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JYL 1421 is a TRPV1 receptor antagonist, with an IC50 of 8 nM.

Incubation with JYL 1421 for 5 min concentration-dependently inhibits the capsaicin (330 nM)-evoked Ca2+ accumulation. The inhibitory effect of the lowest concentration (5 nM) of JYL 1421 reaches the level of significance and 1 μM almost abolishes the response, only 3.1±0.65% of the first capsaicin-induced Ca2+ influx could be observed. The IC50 value is 8 nM for JYL 1421. Meanwhile, the effect of capsazepine is markedly smaller, it induces 41.7% inhibition in 1 μM concentration, but this inhibitory effect does not increase further in 10 μM and does not reach 50%[1].

Instillation of 50 μL capsaicin solution (10 μg/mL) into the left eye of the rat evokes 12.9±1.3 wiping movements within 3 min. Pretreating the rats with 0.4 or 1 mg/kg i.p. JYL 1421 does not influence significantly the wiping behavior, but 2-5 mg/kg dose-dependently reduces the number of wiping movements. The ID50 value is 4.6 mg/kg. The mean arterial pressure of untreated rats is 109.9±4.2 Hgmm (n=6). One and 2 μg/kg capsaicin i.v. injection evokes a transient drop of blood pressure by 47.4±4.7 and 59.6±4.2 Hgmm (n=6), respectively. Both applied doses of JYL 1421 (0.4 and 1.6 mg/kg) fail to evoke hypotension. JYL 1421 dose-dependently inhibits the capsaicin-induced fall in blood pressure as shown by the need for higher capsaicin doses to elicit the reflex hypotension after JYL 1421 administration than before treatment. Capsazepine fails to induce a significant inhibition of the capsaicin-evoked hypotension up to a dose of 2 mg/kg[1].

[1]. Jakab B, et al. Pharmacological characterization of the TRPV1 receptor antagonist JYL1421 (SC0030) in vitro and in vivo in the rat. Eur J Pharmacol. 2005 Jul 4;517(1-2):35-44.

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