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The brain-penetrant 5-HT7 receptor agonist LP-211 reduces the sensory and affective components of neuropathic pain.
Santello, Mirko; Bisco, Alberto; Nevian, Natalie Elisabeth; Lacivita, Enza; Leopoldo, Marcello; Nevian, Thomas.
Afiliación
  • Santello M; Department of Physiology, University of Bern, Bühlplatz 5, 3012 Bern, Switzerland; Institute of Pharmacology and Toxicology, University of Zürich, Winterthurerstrasse 190, 8057 Zürich, Switzerland; Neuroscience Center Zurich, University of Zurich and ETH Zurich, 8057 Zurich, Switzerland. Electronic
  • Bisco A; Department of Physiology, University of Bern, Bühlplatz 5, 3012 Bern, Switzerland.
  • Nevian NE; Department of Physiology, University of Bern, Bühlplatz 5, 3012 Bern, Switzerland.
  • Lacivita E; Department of Pharmacy - Drug Science, University of Bari Aldo Moro, Via Orabona 4, 70125 Bari, Italy.
  • Leopoldo M; Department of Pharmacy - Drug Science, University of Bari Aldo Moro, Via Orabona 4, 70125 Bari, Italy.
  • Nevian T; Department of Physiology, University of Bern, Bühlplatz 5, 3012 Bern, Switzerland; Center for Cognition, Learning and Memory, University of Bern, Bern, Switzerland. Electronic address: nevian@pyl.unibe.ch.
Neurobiol Dis ; 106: 214-221, 2017 Oct.
Article en En | MEDLINE | ID: mdl-28690143
Neuropathic pain is a debilitating pathological condition of high clinical relevance. Changes in neuronal excitability in the anterior cingulate cortex (ACC) play a central role in the negative emotional and affective aspects of chronic pain. We evaluated the effects of LP-211, a new serotonin-receptor-type-7 (5-HT7R) agonist that crosses the blood-brain barrier, on ACC neurons in a mouse model of neuropathic pain. LP-211 reduced synaptic integration in layer 5 pyramidal neurons, which was enhanced in neuropathic pain due to a dysfunction of dendritic hyperpolarization-activated-and-cyclic-nucleotide-regulated (HCN) channels. Acute injection of LP-211 had an analgesic effect, increasing the mechanical withdrawal threshold in neuropathic animals, which was partially mediated by an action in the ACC. Additionally, the acute application of LP-211 blocked the switch in the place escape/avoidance behavior induced by noxious stimuli. Thus systemic treatment with a 5-HT7R agonist leads to modulation of the ACC, which dampens sensory and affective aspects of chronic pain.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piperazinas / Agonistas de Receptores de Serotonina / Analgésicos no Narcóticos / Afecto / Neuralgia Límite: Animals Idioma: En Revista: Neurobiol Dis Asunto de la revista: NEUROLOGIA Año: 2017 Tipo del documento: Article Pais de publicación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piperazinas / Agonistas de Receptores de Serotonina / Analgésicos no Narcóticos / Afecto / Neuralgia Límite: Animals Idioma: En Revista: Neurobiol Dis Asunto de la revista: NEUROLOGIA Año: 2017 Tipo del documento: Article Pais de publicación: Estados Unidos