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Radioligand Binding Properties and Pharmacological Characterization of 6-Amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-a]benzimidazole-2-carboxamide (YM-298198), a High-Affinity, Selective, and…
TLDR
YM-298198 is a newly synthesized, high-affinity, selective, and noncompetitive antagonist of mGluR1 that will be a useful pharmacological tool due to its highly active properties in vitro and in vivo.
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Neuroprotective effects of the selective type 1 metabotropic glutamate receptor antagonist YM-202074 in rat stroke models
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Antinociceptive profile of a selective metabotropic glutamate receptor 1 antagonist YM-230888 in chronic pain rodent models.
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AS1069562, the (+)-Isomer of Indeloxazine, Exerts Analgesic Effects in a Rat Model of Neuropathic Pain with Unique Characteristics in Spinal Monoamine Turnover
TLDR
Assessment of the analgesic effects of AS1069562 in a rat model of chronic constriction injury (CCI)–induced neuropathic pain and the spinal monoamine turnover suggests that it may have potential as a treatment option for patients with neuropathy pain, with a different profile from currently available antidepressants.
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Optical isomerization of R(−)‐clidanac to the biologically active S(+)‐isomer in guinea‐pigs
Optical isomerization of clidanac (RS‐6‐chloro‐5‐cyclohexyl‐1‐indancarboxylic acid, I), an anti‐inflammatory drug having a chiral centre in its molecule, was evaluated in guinea‐pigs. After oral…
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Inhibition of prostaglandin biosynthesis by clidanac and related compounds: structural and conformational requirements for PG synthetase inhibition
TLDR
Structural‐activity studies with clidanac analogues showed that the position of halogen substitution in 1‐indancarboxylic acid is of considerable significance for the conformational requirement for binding to the enzyme.
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Minodronic acid, a third-generation bisphosphonate, antagonizes purinergic P2X(2/3) receptor function and exerts an analgesic effect in pain models.
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Relationship between serotonin transporter occupancies and analgesic effects of AS1069562, the (+)-isomer of indeloxazine, and duloxetine in reserpine-induced myalgia rats
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Correlation between pharmacological and opiate receptor binding activities of tetrapeptide acylhydrazide analogs of enkephalin.
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AS1069562, the (+)-isomer of indeloxazine, but not duloxetine has a curative-like analgesic effect in a rat model of streptozotocin-induced diabetic neuropathy
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