| Hazard Information | Back Directory | [Description]
FR 113680 is a novel tripeptide substance P antagonist with NK1 receptor selectivity. The inhibitory effect of FR 113680 on SP-induced guinea-pig ileum contraction is competitive and the pA2 value is 7.53. It suggest that FR 113680 interacts selectively with the NK1 neurokinin receptor. | [Uses]
FR 113680 is a tripeptide substance P antagonist that interacts selectively with the NK1 neurokinin receptor[1]. | [in vivo]
FR 113680 (32 mg/kg; i.v.; once) significantly inhibits cigarette smoke-induced plasma extravasation[2]. | Animal Model: | Male Wistar rats, cigarette smoke-induced rat tracheal plasma extravasation model[2] | | Dosage: | 0, 10 and 32 mg/kg | | Administration: | IV, once | | Result: | Significantly inhibited cigarette smoke-induced rat tracheal plasma extravasation at a dose of 32 mg/kg. |
| [References]
[1] Morimoto H, et al. FR 113680: a novel tripeptide substance P antagonist with NK1 receptor selectivity. Br J Pharmacol. 1992 May;106(1):123-6. DOI:10.1111/j.1476-5381.1992.tb14303.x
[2] Morimoto H, et al. Effects of FR 113680 and FK 224, novel tachykinin receptor antagonists, on cigarette smoke-induced rat tracheal plasma extravasation. Eur J Pharmacol. 1992 Nov 24;224(1):1-5. DOI:10.1016/0014-2999(92)94810-i |
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