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Pharmacology of acid-sensing ion channels - Physiological and therapeutical perspectives.
This article is part of a Special Issue entitled 'ASIC Channels'. PMID: 25613302 [PubMed - as supplied by publisher]
Source: Neuropharmacology - January 19, 2015 Category: Drugs & Pharmacology Authors: Baron A, Lingueglia E Tags: Neuropharmacology Source Type: research

Convergent Phosphomodulation of the Major Neuronal Dendritic Potassium Channel Kv4.2 by Pituitary Adenylate Cyclase-activating Polypeptide.
Abstract The endogenous neuropeptide pituitary adenylate cyclase-activating polypeptide (PACAP) is secreted by both neuronal and non-neuronal cells in the brain and spinal cord, in response to pathological conditions such as stroke, seizures, chronic inflammatory and neuropathic pain. PACAP has been shown to exert various neuromodulatory and neuroprotective effects. However, direct influence of PACAP on the function of intrinsically excitable ion channels that are critical to both hyperexcitation as well as cell death, remain largely unexplored. The major dendritic K(+) channel Kv4.2 is a critical regulator of neu...
Source: Neuropharmacology - October 8, 2015 Category: Drugs & Pharmacology Authors: Gupte RP, Kadunganattil S, Shepherd AJ, Merrill R, Planer W, Bruchas MR, Strack S, Mohapatra DP Tags: Neuropharmacology Source Type: research

Allosteric modulation of the cannabinoid 2 receptor confers seizure resistance in mice.
Abstract Mounting evidence suggests that modulation of cannabinoid 2 receptors (CB2Rs) is therapeutic in mouse models of neurological disorders, including neuropathic pain, neurodegenerative disease, and stroke. We previously showed that reducing CB2R activity increases seizure susceptibility in mice. In the present study, we evaluated the therapeutic potential of the CB2R positive allosteric modulator, Ec21a, against induced seizures in mice. The pharmacokinetic profile of Ec21 demonstrated a similar distribution in brain and plasma, with detection up to 12 hours following injection. Ec21a increased resistance to...
Source: Neuropharmacology - January 12, 2021 Category: Drugs & Pharmacology Authors: Shapiro L, Gado F, Manera C, Escayg A Tags: Neuropharmacology Source Type: research

New paradigms in purinergic receptor ligand discovery
Neuropharmacology. 2023 Mar 13:109503. doi: 10.1016/j.neuropharm.2023.109503. Online ahead of print.ABSTRACTThe discovery and clinical implementation of modulators of adenosine, P2Y and P2X receptors have progressed dramatically in ∼50 years since Burnstock's definition of purinergic signaling. Although most clinical trials of selective ligands (agonists and antagonists) of these nineteen receptors failed, there is a renewed impetus to redirect efforts to new disease conditions and the discovery of more selective or targeted compounds with potentially reduced side effects, such as biased GPCR agonists. The elucidation of...
Source: Neuropharmacology - March 15, 2023 Category: Drugs & Pharmacology Authors: Kenneth A Jacobson Balaram Pradhan Zhiwei Wen Asmita Pramanik Source Type: research