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AMG 517

CAS No. : 659730-32-2

MCE 站：AMG 517

产品活性：AMG 517是有效的香草素受体-1 (TRPV1) 拮抗剂，IC₅₀值为0.5 nM。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：TRP Channel

In Vitro: AMG 517 retains potency in the capsaicin- and acid-mediated assays with IC₅₀ values of 0.9 and 0.5 nM. AMG 517 inhibits capsaicin, pH 5, and heat-induced⁴⁵Ca²⁺ uptake into cells expressing TRPV1 with IC₅₀ values of 1 to 2 nM. AMG 517 blocks capsaicin-, proton-, and heat-induced inward currents in TRPV1-expressing cells similarly. AMG 517 inhibits native TRPV1 activation by capsaicin in rat dorsal root ganglion neurons with an IC50 value of 0.68 ± 0.2 nM. AMG 517 is a competitive antagonist of both rat and human TRPV1 with dissociation constant (Kb) values of 4.2 and 6.2 nM, respectively.

In Vivo: AMG 517 is shown to be effective in a rodent “on-target” biochemical challenge model (capsaicin-induced flinch, ED₅₀=0.33 mg/kg p.o.) and is antihyperalgesic in a model of inflammatory pain (CFA-induced thermal hyperalgesia, MED=0.83 mg/kg, p.o.).The minimally effective dose is 0.3 mg/kg for AMG 517 and the corresponding plasma concentration is 90 ng/mL. Oral administration of AMG 517 reverses established thermal hyperalgesia in a dose-dependent manner at 21 h after CFA injection. AMG 517 causes transient hyperthermia in rodents, dogs, and monkeys. AMG 517 induces hyperthermia in a steep dose-dependent manner, with 0.3, 1, and 3 mg/kg associated with 0.5, 0.6, and 1.6°C increases in body temperature, respectively. Body temperatures of rats treated with all doses of AMG 517 return to baseline within 10 to 20 h.

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