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Chemical Compound Review:

AC1L42NX 2-[(2S)-1-[2-[(4- carbamimidoylphenyl)carbo...

Synonyms: 176655-58-6, 186909-94-4

Kawamura, M. et al., Kawamura, M. et al., Kawahito, K. et al., Sugihara, H. et al., Tanahashi, N. et al., et al.

Tanahashi, Fukuuchi, Tomita, Tomita, Inoue, Satoh, Abe, Sugihara, Fukushi, Miyawaki, Imai, Terashita, Kawamura, Fujisawa, Kita, Kawamura, Tsuji, Moriya, Terashita, Takada, Kurokawa, Miyazaki, Iwasa, Ogawa,

Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of TAK-029

In a balloon catheter-induced carotid thrombosis model, i.v. administration of TAK-029 significantly inhibited thrombus formation without prolonging BT [1].

High impact information on TAK-029

(S)-4-[(4-Amidinobenzoyl)glycyl]-3-[(methoxycarbonyl)methyl]- 2-oxopiperazine-1-acetic acid, 9 (TAK-029), inhibited in vitro human platelet aggregation with an IC50 value of 0.03 microM and GP IIb-IIIa-fibrinogen binding with an IC50 value of 0.49 nM [2].
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; it also inhibited human platelet aggregation induced by various aggregating agents with IC50 values of 29 to 38 nM [1].
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 [1].
The antithrombotic and bleeding time (BT) prolonging effects of TAK-029, a novel GPIIb/IIIa antagonist, were examined in three arterial thrombosis models [3].
In dogs, TAK-029 at 30 micrograms/kg (i.v.) inhibited ADP-induced ex vivo platelet aggregation by 87% 5 min after administration, and it prevented thrombotic occlusion in injured and stenosed coronary arteries for 22 min without prolonging the BT [3].

Biological context of TAK-029

In conclusion, TAK-029 reduced the platelet activation under the shear forces of an in vitro model, suggesting that TAK-029 is a potential candidate for platelet protection during cardiopulmonary bypass [4].

Anatomical context of TAK-029

Employing video-enhanced contrast (VEC) microscopy, we examined whether TAK-029 (GPIIb/IIIa antagonist) inhibits the adhesion of activated platelets to human brain microvascular endothelial cells (HBEC) in vitro [5].
In monkeys, TAK-029 at 10 micrograms/kg (i.v.) inhibited ADP-induced ex vivo platelet aggregation by 84% and prolonged BT 4.6 times 5 min after the administration, and it prevented thrombotic occlusion in injured and stenosed carotid arteries for 24 min [3].

Gene context of TAK-029

The methods included the comparison of the release of beta-thromboglobulin (beta-TG) between a TAK-029 group (n = 5) and a control group (n = 5) in a mock circulation under a shear force generated by a centrifugal pump [4].

Analytical, diagnostic and therapeutic context of TAK-029

METHODS: Copoly(dl-lactic/glycolic)acid (PLGA) microspheres were used for controlled release of TAK-029 [4-(4-amidinobenzoylglycyl)-3-methoxycarbonyl-2-oxopiperazine++ +-1-acetic acid] [6].
The results showed that the value of deltabeta-TG/deltaT in the TAK-029 group was significantly lower than it was in the control group (4.22 +/- 0.27 x 10(2) ng/ml vs. 7.33 +/- 0.66 x 10(2) ng/ml, respectively) [4].

References

Antithrombotic effects of TAK-029, a novel GPIIb/IIIa antagonist, in guinea pigs: comparative studies with ticlopidine, clopidogrel, aspirin, prostaglandin E1 and argatroban. Kawamura, M., Imura, Y., Moriya, N., Kita, S., Fukushi, H., Sugihara, H., Nishikawa, K., Terashita, Z. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
Novel non-peptide fibrinogen receptor antagonists. 1. Synthesis and glycoprotein IIb-IIIa antagonistic activities of 1,3,4-trisubstituted 2-oxopiperazine derivatives incorporating side-chain functions of the RGDF peptide. Sugihara, H., Fukushi, H., Miyawaki, T., Imai, Y., Terashita, Z., Kawamura, M., Fujisawa, Y., Kita, S. J. Med. Chem. (1998) [Pubmed]
Effects of TAK-029, a novel GPIIb/IIIa antagonist, on arterial thrombosis in guinea pigs, dogs and monkeys. Kawamura, M., Tsuji, N., Moriya, N., Terashita, Z. Thromb. Res. (1997) [Pubmed]
Platelet protective effect of TAK-029, a novel glycoprotein IIb/IIIa antagonist: an in vitro study. Kawahito, K., Fujimura, A., Kobayashi, E., Misawa, Y., Fuse, K. Artificial organs. (1998) [Pubmed]
Adhesion of adenosine diphosphate-activated platelets to human brain microvascular endothelial cells under flow in vitro is mediated via GPIIb/IIIa. Tanahashi, N., Fukuuchi, Y., Tomita, M., Tomita, Y., Inoue, K., Satoh, H., Abe, T. Neurosci. Lett. (2001) [Pubmed]
Utilization of an amorphous form of a water-soluble GPIIb/IIIa antagonist for controlled release from biodegradable microspheres. Takada, S., Kurokawa, T., Miyazaki, K., Iwasa, S., Ogawa, Y. Pharm. Res. (1997) [Pubmed]

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