FK-352
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Grundinformationen
- CAS
143881-08-7- Standard-SMILES
O=C(O)C[C@H]1CCCCN1C(=O)/C=C/c1c(-c2ccccc2)nn2ccccc12- InChIKey
UWTYIJJJSYDUQM-QFQMRYFISA-N- Summenformel
- C23H23N3O3
- Durchschnittliche Molmasse
- 389,4 g/mol
Überblick
FK352B is a adenosine A1 antagonist that is developed for the treatment of dialysis-induced hypotension.
Namen und Bezeichner
- Bevorzugter Name
- FK-352
- IUPAC
- 2-[(2R)-1-[(E)-3-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)prop-2-enoyl]piperidin-2-yl]acetic acid
Namen und Synonyme
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Datenbank-Bezeichner
- CAS
143881-08-7- PubChem CID
- 6442241
- UNII
- H7CU6R2QEX
- Nikkaji
- J895.813K
Eigenschaften
Berechnete StruktureigenschaftenWird ergänzt
- XLogP
- 3
- Polarare Oberfläche (TPSA)
- 74,9 Ų
- H-Brücken-Donoren
- 1
- H-Brücken-Akzeptoren
- 4
- Frei drehbare Bindungen
- 5
- Schwere Atome
- 29
- Formalladung
- 0
- Komplexität
- 616
Chemie und Industrie
Pharmakologische Informationen
Mechanism of Action
Intradialytic hypotension is a most frequent complication of hemodialysis and may contribute to cardiovascular events and high mortality. There is a hypothesis that an increase in adenosine generation during hemodialysis may cause vasodilation and a decrease in cardiac output, which results in systemic hypotension. The A1 receptors, which are reported to be distributed in the ends of sympathetic nerves, suppress the release of catecholamines from the ends of the nerves. Adenosine selectively inhibits contractions of the rabbit portal vein evoked by adrenergic nerve stimulation via activation of an A1 receptor. This means that adenosine could inhibit constriction of peripheral vessels via the A1 receptors in the ends of the nerves. FK352, a highly selective A1 adenosine receptor antagonist, significantly attenuated LPS-induced reductions in renal blood flow and mean arterial pressure. It may restore the adenosine-induced decline in constriction.
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