IRL-1620

The plasma membrane of porcine lung (2 ug of protein) is incubated at 37°C for 1 hr with 30 pM [¹²⁵I]ET-1 or 10 pM [¹²⁵I]ET-3 in the absence or presence of various amounts of nonlabeled ligands (IRL-1620) in a total volume of 1 mL of assay buffer. After the incubation, unbound [¹²⁵I]ETs are separated and radioactivity in the membrane pellet is measured in an autogamma counter^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Rats: Specific ETB receptor agonist, IRL-1620 (5 μg/kg) and specific ETB receptor antagonist, BQ788 (1 mg/kg) are administered intravenously (i.v.) on day 8. IRL-1620 is administered on day 8 three times at a dose of 5 μg/kg, i.v. at 2-h intervals between each injection^[2].

Mice: Tolerance to morphine is induced using a 3-day cumulative dosing regimen. Morphine treatment schedule consisted of twice-daily s.c. injections of morphine for three days given at (i) 30 mg/kg (a.m.) and 45 mg/kg (p.m.) on day 1; (ii) 60 mg/kg (a.m.) and 90 mg/kg (p.m.) on day 2; and (iii) 120 mg/kg twice (a.m. and p.m.) on day 3. The IRL-1620 treatment schedule consists of three times-daily injections of IRL-1620 for two days given at 5 μg/kg, i.v. spaced apart every 2 h on days 1 and 3. At the end of the treatment schedule, a challenge dose of morphine (5 mg/kg, s.c.) is administered on day 4 to assess tolerance^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.