期刊
EUROPEAN JOURNAL OF PHARMACOLOGY
卷 442, 期 3, 页码 273-278出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/S0014-2999(02)01541-8
关键词
emesis, acute; emesis, delayed; apomorphine; vanilloid; (dog); (ferret)
We evaluated the antiemetic activity of resiniferatoxin, an ultrapotent capsaicin analogue, on cisplatin- and apomorphine-induced emesis in dogs, and on cisplatin-induced acute and delayed emesis in ferrets. In the dog, resiniferatoxin (10 mug/kg, s.c.) 30 min before the injection of cisplatin markedly prevented acute emesis induced by cisplatin. When animals were given resiniferatoxin (10 mug/kg, s.c.) 24 It prior to cisplatin, the emesis was still inhibited, but not significantly. Resiniferatoxin (10 mug/kg, s.c.) 30 min before the administration of apomorphine also significantly reduced the emetic responses induced by apomorphine in dogs. In the ferret, resiniferatoxin (10 mug/kg, s.c.) 30 min prior to cisplatin completely inhibited acute emesis caused by cisplatin (10 mg/kg, i.p.). When ferrets were given resiniferatoxin (10 mug/kg, s.c.) 16 It prior to cisplatin, the emesis was still significantly inhibited. Cisplatin (5 mg/kg, i.p.) induced both acute (0-24 h) and delayed (24-72 h) phase emesis, and a single injection of resiniferatoxin (10 mug/kg, s.c.) at 36 h after cisplatin significantly reduced subsequent emetic responses during the 36-72 h period. These results suggest that resiniferatoxin-related vanilloids may be useful drugs against both acute and delayed emesis induced by cancer chemotherapy. (C) 2002 Elsevier Science B.V. All rights reserved.
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