Effects of TAK-029, a novel GPIIb/IIIa antagonist, on ...
In guinea pigs, TAK-029 at 30 micrograms/kg (i.v.) inhibited ADP-induced ex vivo platelet aggregation completely and prolonged BT to 4.5 times the control value 5 min after administration, and it prevented thrombotic occlusion in 2 out of 5 animals in a photochemically-induced basilar thrombosis model.
Antithrombotic effect of SM-20302, a nonpeptide GPIIb/IIIa ...
The oral administration of SM-20302 (0.3-10 mg/kg) to guinea pigs completely inhibited the ADP-induced ex vivo platelet aggregation in citrated PRP. In heparinized PRP, SM-20302 (1-10 mg/kg) showed a dose-dependent inhibition of ex vivo platelet aggregation, and it exhibited complete inhibition at a dose of 3 and 10 mg/kg, respectively.
FK419, a novel nonpeptide GPIIb/IIIa antagonist, restores ...
The antithrombotic efficacy of FK419, a novel nonpeptide platelet glycoprotein IIb/IIIa antagonist, was compared with tirofiban in guinea-pigs. FK419 and tirofiban similarly inhibited platelet aggregation in vitro (IC50 values: 0.43+/-0.076 and 0.41+/-0.053 micromol/L) and dispersed aggregated plate …
Inhibitory effect of a novel orally active GP IIb/IIIa ...
Nov 01, 1996· Superiority of platelet integrin GPIIb-IIIa receptor antagonist over aspirin in preventing cyclic flow reductions in the guinea pig middle cerebral artery. Kawano K, Ikeda Y, Kondo K, Umemura K. Eur J Pharmacol, 374(3):377-385, 01 Jun 1999 Cited by: 8 articles | PMID: 10422782
Effects of TAK-029, a novel GPIIb/IIIa antagonist, on ...
The antithrombotic and bleeding time (BT) prolonging effects of TAK-029, a novel GPIIb/IIIa antagonist, were examined in three arterial thrombosis models. In guinea pigs, TAK-029 at 30 micrograms/kg (i.v.) inhibited ADP-induced ex vivo platelet aggregation completely and prolonged BT to 4.5 times th …
Antithrombotic Effect of SM-20302, a Nonpeptide GPIIb/IIIa ...
May 15, 1999· SM-20302 is a synthetic platelet GPIIb/IIIa receptor antagonist that has been shown to inhibit ex vivo platelet aggregation in rhesus monkeys and guinea pigs . The administration of SM-20302 was found to be less hemorrhagic than aspirin and ticlopidine in a mouse model of hydrochloric acid/ethanol-induced gastrointestinal bleeding [11] .
Antithrombotic effects of TAK-029, a novel GPIIb/IIIa ...
The antithrombotic and bleeding time (BT)-prolonging effects of TAK-029, a novel glycoprotein IIb/IIIa antagonist, were characterized and compared with those of conventional antithrombotic agents in guinea pigs. TAK-029 potently inhibited the binding of fibrinogen and von Willebrand factor to purifi …
Optimal Antagonism of GPIIb/IIIa Favors Platelet Adhesion ...
Jan 01, 1996· Guinea pig platelet membrane glycoproteins have been found to exhibit a very close homology to human platelet GPIIb/IIIa and GPIb/IX, 11 12 and their platelet functions resemble those of human platelets in their responsiveness to ADP and the arachidonic acid cascade. 13 In the present study, we evaluated the influence of a growing thrombus on ...
Superiority of platelet integrin GPIIb-IIIa receptor ...
Jun 25, 1999· Superiority of platelet integrin GPIIb-IIIa receptor antagonist over aspirin in preventing cyclic flow reductions in the guinea pig middle cerebral artery. Kawano K(1), Ikeda Y, Kondo K, Umemura K. Author information: (1)Department of Pharmacology, Hamamatsu University School of Medicine, Japan. [email protected]
Disposition and exposure of the fibrinogen receptor ...
Jan 20, 2000· The disposition of XV459, a potent, selective GP IIb/IIIa antagonist, has been examined following intravenous administration of XP280, the benzenesulphonate salt, and 3 H‐SA202, the trifluroacetic acid salt, to male guinea pigs. A liquid chromatography‐mass spectrometry (LC‐MS) method was developed and validated for XV459 quantitation in ...
Optimal antagonism of GPIIb/IIIa favors platelet adhesion ...
To evaluate the involvement of the glycoprotein (GP) IIb/IIIa-dependent process in platelet deposition and thrombus growth on capillaries coated with human type III collagen, the effects of incremental doses of Lamifiban, a potent specific synthetic GPIIb/IIIa antagonist, were studied in ex vivo capillary perfusion chambers using guinea pig blood.
Optimal antagonism of GPIIb/IIIa favors platelet adhesion ...
Jan 01, 1996· To evaluate the involvement of the glycoprotein (GP) IIb/IIIa-dependent process in platelet deposition and thrombus growth on capillaries coated with human type III collagen, the effects of incremental doses of Lamifiban, a potent specific synthetic GPIIb/IIIa antagonist, were studied in ex vivo capillary perfusion chambers using guinea pig blood.
Novel Non-Peptide Fibrinogen Receptor Antagonists. 1 ...
Jan 24, 1998· Compound 9 dose-dependently inhibited ex vivo platelet aggregation in guinea pigs (0.03 and 0.1 mg/kg, iv), and long-lasting inhibition of platelet aggregation was observed upon oral administration of 9 (3 mg/kg) to guinea pigs. On the other hand, the activity of 26 disappeared within 1 h after a dose of 1 mg/kg (iv).
The Effect of a Novel Glycoprotein IIb/IIIa Antagonist, SR ...
Jan 01, 2001· Kawamura M. Imura Y. Moriya N. et al. Antithrombotic effects of TAK-029, a novel GP IIb/IIIa antagonist, in guinea pigs: comparative studies with ticlopidine, clopidogrel. aspirin, prostaglandin E1, and argatroban.
EFFECTS OF TAK-029, A NOVEL GPIIb/IIIa ANTAGONIST, ON ...
May 15, 1997· TAK-029 is a new, non-peptide, orally active GPIIb/IIIa antagonist that blocks the binding of vWf and fibrinogen to human purified GPIIb/IIIa with IC 50 values of 0.33 and 0.67 nM, respectively, and inhibits ADP-induced aggregation of guinea pig, monkey and dog platelet-rich plasma with IC 50 values of 43 nM, 46 nM and 250 nM, respectively .
About Us - Lysogene
About Us - Lysogene. Our mission is to discover and develop innovative therapies to transform the lives of people with rare central nervous system disorders. Lysogene is a biopharmaceutical gene therapy company with lead programs in neurodegenerative lysosomal storage disorders that affect children.
Lysogene and Sarepta Therapeutics Announce Dosing of the ...
Feb 14, 2019· MPS IIIA is caused by mutations in the SGSH gene, which is involved in producing an enzyme necessary for the breakdown and disposal of long chain sugar molecules. LYS-SAF302 is intended to deliver a functional copy of the SGSH gene and allow the brain to secrete the missing enzyme. The goal of the trial is to show improved or stabilized ...
Molecular cloning of the alpha subunit of human and guinea ...
Molecular cloning of the alpha subunit of human and guinea pig leukocyte adhesion glycoprotein Mo1: chromosomal localization and homology to the alpha subunits of integrins. M A Arnaout, E Remold-O'Donnell, M W Pierce, P Harris, and D G Tenen ... and platelet IIb/IIIa receptors. These data suggest that the alpha subunits of Leu-CAMs evolved by ...
Relative Involvement of GPIb/IX-vWF Axis and GPIIb/IIIa in ...
Unfractionated commercial ammonium salt of ATA (Sigma Chimie) was dissolved in PBS, pH 7.4, and filtered through a 22-μm filter (Millipore). 26 Lamifiban (Ro44-9883), kindly provided by Dr S. Roux (F. Hoffmann-La Roche, Basel, Switzerland), is a synthetic nonpeptidic GPIIb/IIIa inhibitor with an IC 50 of 450 nmol/L in guinea pig platelet-rich ...
ME3277, a GPIIb/IIIa Antagonist Reduces Cerebral ...
followed by rethrombosis in guinea pigs and primates (Kaku et aI., 1998; Kawano et aI., 1998). The effect of a nonpeptide GPIIb/IIIa antagonist, ME3277 (sodium hy drogen [4-[(4,5,6,7-tetrahydrothieno [3, 2-c] pyridin - 2-yl) carbonylamino] acetyl-o-phenylene] dioxydiac etate) in a guinea …
FK419, a Novel Nonpeptide GPIIb/IIIa Antagonist, Restores ...
in vitro antiplatelet profile and efficacy in a guinea-pig photochemically induced MCA occlusion of FK419 to clarify its potential for the treatment of acute ischemic stroke in comparison with tirofiban which is well-evaluated GPIIb/IIIa antagonist. Materials and methods Animals Male Hartley guinea-pigs …
MPS IIIA - Lysogene
MPS IIIA - Lysogene. Mucopolysaccharidosis type IIIA (MPS IIIA), or Sanfilippo syndrome type A, is a rare neurodegenerative lysosomal storage disorder that typically appears in infancy or early childhood. It affects about 1 in 100,000 births and about 2,500 to 3,000 children globally.
Profound and sustained inhibition of platelet aggregation ...
BACKGROUND Clinical trials have demonstrated that platelet glycoprotein (GP) IIb/IIIa antagonists effectively prevent acute thrombotic events. Orally active GP IIb/IIIa antagonists are essential to evaluate the clinical benefit of long-term treatment. We therefore investigated platelet inhibition by the GP IIb/IIIa antagonist Fradafiban (BIBU 52; Fradafiban is the recommended INN of BIBU 52 ...
ASN Aircraft accident Lockheed 414-56 Hudson IIIA VH-ALA ...
A Lockheed 414-56 Hudson IIIA passenger plane, registered VH-ALA, was destroyed in an accident 4 km W of Lae Airfield, Papua New Guinea. There were 35 passengers and two crew members on board. The airplane operated on a flight from Lae Airfield to Bulolo Airport (BUL).
Optimal Antagonism of GPIIb/IIIa Favors Platelet Adhesion ...
Jan 01, 1996· Guinea pig platelet membrane glycoproteins have been found to exhibit a very close homology to human platelet GPIIb/IIIa and GPIb/IX, 11 12 and their platelet functions resemble those of human platelets in their responsiveness to ADP and the …
Inhibitory effect of a novel orally active GP IIb/IIIa ...
The inhibitory effect of a novel orally active platelet membrane glycoprotein receptor complex IIb/IIIa (GP IIb/IIIa) inhibitor, SC-54684A is studied on intimal thickening in the guinea pig femoral artery. A segment of the femoral artery was occluded by a platelet-rich thrombus induced by photochemical reaction between systemically administered Rose Bengal and transluminal green light which ...
Targeting Platelets in Acute Experimental Stroke | Circulation
Apr 16, 2007· 48 Moriguchi A, Maeda M, Mihara K, Aoki T, Matsuoka N, Mutoh S. FK419, a novel nonpeptide GPIIb/IIIa antagonist, restores microvascular patency and improves outcome in the guinea-pig middle cerebral artery thrombotic occlusion model: comparison with tirofiban. J Cereb Blood Flow Metab. 2005; 25: 75–86. Crossref Medline Google Scholar
Antithrombotic Effects of FK419, a Novel Nonpeptide ...
Mar 01, 2004· Antithrombotic Effects of FK419, a Novel Nonpeptide Platelet GPIIb/IIIa Antagonist, in a Guinea Pig Photochemically Induced Middle Cerebral Artery Thrombosis Model: Comparison with Ozagrel and Argatroban. Akira Moriguchi, Toshiaki Aoki, Kayoko Mihara, Nobuteru Tojo, Nobuya Matsuoka and Seitaro Mutoh.
Antithrombotic effect of SM-20302, a nonpeptide GPIIb/IIIa ...
May 15, 1999· 1. Thromb Res. 1999 May 15;94(4):227-34. Antithrombotic effect of SM-20302, a nonpeptide GPIIb/IIIa antagonist, in a photochemically induced thrombosis model in guinea pigs.
Synthetic Inhibitors of Platelet Glycoprotein IIb/IIIa in ...
Feb 15, 2000· Abstract—Activation of the platelet glycoprotein (GP IIb/IIIa) receptor on the platelet surface is the final pathway of platelet aggregation, regardless of the initiating stimulus. Inhibitors of GP I
Antagonism of the GPIIb/IIIa Receptor with the Nonpeptidic ...
In the guinea pig aorta, BIBU52 inhibited thrombus formation dose dependently, with lack of thrombus formation for 1 h after a bolus dose of 1.0 mg/kg i.v.. Both acetylsalicylic acid and dazoxiben were less effective in this model. ... GPIIb/IIIa is a member of the integrin family of adhesion receptors and binds to ligands containing a specific ...
Antithrombotic Effects of FK419, a Novel Nonpeptide ...
Mar 01, 2004· Antithrombotic Effects of FK419, a Novel Nonpeptide Platelet GPIIb/IIIa Antagonist, in a Guinea Pig Photochemically Induced Middle Cerebral Artery Thrombosis Model: Comparison with Ozagrel and Argatroban. Akira Moriguchi, Toshiaki Aoki, …
Aircraft Photo of VH-BLA | Lockheed 414 Hudson IIIA ...
Aircraft photo of VH-BLA - Lockheed 414 Hudson IIIA - Guinea Air Traders, taken by Ben Dannecker (via David Carter) at Archerfield (YBAF) in Queensland, Australia between August 1948 and June 1950. Reregistered VH-AGG in September 1950.
A New Compartment at Stereocilia Tips Defined by Spatial ...
Oct 04, 2006· Class III myosins are motor proteins that contain an N-terminal kinase domain and a C-terminal actin-binding domain. We show that myosin IIIa, which has been implicated in nonsyndromic progressive hearing loss, is localized at stereocilia tips. Myosin IIIa progressively accumulates during stereocilia maturation in a thimble-like pattern around the stereocilia tip, distinct from the cap-like ...
Antithrombotic effects of TAK-029, a novel GPIIb/IIIa ...
Apr 01, 1996· The antithrombotic and bleeding time (BT)-prolonging effects of TAK-029, a novel glycoprotein IIb/IIIa antagonist, were characterized and compared with those of conventional antithrombotic agents in guinea pigs. TAK-029 potently inhibited the binding of fibrinogen and von Willebrand factor to purified human GPIIb/IIIa with IC50 values of 0.67 +/- 0.03 and 0.33 +/- 0.04 nM; …
Restoration of middle cerebral artery thrombosis by novel ...
Sep 13, 2004· Though inhibition of PAI-1 secretion was not confirmed in guinea pig platelets, inhibition of PAI-1 release could be involved in its beneficial effects in this stroke model. The recanalization promoting efficacy of glycoprotein IIb/IIIa antagonist was also observed in rat embolic stroke model (Yang et al., 2001). Rt-PA has been well known as a ...
Relative involvement of GPIb/IX-vWF axis and GPIIb/IIIa in ...
Relative involvement of GPIb/IX-vWF axis and GPIIb/IIIa in thrombus growth at high shear rates in the guinea pig. André P(1), Hainaud P, Bal dit Sollier C, Garfinkel LI, Caen JP, Drouet LO. Author information: (1)INSERM U353, Paris, France.