V116517 是一种有效的口服活性瞬时受体电位香草醛(TRPV1)拮抗剂。V116517 在表达天然 TRPV 的大鼠 DRG 神经元中显示出抑制辣椒素 (CAP) 和酸 (pH 5) 诱导电流的有效活性 (对于CAP，IC50=423.2 nM；对于acid，IC50=180.3 nM)。V116517 可用于疼痛的研究。
| 生物活性 | V116517 is a potent, orally active transient receptor potential vanilloid(TRPV1)antagonist. V116517 shows potent activity in inhibiting both capsaicin (CAP)- and acid (pH 5)-induced currents in rat DRG neurons expressing nativeTRPV(IC50=423.2 nM for CAP; IC50=180.3 nM for acid). V116517 can be used for the research of pain[1]. |
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体外研究
(In Vitro) | V116517 is highly selective for TRPV1 and did not show potency up to 10 μM in both TRPV3 and TRPV4 assays[1].
V116517 has fast-off kinetics for antagonism of both mode activations of TRPV1[1].
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体内研究
(In Vivo) | V116517 shows dose-dependent reversal of thermal hyperalgesia with an ED50 of 2 mg/kg (PO) in complete Freund’s adjuvant (CFA) inflammatory pain model[1].
V116517 exhibits high oral bioavailability (rat 74%, dog 100%, monkey 107%) and Cmax (rat 1380, dog 1120, monkey 459 ng/mL) following oral administration (rat 3, dog 3, monkey 3 mg/kg)[1].
V116517 exhibits terminal elimination half-lives (rat 3.3, dog 3.6 and, monkey 18 h) due to high plasma clearance (0.24, 0.28, and 0.36 L/h/kg respectively) combined with large volumes of distribution (0.68, 1.2, and 6.0 L/kg respectively) following intravenous administration (rat 1, dog 1 and, monkey 1 mg/kg)[1].
V116517 (rat 3 mg/kg; oral administration) is primarily restricted in periphery.The ratio of brain-to-plasma concentration is 0.09 at 3 h[1].
| Animal Model: | Male Sprague-Dawley rats (6 weeks, 180-280 g) bearing acute inflammatory CFA model[1] | | Dosage: | 0.3, 1, 3, 10, 30 mg/kg | | Administration: | Oral administration | | Result: | Dose-dependently reversed inflammatory thermal hyperalgesia. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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