RGD Reference Report - Pharmacodynamics and antithrombotic effects after intravenous administration of the new thromboxane A2 receptor antagonist sodium 4-[[1-[[[(4-chlorophenyl)sulfonyl]amino]methyl]cyclopentyl] methyl]benzeneacetate.

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Pharmacodynamics and antithrombotic effects after intravenous administration of the new thromboxane A2 receptor antagonist sodium 4-[[1-[[[(4-chlorophenyl)sulfonyl]amino]methyl]cyclopentyl] methyl]benzeneacetate.
Authors:	Depin, JC Vigie, A Chavernac, G Rousselot, C Lardy, C Guerrier, D
Citation:	Depin JC, etal., Arzneimittelforschung. 1994 Nov;44(11):1203-7.
RGD ID:	11059887
Pubmed:	PMID:7848332 (View Abstract at PubMed)
The antiplatelet and antithrombotic activities of LCB 2853 (sodium 4-[[1-[[[(4-chlorophenyl)sulfonyl]amino]methyl]cyclopentyl] methyl]benzeneacetate, CAS 141335-11-7) a novel thromboxane A2 (TXA2) receptor antagonist were examined after intravenous administration. The correlation between LCB 2853 plasma concentration and ex vivo inhibition of arachidonic acid-induced aggregation was observed in rats, for 4 h, as long as LCB 2853 was detected in plasma by HPLC analysis. Pharmacokinetic parameters were determined. The antithrombotic activity was tested in arterial and venous thrombosis models. In dog coronary stenosis, LCB 2853 shown a very high efficacy (ED50 = 7.2 micrograms/kg), whereas acetylsalicylic acid (ASA) was only active at 3.2 mg/kg and ticlopidine was ineffective at 12.8 mg/kg. In rat venous thrombosis induced by combination of venous injury and blood stasis, perfused LCB 2853 decreased the weight of thrombi in a dose related manner (ED50 = 220 micrograms/kg/min). In a comparative study, at 250 micrograms/kg/min, ticlopidine was less potent and ASA failed to show any protection. The potent immediate efficacy of LCB 2853 and the advantageous comparisons with ASA (which was ineffective in some models) or ticlopidine (which needs metabolization lag time) observed in many models suggest that this compound may have beneficial effects in patients with TXA2-associated disturbances.

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Object Symbol	Species	Term	Qualifier	Evidence	With	Notes	Source	Original Reference(s)
TBXA2R	Human	Venous Thrombosis	treatment	ISO	Tbxa2r (Rattus norvegicus)		RGD
Tbxa2r	Rat	Venous Thrombosis	treatment	IMP			RGD
Tbxa2r	Mouse	Venous Thrombosis	treatment	ISO	Tbxa2r (Rattus norvegicus)		RGD

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Object Symbol	Species	Term	Qualifier	Evidence	With	Notes	Source	Original Reference(s)
Tbxa2r	Rat	positive regulation of blood coagulation		IMP			RGD

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Genes (Rattus norvegicus)

Tbxa2r (thromboxane A2 receptor)

Genes (Mus musculus)

Tbxa2r (thromboxane A2 receptor)

Genes (Homo sapiens)

TBXA2R (thromboxane A2 receptor)

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Pharmacodynamics and antithrombotic effects after intravenous administration of the new thromboxane A2 receptor antagonist sodium 4-[[1-[[[(4-chlorophenyl)sulfonyl]amino]methyl]cyclopentyl] methyl]benzeneacetate.