrolimus suggests that it has potential to specifically suppress the production of pathogenic inflammatory cytokines with a low frequency of infection, improve joint inflammation and bone/cartilage destruction, fully recover loss of functional status, exert rapid relief in arthritic pain, and promote osteogenic and chondrogenic differentiation. Expand
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