The NK1 antagonist GR203040 inhibits cyclophosphamide-induced damage in the rat and ferret bladder.

Abstract

1. The effect of the tachykinin neurokinin1 (NK1) receptor antagonist GR203040 on cyclophosphamide (CYP)-induced bladder damage was investigated in rats and ferrets. The 5-hydroxytryptamine3 receptor antagonists ondansetron and granisetron were similarly examined in ferrets. 2. In the rat, GR203040 (10 and 30 mg/kg i.p.) reduced the CYP-induced plasma protein extravasation in the bladder by 44% and 73%, respectively (P < 0.05 and 0.005; cf. CYP controls); in the ferret, a 57% reduction (P < 0.005) was observed after GR203040 (0.3 mg/kg SC). No decrease was observed in ferrets with either ondansetron or granisetron (1 mg/kg SC). 3. GR203040 attenuated the CYP-induced damage in the rat and ferret bladder, at the same dose in the ferret previously shown to inhibit CYP-induced emesis.

• Authors: A Alfieri, C Gardner
• Journal: General pharmacology (Gen Pharmacol) Vol. 29 Issue 2 Pg. 245-50 (Aug 1997) ISSN: 0306-3623 [Print] England
• PMID: 9251907 (Publication Type: Journal Article)

Chemical References

• Blood Proteins
• Neurokinin-1 Receptor Antagonists
• Piperidines
• Tetrazoles
• (2-methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine
• Cyclophosphamide

Topics

• Animals
• Blood Proteins (metabolism)
• Cyclophosphamide (antagonists & inhibitors, toxicity)
• Ferrets
• Male
• Neurokinin-1 Receptor Antagonists
• Piperidines (pharmacology)
• Rats
• Rats, Wistar
• Tetrazoles (pharmacology)
• Urinary Bladder (anatomy & histology, drug effects)