Mavatrep

Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with high affinity for hTRPV1 channels ( K i =6.5 nM). Mavatrep antagonizes capsaicin-induced Ca 2+ influx with an IC 50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain. In Vitro Mavatrep (series of decreasing concentrations from 1 μM; 25 min) inhibits capsaicin-induced Ca 2+ influx in HEK293 cells expressing TRPV1 channels. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: HEK293 cells (stably expressing TRPV1 channels) Concentration: Series of decreasing concentrations from 1 μM Incubation Time: 25 min Result: Inhibited capsaicin-induced Ca 2+ influx with an IC 50 value of 4.6 nM. In Vivo Mavatrep (1, 3, 10, 30 mg/kg; p.o.; single) shows complete reversal of thermal hypersensitivity both in CFA model of inflammatory of pain and (0.1, 0.3, 1, 3, 10 mg/kg) carrageenan model of inflammatory pain . Mavatrep (10 mg/kg; p.o.; single) exhibits substantial bioavailability in the rat (51%) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats (195-350 g; CFA model of inflammatory of pain) . Dosage: 10 mg/kg Administration: Oral administration, single. Result: Significantly reversed CFA-induced thermal hypersensitivity, beginning 30 min after administration and lasting for at least 3 h. Animal Model: Male Sprague-Dawley rats (195-350 g; CFA model of inflammatory of pain) . Dosage: 1, 3, 10, 30 mg/kg Administration: Oral administration, single. Result: Exhibited complete reversal of thermal hypersensitivity, with ED 50 and ED 80 values of 1.8 and 7.8 mg/kg, and the corresponding plasma levels were 41.9 and 270.8 ng/mL, respectively. Animal Model: Male Sprague-Dawley rats (195-350 g; carrageenan model of inflammatory pain) . Dosage: 0.1, 0.3, 1, 3, 10 mg/kg Administration: Oral administration, single. Result: Completely reversed carrageenan-induced thermal hypersensitivity, with ED 50 and ED 80 values of 0.18 and 0.48 mg/kg, and the corresponding plasma levels were 3.8 and 9.2 ng/mL, respectively. Animal Model: Male Sprague-Dawley rats (195-350 g) . Dosage: 2 mg/kg (for i.v.); 10 mg/kg (for p.o.). (Dissolved in 20% HPβCD) Administration: Oral administration, single. Result: 1.19 Pharmacokinetic Parameters of Mavatrep in male Sprague-Dawley rats . IV (2 mg/kg) PO (10 mg/kg) CL (mL/min/kg) V ss (L/kg) T 1/2 (h) C max (ng/mL) AUC max (ng•h/mL) T 1/2 (h) F (%) 33 10 3.4 421 4203 3.8 51 Form:Solid

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