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Recent Advances in the Development of T ‐type Calcium Channel Blockers for Pain Intervention
Abstract Cav3.2 T‐type calcium channels are important regulators of pain signals in afferent pain pathway, and their activities are dysregulated during various chronic pain states. Therefore it stands to reason that inhibiting T‐type calcium channels in dorsal root ganglion neurons and in the spinal dorsal horn can be targeted for pain relief. This is supported by early pharmacological studies with T‐type channel blockers such as ethosuximide, and by analgesic effects of siRNA depletion of Cav3.2 channels. In the past five years, considerable effort has been applied towards identifying novel classes of T‐type calci...
Source: British Journal of Pharmacology - June 13, 2017 Category: Drugs & Pharmacology Authors: Terrance P Snutch, Gerald W Zamponi Tags: REVIEW ARTICLE THEMED ISSUE Source Type: research

G protein‐gated inwardly rectifying potassium (KIR3) channels play a primary role in the antinociceptive effect of oxycodone, but not morphine, at supraspinal sites
Conclusion and ImplicationsThese results demonstrate that KIR3.1 channels play a primary role in the antinociceptive effects of oxycodone, but not those of morphine, at supraspinal sites and suggest that supraspinal KIR3.1 channels are responsible for the unique analgesic profile of oxycodone.
Source: British Journal of Pharmacology - December 10, 2013 Category: Drugs & Pharmacology Authors: Atsushi Nakamura, Masahide Fujita, Hiroko Ono, Yoshie Hongo, Tomoe Kanbara, Koichi Ogawa, Yasuhide Morioka, Atsushi Nishiyori, Masahiro Shibasaki, Tomohisa Mori, Tsutomu Suzuki, Gaku Sakaguchi, Akira Kato, Minoru Hasegawa Tags: RESEARCH PAPER Source Type: research

Heterologous Regulation of Agonist‐Independent μ‐Opioid Receptor Phosphorylation by Protein Kinase C
Conclusions & ImplicationsThe present results unravel novel mechanisms of heterologous regulation of MOR phosphorylation by PKC. These findings represent a useful starting point for definitive experiments elucidating the exact contribution of PKC‐driven MOR phosphorylation to diminished MOR responsiveness in morphine tolerance and pathological pain.
Source: British Journal of Pharmacology - December 6, 2013 Category: Drugs & Pharmacology Authors: Susann Illing, Anika Mann, Stefan Schulz Tags: Research Paper Source Type: research

G protein‐gated inwardly rectifying potassium (GIRK) channels play a primary role in the antinociceptive effect of oxycodone, but not morphine, at supraspinal sites
Conclusion and ImplicationsThe results demonstrated that GIRK1 channels play a primary role in the antinociceptive effects of oxycodone, but not morphine, at supraspinal sites, and suggested that supraspinal GIRK1 channels are responsible for the unique analgesic profile of oxycodone.
Source: British Journal of Pharmacology - October 7, 2013 Category: Drugs & Pharmacology Authors: Atsushi Nakamura, Masahide Fujita, Hiroko Ono, Yoshie Hongo, Tomoe Kanbara, Koichi Ogawa, Yasuhide Morioka, Atsushi Nishiyori, Masahiro Shibasaki, Tomohisa Mori, Tsutomu Suzuki, Gaku Sakaguchi, Akira Kato, Minoru Hasegawa Tags: Research Paper Source Type: research