dizocilpine-maleate has been researched along with efaroxan* in 2 studies
2 other study(ies) available for dizocilpine-maleate and efaroxan
| Article | Year |
|---|---|
Possible role of NMDA receptors in antinociception induced by rilmenidine in mice in the formalin test.
The aim of the study was to investigate the possible role of MK-801, an NMDA antagonist, in analgesia induced by rilmenidine, an imidazoline (I(1)) agonist, in mice in the formalin test.. 25 microl of formalin 2.5% was injected into the dorsal surface of the right hind paw of the mouse. Pain response was scored after formalin injection for a period of 50 min. A weighted average of nociceptive score, ranging from 0 to 3, was calculated. The mean +/-SEM of scores between 0-5 and 15-40 min after formalin injection was presented.. The study showed that rilmenidine (1.25, 2.5 and 5 mg/kg, i.p.) produced analgesia dose-dependently (p<0.001) in formalin test. In addition, the results demonstrated that efaroxan (0.1 and 1 mg/kg, i.p.) could reduce the antinociceptive effect of rilmenidine (2.5 mg/kg, i.p.) (p<0.01) in animals, however, yohimbine (0.1 and 0.2 mg/kg, i.p.) could not block the analgesia induced by rilmenidine (2.5 mg/kg, i.p.) (p>0.05). On the other hand, MK-801 (0.05 mg/kg, i.p.) reduced the pain related behaviors in mice (p>0.05). Moreover, our findings demonstrated that MK-801 (0.01 mg/kg, i.p.) could potentiate the analgesic effect of rilmenidine (1.25 mg/kg, i.p.) significantly (p<0.01).. The present study suggests that imidazoline (I(1)) receptors play an important role in mediating the antinociception induced by rilmenidine in formalin test. Furthermore, it may be concluded that there is an interaction between NMDA receptors and imidazoline (I(1)) binding sites. Topics: Adrenergic alpha-Agonists; Adrenergic alpha-Antagonists; Analgesics; Animals; Benzofurans; Binding Sites; Binding, Competitive; Dizocilpine Maleate; Dose-Response Relationship, Drug; Drug Synergism; Excitatory Amino Acid Antagonists; Imidazoles; Imidazoline Receptors; Male; Mice; Nervous System; Neurons, Afferent; Nociceptors; Oxazoles; Pain; Pain Measurement; Receptors, Drug; Receptors, N-Methyl-D-Aspartate; Rilmenidine; Yohimbine | 2007 |
Evidence that the ability of imidazoline compounds to stimulate insulin secretion is not due to interaction with sigma receptors.
Recent studies have suggested that a variety of ion channels possess a binding site for ligands such as phencyclidine (PCP), dizocilpine and certain sigma ligands and that some imidazoline compounds can also bind to this site. We have investigated whether interaction with this binding site could account for the ability of imidazolines to stimulate insulin secretion from rat islets. Neither PCP nor dizocilpine shared the insulin secretory activity of the imidazoline efaroxan in rat islets suggesting that they do not have similar actions in the pancreatic B-cell. Further, we were able to define a new antagonist, KU14R (2(2-ethyl 2,3-dihydro-2-benzofuranyl)-2-imidazole), which selectively blocks the insulin secretory response to imidazolines. The results suggest that imidazolines do not stimulate insulin secretion by causing physical blockade of the K(+)-ATP channel in pancreatic B-cells and show that their effects are not reproduced by PCP or sigma receptor ligands. Topics: Adenosine Triphosphate; Animals; Benzofurans; Dizocilpine Maleate; Imidazoles; Imidazoline Receptors; In Vitro Techniques; Insulin; Insulin Secretion; Islets of Langerhans; Ligands; Phencyclidine; Potassium Channels; Rats; Rats, Wistar; Receptors, Drug; Receptors, sigma | 1997 |