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Picotamide (CAS 32828-81-2)

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Application:
Picotamide is a dual inhibitor of thromboxane A2 and thromboxane A2 synthase
CAS Number:
32828-81-2
Purity:
≥98%
Molecular Weight:
376.2
Molecular Formula:
C21H20N4O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Picotamide is a dually active thromboxane A2 and thromboxane A2 synthase inhibitor. It has been shown to exhibit platelet inhibitory effects ex vivo and in vitro. It suppresses arachidonic acid, low-dose collagen, and TXA2-induced human platelet aggregation. However, it does not afftect A23187 induced aggregation or primary aggregation by ADP. It has been shown to inhibit the synthesis of TXA2 by platelets in a dose dependent fashion. It has been reported to enhance PGE2 formation, and enhance PGI2 formation by aspirinated endothelial cells. It has also been shown to raise intraplatelet cAMP levels in platelets stimulated with arachidonic acid.


Picotamide (CAS 32828-81-2) References

  1. In vitro effects of picotamide on human platelet aggregation, the release reaction and thromboxane B2 production.  |  Cattaneo, M., et al. 1991. Thromb Res. 62: 717-24. PMID: 1926062
  2. 'In vitro' and 'ex vivo' effects of picotamide, a combined thromboxane A2-synthase inhibitor and -receptor antagonist, on human platelets.  |  Berrettini, M., et al. 1990. Eur J Clin Pharmacol. 39: 495-500. PMID: 1963845
  3. Picotamide protects mice from death in a pulmonary embolism model by a mechanism independent from thromboxane suppression.  |  Gresele, P., et al. 1990. Thromb Haemost. 64: 80-6. PMID: 2274931
  4. The receptor antagonist picotamide inhibits adrenergic and thromboxane-induced contraction of hyperplastic human prostate smooth muscle.  |  Hennenberg, M., et al. 2013. Am J Physiol Renal Physiol. 305: F1383-90. PMID: 24049147
  5. Competitive inhibition of platelet thromboxane A2 receptor binding by picotamide.  |  Modesti, PA., et al. 1989. Eur J Pharmacol. 169: 85-93. PMID: 2532145
  6. Characterization of N,N'-bis(3-picolyl)-4-methoxy-isophtalamide (picotamide) as a dual thromboxane synthase inhibitor/thromboxane A2 receptor antagonist in human platelets.  |  Gresele, P., et al. 1989. Thromb Haemost. 61: 479-84. PMID: 2552606
  7. Acetylsalicylic acid, BM 13.177 and picotamide improve the survival of endotoxin-infused rabbits.  |  Feldhoff, CM., et al. 1988. Thromb Res. 52: 487-92. PMID: 2975872
  8. Inhibition by picotamide of thromboxane production in vitro and ex vivo.  |  Violi, F., et al. 1988. Eur J Clin Pharmacol. 33: 599-602. PMID: 3366163
  9. Picotamide inhibits a wide spectrum of agonist-induced smooth muscle contractions in porcine renal interlobar and coronary arteries.  |  Li, B., et al. 2021. Pharmacol Res Perspect. 9: e00771. PMID: 33929093
  10. Studies on in vitro effect of picotamide on human platelet aggregation in platelet-rich plasma and whole blood.  |  Anfossi, G., et al. 1995. Thromb Res. 77: 399-410. PMID: 7778055
  11. Binding kinetics and antiplatelet activities of picotamide, a thromboxane A2 receptor antagonist.  |  Modesti, PA., et al. 1994. Br J Pharmacol. 112: 81-6. PMID: 8032666
  12. Effect of picotamide on the calcium mobilization and phospholipase C activation in human platelets.  |  Pulcinelli, FM., et al. 1994. Thromb Res. 74: 453-61. PMID: 8085246
  13. Mechanism of the persisting TxA2 receptor antagonism by picotamide.  |  Pulcinelli, FM., et al. 1997. Thromb Res. 85: 207-15. PMID: 9058495

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Picotamide, 10 mg

sc-201334
10 mg
$92.00

Picotamide, 50 mg

sc-201334A
50 mg
$366.00