txa2 receptor

Linotroban(CL-871502) is a potent selective thromboxane (TXA2) receptor antagonist with antithrombotic activity.

Daltroban (SKF 96148) is a specific thromboxane A2 (TXA2) receptor antagonist. Daltroban shows protective effect in reperfusion injury. Daltroban increase intracellular calcium in vascular smooth muscle cells.

sulotroban is a TXA2 receptor antagonist that acts synergistically with iloprost to inhibit TXA2-dependent platelet activation.

LCB-2853 is a potent thromboxane A2 prostaglandin H2 (TXA2 PGH2) receptor antagonist with antiplatelet aggregation, antivasospasm, and antithrombotic effects.

RS-601 is a potent dual leukotriene D4 thromboxane A2 inhibitor that inhibits antigen-induced airway hyperresponsiveness (AHR) and shows asthmatic effects in a guinea pig model of asthma.

Ozagrel (Domenan) is a selective thromboxane A(2) (TXA(2)) synthetase inhibitor with IC50 of 11 nM for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

Ozagrel hydrochloride (OKY-046 HCl) is a selective thromboxane A(2) synthetase inhibitor used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.

NTP42 is an antagonist of thromboxane A2 (TXA2) receptor(IC50 of 3.278 nM)

TPα and TPβ are two isoforms of the human TP receptor, the G protein-coupled receptor (GPCR) that mediates the actions of thromboxane A2 (TXA2). Although their distinct physiological functions have not been fully elucidated, TPβ is believed to be responsible for vascular endothelial growth factor-induced endothelial cell differentiation and migration whereas TPα appears to be the predominant isoform expressed in platelets. CAY10535 is a TP receptor antagonist that shows ~20-fold selectivity for TPβ (IC50 = 99 nM) relative to TPα (IC50 = 1,970 nM) in the inhibition of U46619-mediated Ca2+ mobilization. This compound exhibits relatively poor activity on platelets (IC50 = 985 nM) when inhibiting U-46619-induced platelet aggregation.

KP496 is a selective, dual antagonist for the Thromboxane A2 receptor (TP) and the Leukotriene D4 receptor (cysLT1).

Ifetroban is a potent and selective TxA2 PGH2 receptor antagonist.

KT2-962 is a TXA2 prostaglandin endoperoxide receptor antagonist.

Seratrodast (ABT-001) (INN), a thromboxane A2 (TXA2) receptor (TP receptor) antagonist, is mainly used in the therapy of asthma. It was the first TP receptor antagonist developed as an anti-asthmatic drug and attained marketing qualification in Japan in 1997.

Ifetroban (BMS-180291) sodium is an orally active thromboxane A2 (TXA2) and prostaglandin H2 (PGH2) receptor antagonist used to study myocardial ischemia, stroke, hypertension, thrombosis, and cardiomyopathy.

Ici D1542 is a drug that exhibits both potent, selective TXS inhibition and TXA2 receptor antagonism. Ici D1542 is an effective thromboxane A2 synthase inhibitor and receptor antagonist in vitro.

L-657926 is a stereoselective antagonist of the thromboxane A2 (TxA2) receptor, composed of (-)-9-chlorobenzyl-6-fluoro-1,2,3,4-tetrahydrocarbazol-1-yl acetic acid and (+)-9-chlorobenzyl-6-fluoro-1,2,3,4-tetrahydrocarbazol-1-yl acetic acid. The IC50 values for the (-) and (+) configurations against TxA2 are 0.27 nM and 124 nM, respectively.

YM158 free base is a potent and selective antagonist of the TXA2 and LTD4 receptors (pA2 values of approximately 8.81 and 8.87).

U-46619 is an effective thromboxane A2 (TXA2) agonist and a thromboxane A2 analog (endoperoxide), capable of inducing contraction in the aortic smooth muscle (SM) of mice with a myosin light chain 9 (Myl9) gene deletion.

STA 2 is an analogue of TXA2, a thromboxane receptor in the colonic epithelium.