GABAergic and cholinergic mediation in the antinociceptive action of homotaurine.

  title={GABAergic and cholinergic mediation in the antinociceptive action of homotaurine.},
  author={I. Serrano and R. Ruiz and J. Serrano and A. Fern{\'a}ndez},
  journal={General pharmacology},
  volume={23 3},
1. The role of GABAergic and cholinergic mechanisms in the antinociceptive effect of homotaurine (22.25-111.24 mg/kg i.p.) in chemical (acetic acid) and thermal (tail flick, tail immersion) tests has been studied by means of the interaction with baclofen and anticholinergic drugs. 2. Baclofen (2 mg/kg p.o.) and scopolamine sulfate (2.5 mg/kg i.p.) potentiate the antinociceptive effect of the amino acid in the chemical test. 3. Bicuculline (1 mg/kg i.p.) pretreatment does not modify the… Expand
GABA(B) receptors and opioid mechanisms involved in homotaurine-induced analgesia.
Data imply that GABA(B) receptor subpopulations and opiate mechanisms are involved in the antinociceptive effect of homotaurine, and an interaction of the two mechanisms may be operating in the effects described. Expand
Role of GABAA and GABAB receptors and peripheral cholinergic mechanisms in the antinociceptive action of taurine.
The results suggest that the antinociceptive effect of taurine may be partly mediated by spinal GABAA receptors and peripheral cholinergic mechanisms. Expand
Role of K+‐channels in homotaurine‐induced analgesia
Results suggest an involvement of the three types of K+‐channels in antinociception by homotaurine, depending on specific hom Minotaurine and blocker doses. Expand
Pharmacology of GABAB Receptors
It is now about 20 years since we first examined the Cl−-dependent action of GABA on peripheral neurones and, in particular, on nerve terminals of sympathetic fibres. At the time we were trying toExpand
International Union of Pharmacology. XXXIII. Mammalian γ-Aminobutyric AcidB Receptors: Structure and Function
The emergence of high-affinity antagonists for GABAB receptors has enabled a synaptic role to be established, however, the antagonists have generally failed to establish the existence of pharmacologically distinct receptor types within the GABAB receptor class. Expand
GABAB Receptor ad a Potential Therapeutic Target
This chapter seeks to examine the potential significance of agonists and also of allosteric modulators for the receptor, which have been recognized during the past 5 yr, and there seems to be every reason to believe that the rewards for discovering clinically available GABA-B receptor ligands could be high. Expand
Radiation protection following nuclear power accidents: a survey of putative mechanisms involved in the radioprotective actions of taurine during and after radiation exposure
It is proposed that taurine may have radioprotective effects by a combination of several mechanisms: 1 during the exposure to ionizing radiation by functioning as an antioxidant, but perhaps more because it counteracts the prooxidant catalytic effect of iron, 2 after the ionizing Radiation exposure by helping to reduce the intensity of the post-traumatic inflammatory response, and thus reducing the extent of tissue damage. Expand
Mammalian-Aminobutyric AcidB Receptors : Structure and Function
. . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 247
More about hypervirulent avian influenza: Is the world now better prepared?
The World Health Organization (WHO) no longer regards the Spanish flu pandemic as a worst case scenario as the basis for contingency planning, as to how to meet a possible pandemic with hypervirulentExpand
More about hypervirulent avian influenza: Is the world now better prepared?
The World Health Organization (WHO) no longer regards the Spanish flu pandemic as a worst case scenario as the basis for contingency planning, as to how to meet a possible pandemic with hypervirulentExpand


Effect of homotaurine in experimental analgesia tests.
From the above results the implication of peripheral and spinal mechanisms in the antinociceptive effect of homotaurine may be concluded. Expand
Antinociception induced by systemic administration of local anaesthetics depends on a central cholinergic mechanism
A facilitation of cholinergic transmission by the local anaesthetics is postulated; this could be due to blockade of presynaptic muscarinic receptors. Expand
Comparison of the antinociceptive effect of gamma-aminobutyric acid (GABA) agonists: evidence for a cholinergic involvement.
Findings suggest that, regardless of their mechanism, the three types of GABA agonists tested are capable of inducing an antinociceptive response in mice and that this action is apparently secondary to a GABA-mediated increase in brain cholinergic function. Expand
Gabaergic mechanisms in antinociception
  • J. Sawynok
  • Chemistry, Medicine
  • Progress in Neuro-Psychopharmacology and Biological Psychiatry
  • 1984
An understanding of the role of GABAA and GABAB receptors in antinociception will require clarification of some curious pharmacological actions of bicuculline and the use of a specific GABAB receptor antagonist. Expand
A comparison of the antinociceptive responses to the GABA-receptor agonists THIP and baclofen
The results suggest that while the analgesic response to THIP and baclofen is partially mediated by a common system, the two agents act by independent mechanisms as well. Expand
Pertussis toxin inhibits antinociception produced by intrathecal injection of morphine, noradrenaline and baclofen.
The sensitivity of spinal antinociception to pertussis toxin suggests involvement of a guanine nucleotide regulatory protein in spinal actions of morphine, noradrenaline and L-baclofen and there is support in the literature for the additional involvement of adenylate cyclase in the action of morphine and norad Renaline but not of bacl ofen. Expand
GABA-induced hypothermia in rats: involvement of serotonergic and cholinergic mechanisms.
The results support the hypothesis that the hypothermia induced by GABA is modulated by nicotinic receptors and indicate that it may be mediated by serotonin and acetylcholine release. Expand
D-Baclofen is an antagonist at baclofen receptors mediating antinociception in the spinal cord.
Antinociception produced by intrathecal administration of Baclofen appears to result from activation of a receptor which is stereoselective for the L-isomer and can be blocked by D-baclofen in doses which have initial agonist activity. Expand
GABA uptake inhibitors produce a greater antinociceptive response in the mouse tail-immersion assay than other types of GABAergic drugs.
In vitro uptake experiments revealed that the SKF compounds selectively inhibit GABA transport, having no effect on the accumulation of aspartic acid, glutamic acid, beta-alanine or glycine, and data suggest that uptake inhibitors may be facilitating GABA transmission in a system that is less affected by other types of GABAergic compounds. Expand
Baclofen activates two distinct receptors in the rat spinal cord and guinea pig ileum
Receptors with which baclofen interacts in the spinal cord to produce antinociception differ from GABAB receptors with respect to the rank order of potency of antagonists as well as close structural analogs, and these criteria could be used for characterization of such receptors. Expand