Baclofen as an analgesic

Saelens, Jeffrey K.; Bernard, Patrick S.; Wilson, Douglas E.

doi:10.1016/0361-9230(80)90090-8

Cited by 17 publications

(3 citation statements)

References 9 publications

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“…The narcotic analgesics are potent but have several undesirable actions and their use leads to dependence. It is well known that 4(1H)-pyridinone derivatives have shown various pharmacological effects such as antibacterial [1,2], antifungal [3], antimalarial [4,5], cardiotonic agents [6], antihypertensive [7], antineoplastic [8][9][10][11], anti-inflammatory [12], analgesic effects [13][14][15][16], and favourable effect in Parkinson's disease [17,18]. Especially 1,2-dimethyl and 1,2-diethyl-3hydroxy-4(1H)-pyridinone derivatives have shown chelating effect [19][20][21][22][23].…”

Section: Introductionmentioning

confidence: 99%

New 4(1H)-Pyridinone Derivatives as Analgesic Agents

Aytemir

Uzbay²,

Erol

2011

Arzneimittelforschung

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A number of 2-methyl/ethyl-3-hydroxy-4(1H)-pyridinones have been synthesized by reacting with 4-pyrones and primary aromatic amines in ethanol. Their structures were confirmed by microanalysis, IR and 1H-NMR spectral analysis. Possible analgesic and anti-inflammatory activities of the synthesized compounds were investigated by acetic acid-induced writhing and carrageenan rat paw edema tests. All compounds exhibited higher analgesic activities than acetylsalicylic acid, 1-(2-Piperidinoethyl)-2- methyl-3-hydroxy-4-(1H)-pyridinone.2HBr(1), 1-[2-(1-methyl-pyrrolidine-2- yl)-ethyl]-2- methyl-3-hydroxy-4(1H)-pyridinone.2HBr (3) and 1-[2-(1-methyl-pyrrolidine- 2-yl)-ethyl]-2- ethyl-3-hydroxy-4(1H)-pyridinone.2HBr (6) showed higher anti-inflammatory activities than indometacin.

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Section: Introductionmentioning

confidence: 99%

New 4(1H)-Pyridinone Derivatives as Analgesic Agents

Aytemir

Uzbay²,

Erol

2011

Arzneimittelforschung

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“…5 For example, 4-pyrones that are oxygen containing six-membered heterocycles have been known as precursors for the synthesis of 4(1H)-pyridinones for almost a century. 6 The synthesis of 4(1H)-pyridinones have attracted considerable research interest from organic chemists due to their various pharmacological effects like being antibacterial, 7 antifungal, 8 anti-malarial, 9 cardiotonic agents, 10 antihypertensive, 11 antineoplastic, 12 anti-inflammatory, 13 analgesic, 14 and anti-Parkinson's disease. 15 Şener et al 16 performed the synthesis 3-acetyl-5-benzoyl-6-methyl-2-phenyl-4H-pyran-4-one (1a) and 3,5-dibenzoyl-2,6-diphenyl-4-pyrone (1b) and used these pyrone derivatives as precursors for the synthesis of novel pyridinone systems by reacting them with various amines.…”

Section: Introductionmentioning

confidence: 99%

Studies on the Different Reaction Pathways between 3-Acetyl-5-benzoyl-6-methyl-2-phenyl-4H-pyran-4-one and Alkylamines

Genç¹,

Tan²,

Gümüş³

et al. 2010

Bulletin of the Korean Chemical Society

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3-Acetyl-5-benzoyl-6-methyl-2-phenyl-4H-pyran-4-one has been subjected to condensation with a series of primary amines (ethylamine -octylamine) to clarify the proposed mechanism in our previous study. The reactions of the shorter amines of the series (ethylamine -butylamine) yielded unsymmetric pyridinone products, whereas the other amines (pentylamine -octylamine) yielded symmetrical pyridinones. The starting material and the products as well as the intermediates have been subjected to theoretical analysis by quantum chemical calculations at B3LYP/6-31G(d,p) level, which provided supporting data for the experimental findings.

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“…Other reports have shown that GABA agonists can elicit antinociceptive activity without the presence of opioids. Proudfit and Levy [1978], Saelens et al [1980]. and Sawynok and LaBella [ 19841 demonstrated antinociceptive activity of muscimol, and baclofen (GABAB bicuculline insensitive receptor agonist) when given systemically.…”

Section: Introductionmentioning

confidence: 99%

GABA agonists enhance morphine and fentanyl antinociception in rabbit tooth pulp and mouse hot plate assays

Bergman

Wynn

Peterson

et al. 1988

Drug Development Research

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Parallel experiments in the rabbit tooth pulp and mouse hot plate paradigms were performed to elucidate the effect of pretreatment with the GABA mimetic compound muscimol (M) and diazepam (DZ) on the antinociceptive effect of both morphine sulfate (MS) and fentanyl citrate (F). The ED50 values for F in both rabbits and mice were lowered significantly (p < 0.05) by pretreatment with either i.v. DZ or M in rabbits or i.p DZ or i.v. M in mice. There was a significant 7-fold shift of the F dose-response curve after pretreatment with M in rabbits and a 3-fold shift in mice compared to controls; a 10-fold shift after pretreatment with i.v. DZ in rabbits and a 2-fold shift after i.p DZ in mice. completely reversed the enhanced antinociception produced by DZ + MS, whereas scopolamine had no significant effect. These results suggest that GABAA agonists, both direct M and indirect DZ enhance the antinociceptive effect of the opioids F and MS. Since naloxone completely reversed this effect and scopolamine had no significant effect, this implies that GABAA agonists enhance opioid antinociception by an opioid and not a cholinergic mechanism.

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Baclofen as an analgesic

Cited by 17 publications

References 9 publications

New 4(1H)-Pyridinone Derivatives as Analgesic Agents

New 4(1H)-Pyridinone Derivatives as Analgesic Agents

Studies on the Different Reaction Pathways between 3-Acetyl-5-benzoyl-6-methyl-2-phenyl-4H-pyran-4-one and Alkylamines

GABA agonists enhance morphine and fentanyl antinociception in rabbit tooth pulp and mouse hot plate assays

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