MTPPA

MTPPA ((Rac)-M-5011) is an orally active anti-inflammatory, analgesic and anti-rheumatic compound. MTPPA mediates the inhibition of prostaglandin biosynthesis. MTPPA acts as a four-point tetrahedral organophosphonate bridging ligand. MTPPA can be used in research related to inflammation, pain and adjuvant arthritis^[1][2]. In Vitro:MTPPA potently inhibits prostaglandin biosynthesis in guinea pig lung homogenate, with an ID₅₀ value of 1.4 μM^[1]. In Vivo:The d-isomer of MTPPA (0.2-1 mg/kg; p.o.; single dose) demonstrates dose-dependent inhibition of acetic acid-induced vascular permeability in rats with an ED₃₀ of 0.52 mg/kg p.o., while racemic MTPPA (0.5-5 mg/kg; p.o.; single dose) has an ED₃₀ of 1.1 mg/kg p.o.^[1].
The d-isomer of MTPPA (1-5 mg/kg; p.o.; single dose) inhibits carrageenin-induced paw edema in rats by up to 57.2% at 5 mg/kg p.o., while racemic MTPPA (1-5 mg/kg; p.o.; single dose) inhibits swelling by up to 48.5% at the same dose^[1].
The d-isomer of MTPPA (1 mg/kg; p.o.; once daily; 7 days) inhibits adjuvant-induced arthritis in rats by 21.6% at 1 mg/kg p.o. daily for 1 week, while racemic MTPPA (1 mg/kg; p.o.; once daily; 7 days) inhibits swelling by 14.4% at the same dose^[1].
The d-isomer of MTPPA (5-20 mg/kg; p.o.; single dose) demonstrates dose-dependent analgesic activity in the phenylbenzoquinone writhing mouse model with an ED₅₀ of 7.5 mg/kg p.o., while racemic MTPPA (5-20 mg/kg; p.o.; single dose) has an ED₅₀ of 9.7 mg/kg p.o.^[1].
The d-isomer of MTPPA (2.5-40 mg/kg; p.o.; single dose) demonstrates dose-dependent analgesic activity in a chronic mouse pain model with an ED₅₀ of 5.2 mg/kg p.o., while racemic MTPPA (2.5-40 mg/kg; p.o.; single dose) has an ED₅₀ of 7.0 mg/kg p.o^[1].