24 research outputs found

    Comparison of the novel subtype-selective GABAA receptorpositive allosteric modulator NS11394 [3’-[5-(1-hydroxy-1-methyl-ethyl)- benzoimidazol-1-yl]-biphenyl-2-carbonitrile] with diazepam, zolpidem

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    ABSTRACT Spinal administration of GABA A receptor modulators, such as the benzodiazepine drug diazepam, partially alleviates neuropathic hypersensitivity that manifests as spontaneous pain, allodynia, and hyperalgesia. However, benzodiazepines are hindered by sedative impairments and other side effect issues occurring mainly as a consequence of binding to GABA A receptors containing the ␣ 1 subunit. Here, we report on the novel subtype-selective GABA A receptor-positive modulator NS11394 [3Ј-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile], which possesses a functional efficacy selectivity profile of ␣ 5 Ͼ ␣ 3 Ͼ ␣ 2 Ͼ ␣ 1 at GABA A ␣ subunit-containing receptors

    P2Y receptors and pain transmission

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    It is widely accepted that the most important ATP receptors involved in pain transmission belong to the P2X3 and P2X2/3 subtypes, selectively expressed in small diameter dorsal root ganglion (DRG) neurons. However, several types of the metabotropic ATP (P2Y) receptors have also been found in primary afferent neurons; P2Y1 and P2Y2 receptors are typically expressed in small, nociceptive cells. Here we review the results available on the involvement of P2Y receptors in the modulation of pain transmission
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