Disease relevance of Tocris-0889

• An I2 imidazoline ligand, RS 45041, potentiates hyperalgesia in acute arthritis [1].

High impact information on Tocris-0889

• In decerebrated, spinalized rabbits, intrathecal RS-45041-190 (60 microg, single dose) increased spinal reflex responses to 109% of pre-drug values, a significantly smaller effect than that seen in non-spinal preparations, and had no effect on blood pressure [2].
• 3. RS-45041-190 showed moderate potency for the inhibition of monoamine oxidase A in vitro (pIC50 = 6.12), but had much lower potency for monoamine oxidase B (pIC50 = 4.47), neither of which equated with its affinity for I2 receptors [3].
• In conscious rats, RS-45041-190 had no effect on body core temperature or tail skin temperature (1 mg kg-1, s.c.) or on activity or rotarod performance (10 mg kg-1, i.p.). There were also no effects on barbiturate sleeping time in mice after doses of 1-10 mg kg-1, i.p. 5 [3].
• 4. RS-45041-190 (0.001 to 3 mg kg-1, i.v. and 1 ng-50 micrograms i.c.v.) had only small, transient effects on blood pressure and heart rate in anaesthetized rats [3].

References