A 841720 - CAS 869802-58-4
Category: Inhibitor
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A 841720 is a potent non-competitive mGlu1 receptor antagonist (IC50 = 10 nM) exhibiting 34-fold selectivity over mGluR5 and inactive to other mGluR receptors, neurotransmitter receptors, ion channels, and transporters. It inhibits complete Freund's adjuvant-induced inflammatory pain (ED50 = 23 µmol/kg) and decreases mechanical allodynia (ED50 = 28 µmol/kg) in mouse models.
Brife Description:
mGlu1 receptor antagonist
A-841720; 3-(azepan-1-yl)-9-(dimethylamino)pyrido[1,2]thieno[3,4-d]pyrimidin-4-one
Canonical SMILES:
1.Analgesic activity of metabotropic glutamate receptor 1 antagonists on spontaneous post-operative pain in rats.
Zhu CZ;Baker S;EI-Kouhen O;Lehto SG;Hollingsworth PR;Gauvin DM;Hernandez G;Zheng G;Chang R;Moreland RB;Stewart AO;Brioni JD;Honore P Eur J Pharmacol. 2008 Feb 12;580(3):314-21. Epub 2007 Nov 13.
Activation of metabotropic glutamate (mGlu) receptors has previously been shown to play a role in inflammatory or neuropathic pain states. However, the role of mGlu type 1 receptors in post-operative pain remains to be investigated. In the present study, effects of potent and selective mGlu1 receptor antagonists A-841720, A-794282, A-794278, and A-850002 were evaluated in a skin incision-induced post-operative pain model in rats. Post-operative pain was examined 2 h following surgery using weight-bearing difference between injured and uninjured paws as a measure of spontaneous pain. In this model, A-841720, A-794282, A-794278, and A-850002 induced significant attenuation of spontaneous post-operative pain behavior, with ED50s of 10, 50, 50, and 65 micromol/kg i.p., respectively. Depending on the compound, significant motor side effects were also observed at 3 to 10 fold higher doses. These results support the notion that mGlu1 receptor activation plays a significant role in nociceptive transmission in post-operative pain, though motor impairment may be a limiting factor in developing mGlu1 receptor antagonists as novel analgesics.
2.Comparison of the mGluR1 antagonist A-841720 in rat models of pain and cognition.
Morè L;Gravius A;Pietraszek M;Belozertseva I;Malyshkin A;Shekunova E;Barberi C;Schaefer D;Schmidt WJ;Danysz W Behav Pharmacol. 2007 Jul;18(4):273-81.
In the current study we compared the potency of the selective metabotropic glutamate receptor (mGluR1) antagonist A-841720 (7-Azepan-1-yl-4-dimethylamino-7H-9-thia-1,5,7-triaza-fluoren-8-one) in rodent models of pain with its effects in models of learning and memory, to obtain information regarding the therapeutic window of this compound. A-841720 significantly reduced formalin-induced behaviours and complete Freund's adjuvant (CFA)-induced tactile allodynia, starting at doses of 1 and 10 mg/kg, respectively. At the dose of 3 mg/kg, however, A-841720 significantly reduced the percentage of spontaneous alternations in a radial-maze task. In contextual-fear conditioning, A-841720, given at the dose of 10 mg/kg before acquisition, significantly reduced freezing behaviour tested 24 h later. In the same task, repeated treatment for 5 days did not reduce the impairing effect of the challenge dose, indicating a lack of tolerance development. In a passive-avoidance task, A-841720 at 10 mg/kg administered before acquisition, significantly reduced the latency to enter the dark box on the retention test. Given that complete Freund's adjuvant is a better measure of analgesia, these results indicate that the selective mGluR1 antagonist A-841720 has analgesic potential in a dose range at which it also produces memory impairments.
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