ArticleMolecular pain2008
Sumatriptan inhibits synaptic transmission in the rat midbrain periaqueductal grey.
Article in Molecular pain, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 45 citations in OpenAlex.
- Gamma-aminobutyric acid and glutamate/glutamine levels in the dentate nucleus and periaqueductal gray in new daily persistent headache: a magnetic resonance spectroscopy study.The journal of headache and pain · 2024Article
- Sex-specific modulation of the medial prefrontal cortex by glutamatergic median raphe neurons.Science advances · 2023Article
- Multi-omic analyses of triptan-treated migraine attacks gives insight into molecular mechanisms.Scientific reports · 2023Article
- The Roles of Serotonin in Neuropsychiatric Disorders.Cellular and molecular neurobiology · 2022Review
- Parenchymal neuroinflammatory signaling and dural neurogenic inflammation in migraine.The journal of headache and pain · 2021Review
- Sex hormones regulate NHE1 functional expression and brain endothelial proteome to control paracellular integrity of the blood endothelial barrier.Brain research · 2021Article
- International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function.Pharmacological reviews · 2021Review
- Eslicarbazepine acetate interacts in a beneficial manner with standard and alternative analgesics to reduce trigeminal nociception.Psychopharmacology · 2020Article
- Phytomedicines in the Treatment of Migraine.CNS drugs · 2019Review
- The Role of Descending Pain Modulation in Chronic Primary Pain: Potential Application of Drugs Targeting Serotonergic System.Neural plasticity · 2019Review
- Targeted 5-HTNeurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2018Review
- Characterization of serotonin-induced inhibition of excitatory synaptic transmission in the anterior cingulate cortex.Molecular brain · 2017Article
- Endocannabinoids in the brainstem modulate dural trigeminovascular nociceptive traffic via CB1 and "triptan" receptors: implications in migraine.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2013Article
- Pronociceptive effect of 5-HT(1A) receptor agonist on visceral pain involves spinal N-methyl-D-aspartate (NMDA) receptor.Neuroscience · 2012Article
- 5-HT(1B) receptors inhibit glutamate release from primary afferent terminals in rat medullary dorsal horn neurons.British journal of pharmacology · 2012Article
- Abdominal migraine reviewed from both central and peripheral aspects.World journal of experimental medicine · 2012Review
- Where does a migraine attack originate? In the brainstem.Journal of neural transmission (Vienna, Austria : 1996) · 2012Review
- Role of 5-HT(1) receptor subtypes in the modulation of pain and synaptic transmission in rat spinal superficial dorsal horn.British journal of pharmacology · 2012Article
- Serotonergic agents in the management of cluster headache.Current pain and headache reports · 2011Review
- Migraine is a neuronal disease.Journal of neural transmission (Vienna, Austria : 1996) · 2011Review
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundThere is evidence to suggest that the midbrain periaqueductal grey (PAG) has a role in migraine and the actions of the anti-migraine drug sumatriptan. In the present study we examined the serotonergic modulation of GABAergic and glutamatergic synaptic transmission in rat midbrain PAG slices in vitro.
resultsSerotonin (5-hydroxytriptamine, 5-HT, IC50 = 142 nM) and the selective serotonin reuptake inhibitor fluoxetine (30 microM) produced a reduction in the amplitude of GABAA-mediated evoked inhibitory postsynaptic currents (IPSCs) in all PAG neurons which was associated with an increase in the paired-pulse ratio of evoked IPSCs. Real time PCR revealed that 5-HT1A, 5-HT1B, 5-HT1D and 5-HT1F receptor mRNA was present in the PAG. The 5-HT1A, 5-HT1B and 5-HT1D receptor agonists 8-OH-DPAT (3 microM), CP93129 (3 microM) and L694247 (3 microM), but not the 5-HT1F receptor agonist LY344864 (1 - 3 microM) inhibited evoked IPSCs. The 5-HT (1 microM) induced inhibition of evoked IPSCs was abolished by the 5-HT1B antagonist NAS181 (10 microM), but not by the 5-HT1A and 5-HT1D antagonists WAY100135 (3 microM) and BRL15572 (10 microM). Sumatriptan also inhibited evoked IPSCs with an IC50 of 261 nM, and reduced the rate, but not the amplitude of spontaneous miniature IPSCs. The sumatriptan (1 microM) induced inhibition of evoked IPSCs was abolished by NAS181 (10 microM) and BRL15572 (10 microM), together, but not separately. 5-HT (10 microM) and sumatriptan (3 microM) also reduced the amplitude of non-NMDA mediated evoked excitatory postsynaptic currents (EPSCs) in all PAG neurons tested.
conclusionThese results indicate that sumatriptan inhibits GABAergic and glutamatergic synaptic transmission within the PAG via a 5-HT1B/D receptor mediated reduction in the probability of neurotransmitter release from nerve terminals. These actions overlap those of other analgesics, such as opioids, and provide a mechanism by which centrally acting 5-HT1B and 5-HT1D ligands might lead to novel anti-migraine pharmacotherapies.
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