scholarly journals Ketamine: More than Just NMDA Blocker

2021 ◽  
Author(s):  
Bhargab Deka ◽  
Biswajit Dash ◽  
Alakesh Bharali ◽  
Ashique Ahmed
Keyword(s):  
Chronic Pain ◽  
Nmda Receptors ◽  
Mechanism Of Action ◽  
Clinical Studies ◽  
Cellular Level ◽  
Inhibitory Effects ◽  
Medical Field ◽  
Biochemical Processes ◽  
Opioid Systems ◽  
Light Sleep

Ketamine has been extensively used in the medical field for more than 50 years, but its exact mechanism of action remains unknown. It\'s used to induce dissociative anesthesia (a state of profound analgesia, amnesia with light sleep, immobility, and a sense of disassociation from one\'s own body and surroundings). Clinical studies on ketamine as a dissociative anesthetic, a model for psychosis, and as a rapidly acting antidepressant have sparked great interest in understanding its effects at the molecular and cellular level. It exerts uncompetitive inhibitory effects on NMDARs (N-Methyl-D-asperate) and may preferentially affect the function of NMDARs in interneurons. The hypnotic effects of this drug are attributed to its blocking action on NMDA and HCN1 receptors; however, both positive and negative modulation of choline, amine, and opioid systems appears to occur. It is likely that ketamine\'s effect on chronic pain and depression far outlasts its actual levels. This could be due to the hyperglutamatergic state induced by ketamine causing a secondary increase in structural synaptic connectivity. The authors of this review have attempted to highlight the action of ketamine not only on NMDA receptors but also on a variety of biochemical processes and functions found in intercellular environments, which may explain its diverse role in many diseases.

Inhibitory effects of indicaxanthin on mouse ileal contractility: Analysis of the mechanism of action

2011 ◽  
Vol 658 (2-3) ◽  
pp. 200-205 ◽  
Author(s):  
Sara Baldassano ◽  
Alessandra Rotondo ◽  
Rosa Serio ◽  
Maria Antonietta Livrea ◽  
Luisa Tesoriere ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
Inhibitory Effects

scholarly journals A model of chronic pain in the rat: functional correlates of alterations in the activity of opioid systems

1987 ◽  
Vol 7 (1) ◽  
pp. 77-87 ◽  
Author(s):  
MJ Millan ◽  
A Czlonkowski ◽  
CW Pilcher ◽  
OF Almeida ◽  
MH Millan ◽  
...  
Keyword(s):  
Chronic Pain ◽  
Opioid Systems

Antidepressant Drugs and Migraine

Cephalalgia ◽  
1985 ◽  
Vol 5 (2_suppl) ◽  
pp. 225-228 ◽  
Author(s):  
N Martucci ◽  
V Manna ◽  
A Agnoli
Keyword(s):  
Mechanism Of Action ◽  
Clinical Studies ◽  
Mode Of Action ◽  
Antidepressant Drugs ◽  
Antidepressant Activity

There is evidence that some antidepressant drugs, above all amitriptyline and mianserine, are beneficial in the prophylaxis of migraine. The mechanism of action of antidepressants in migraine is likely to be complex. Mood disturbances accompanying migraine syndromes suggest a mode of action of such a class of drugs. In the last few years some clinical studies tend to show that the antimigraine effects of these drugs seem relatively independent of the antidepressant activity.

scholarly journals Possible Nonopioid-Mediated Analgesia Produced by Methotrimeprazine in Rats

1996 ◽  
Vol 1 (4) ◽  
pp. 207-211
Author(s):  
Perry N Fuchs ◽  
Bradley Kerr ◽  
Ronald Melzack
Keyword(s):  
Mechanism Of Action ◽  
Formalin Test ◽  
Saline Control ◽  
Endogenous Opioid ◽  
Potential Source ◽  
Sedative Effects ◽  
Endogenous Opioid Systems ◽  
Opioid Systems ◽  
Crossing Test ◽  
Line Crossing

BACKGROUND:Several reports in the 1960s demonstrated that methotrimeprazine (MTMZ), a phenothiazine derivative, is effective for treating acute and chronic pain. Although MTMZ has received little attention in recent decades, the fact that it derives from a class of drugs usually associated with cognitive and emotional processes, rather than the traditional analgesics, makes it interesting as a potential source of information about the mechanisms of analgesia.OBJECTIVE:To explore the analgesic properties of MTMZ in a dose-related design in the formalin test, and to examine whether the lowest dose of MTMZ that produces analgesia will activate endogenous opioid systems.METHODS:The analgesic properties of three doses of MTMZ, compared with a saline control, were explored in male Sprague-Dawley rats using the formalin test. Sedative effects were studied by using the line-crossing test concomitantly with the formalin test.RESULTS:MTMZ had no effect during the first phase of formalin responding. During the second phase of the formalin test, MTMZ doses of 5.0 and 10.0 mg/kg produced a significant decrease in formalin responses. Sedative effects were observed at all doses, even though the dose of 2.5 mg/kg did not significantly decrease formalin responses compared with controls. Statistical analyses revealed no significant correlation between the degree of sedation and the degree of analgesia at any dose of MTMZ. The nonspecific opioid antagonist naloxone did not alter the analgesic effect of 5.0 mg/kg MTMZ, indicating that the mechanism of action is independent of endogenous opioid systems.CONCLUSION:MTMZ decreased responses in the formalin pain test in rats. Although the drug's sedative effects were apparent in the line crossing test, they were not significantly correlated with pain responses. These results suggest that the decrease in formalin responses might be due, in part at least, to the analgesic properties of MTMZ. The fact that MTMZ belongs to a class of drugs that is relatively unexplored in relation to pain and analgesia indicates a potential source for the development of new pharmacological agents for treating persistent pain. Furthermore, the nonopioid mechanism of action suggests that this agent may be useful when opioid medications are contraindicated.

Characterization of a zebrafish estrogen-sulfating cytosolic sulfotransferase: inhibitory effects and mechanism of action of phytoestrogens

2004 ◽  
Vol 147 (1) ◽  
pp. 1-7 ◽  
Author(s):  
Kei Ohkimoto ◽  
Ming-Yih Liu ◽  
Masahito Suiko ◽  
Yoichi Sakakibara ◽  
Ming-Cheh Liu
Keyword(s):  
Mechanism Of Action ◽  
Inhibitory Effects
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