Role of cannabinoid receptor agonists in mechanisms of suppression of central pain syndrome

Кукушкин, М. Л.; Igonʼkina, S. I.; Churyukanov, M.V.; Churyukanov, V. V.; Bobrov, M. Yu.; Безуглов, В. В.; Gretskaya, Nataliya

doi:10.1007/s10517-006-0286-x

Cited by 6 publications

(9 citation statements)

References 10 publications

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“…, 2001; Lim et al. , 2003) and penicillin‐induced central pain in rodents (Kukushkin et al. , 2006).…”

Section: Discussionmentioning

confidence: 99%

“…In line with our result, i.t. application of WIN has been shown to suppress CFA-induced allodynia, carrageenan-induced thermal hyperalgesia (Richardson et al, 1998a;Martin et al, 1999), capsaicin-induced thermal and mechanical hyperalgesia (Johanek et al, 2001), formalin-induced persistent nociceptive behaviours (Yoon and Choi, 2003;Kang et al, 2007), peripheral nerve injuryinduced neuropathic pain (Fox et al, 2001;Lim et al, 2003) and penicillin-induced central pain in rodents (Kukushkin et al, 2006). In addition, i.c.v.…”

Section: Discussionmentioning

confidence: 99%

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Peripheral and central sites of action for the non‐selective cannabinoid agonist WIN 55,212‐2 in a rat model of post‐operative pain

Zhu

Mikusa

Fan

et al. 2009

British J Pharmacology

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Both CB(1) and CB(2) receptors were involved in the peripheral anti-allodynic effect of systemic WIN in a pre-clinical model of post-operative pain. In contrast, the centrally mediated anti-allodynic activity of systemic WIN is mostly due to the activation of CB(1) but not CB(2) receptors at both the spinal cord and brain levels. However, the increased potency of WIN following i.c.v. administration suggests that its main site of action is at CB(1) receptors in the brain.

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“…, 2001; Lim et al. , 2003) and penicillin‐induced central pain in rodents (Kukushkin et al. , 2006).…”

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Peripheral and central sites of action for the non‐selective cannabinoid agonist WIN 55,212‐2 in a rat model of post‐operative pain

Zhu

Mikusa

Fan

et al. 2009

British J Pharmacology

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“…5HT‐3 is widely expressed on central and peripheral nervous tissue, particularly the vomiting centers of the brain stem and autonomic innervation of the gastrointestinal organs . Further, 5HT‐3 receptors may be involved in peripheral nociception and perception of central pain . It is noteworthy that headache is a commonly reported side effect among most marketed 5HT‐3 antagonists such as ondansetron .…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics, Safety, and Tolerability Evaluation of Single and Multiple Doses of GSK3342830 in Healthy Volunteers

Tenero

Farinola

Berkowitz

et al. 2018

Clinical Pharm in Drug Dev

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This was a first‐time‐in‐human randomized, double‐blind, single‐center, placebo‐controlled dose‐escalation study to determine the safety, tolerability, and pharmacokinetic (PK) profiles of GSK3342830 after single and repeat intravenous doses in healthy adult subjects (NCT0271424). Sixty‐two subjects were enrolled: 48 subjects in part 1 (single dose) and 14 subjects in part 2 (multiple doses). Following single intravenous infusions, total systemic exposure of GSK3342830 was dose proportional over the 250‐ to 6000‐mg dose range evaluated, whereas peak exposure was approximately dose proportional over the dose range. Following repeat intravenous infusions 3 times a day, GSK3342830 showed time invariance with no drug accumulation. Steady state was reached before day 3, and approximately 90% of GSK3342830 was excreted unchanged in urine. All 48 subjects in part 1 (100.0%) completed the study. In part 2, 9 subjects (64.3%) completed the study, and 5 subjects, all receiving GSK3342830, discontinued early (35.7%), 4 after experiencing fever, headache, and malaise, whereas 1 subject met predefined criteria for drug discontinuation because of transaminitis. GSK3342830 demonstrated PK consistent with other cephalosporin‐class antibiotics but poor tolerability following multiple doses in healthy volunteers.

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“…Thus, in the spinal cord the AEA is antinociceptive that is realized through the activation of TRPV1 receptors. Effects of AEA and WIN 55,212-2 have been studied in regard to the experimentally induced central pain syndrome in rats [77] .…”

Section: Peripheral Nervous Systemmentioning

confidence: 99%

Addictive neurons

2018

Ther Targets Neurol Dis

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Since the reward center is considered to be the area tegmentalis ventralis of the hypothalamus, logically its neurons could mainly be responsible for addiction. However, the literature asserts that almost any neurons of CNS can respond to one or another addictive compound. Obviously not only addictive nicotine, but also alcohol, amphetamine, cannabis, cocaine, heroin and morphine may influence dopaminergic cells alone in VTA. Moreover, paradoxically some of these drugs ameliorate symptoms, counterbalance syndromes, cure diseases and improve health, not only those related to the CNS and in adults, but also almost all other organs and in children, e.g. epilepsy.

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Role of cannabinoid receptor agonists in mechanisms of suppression of central pain syndrome

Cited by 6 publications

References 10 publications

Peripheral and central sites of action for the non‐selective cannabinoid agonist WIN 55,212‐2 in a rat model of post‐operative pain

Peripheral and central sites of action for the non‐selective cannabinoid agonist WIN 55,212‐2 in a rat model of post‐operative pain

Pharmacokinetics, Safety, and Tolerability Evaluation of Single and Multiple Doses of GSK3342830 in Healthy Volunteers

Addictive neurons

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