The effect of naloxonazine, a selective mu(1)-opioid receptor antagonist, on oxycodone-induced antinociception was examined in streptozotocin-induced diabetic mice. Oxycodone (5 mg/kg, s.c.) induced significant antinociception in both non-diabetic and diabetic mice. This antinociceptive effect of oxycodone was completely antagonized by pretreatment with naloxonazine (35 mg/kg, s.c.) in both non-diabetic and diabetic mice. The selective kappa-opioid receptor antagonist nor-binaltorphimine (20 mg/kg, s.c.) also antagonized oxycodone-induced antinociception in diabetic mice, but only had a partial effect in non-diabetic mice. These results suggest that although primarily interacts with mu(1)-opioid receptor, kappa-opioid receptors are also strongly involved in oxycodone-induced antinociception.

Eur J Pharmacol. 2007 Apr 10;560(2-3):160-2. Epub 2007 Jan 19.

O-4394 and O-4395 exhibit similar in vitro potencies to eDelta(9)-THCV as CB(1) receptor ligands and as antagonists of cannabinoid receptor agonists and can antagonize Delta(9)-tetrahydrocannabinol in vivo.

Br J Pharmacol. 2007 Mar;150(5):586-94. Epub 2007 Jan 22.

Gotta take the dog out!!!
beachguy in thongs Reviewed by beachguy in thongs on . Wondering about a particular effect of THC on the MU1 receptor-agonist mechanisms Last night I was in a significantly extra large amount pain so I took an extra dose of tramadol (a morphine receptor agonist), and now I've woken up at 3:00am with seratonin blasting through my brain. I'm unable to sleep because my brain is utterly excited, eccentric and wildly creative in thought, enthusiastic and possitive in outlook (as opposed to the usual as of late), and overal very clear thinking. I attribute this to the increase and reuptake-inhibition of seratonin triggered by tramadol Rating: 5