Gyires K, Zádori ZS, Shujaa N, Al-Khrasani M, Pap B, Mózes MM, Mátyus P
Pharmacological analysis of alpha(2)-adrenoceptor subtypes mediating analgesic, anti-inflammatory and gastroprotective actions. [JOURNAL ARTICLE]
Inflammopharmacology 2009 Jun 13.
Our previous findings suggest that alpha(2)-adrenoceptor stimulants induce gastroprotective action, the effect is likely to be mediated by alpha(2B)-adrenoceptor subtype. Clonidine (0.094 mumol/kg p.o.) and rilmenidine (0.014 mumol/kg p.o.) in gastroprotective dose range, as well as ST-91 (2.2 mumol/kg p.o.), a clonidine analogue showing higher affinity to alpha(2B)-adrenoceptor subtype than to alpha(2A)-one, inhibited the carrageenan-induced hyperalgesia in Randall-Selitto test, the antinociceptive action was reversed by yohimbine (5 mumol/kg s.c.) and the alpha(2B)-adrenoceptor antagonist prazosin (0.24 mumol/kg i.p.). Similarly, clonidine and rilmenidine in the same dose range reduced the oedema formation induced by carrageenan, yohimbine and the alpha(2A)-adrenoceptor antagonist BRL-44408 (3 mumol/kg i.p.) inhibited the anti-inflammatory effect; however, prazosin failed to affect it. These results suggest that alpha(2B/C)-like adrenoceptor subtype may be involved in the antihyperalgesic action, but not in the antiphlogistic effect of alpha(2)-adrenoceptor stimulants. The later effect may be mediated by alpha(2A)-like adrenoceptor subtype.
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