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Comparison of the mGluR1 Antagonist A-841720 in Rat Models of Pain and Cognition

Comparison of the mGluR1 Antagonist A-841720 in Rat Models of Pain and Cognition

Lorenzo Morè, Andreas Gravius, Malgorzata Pietraszek, Irina Belozertseva, Andrey Malyshkin, Elena Shekunova, Caroline Barberi, Daniela Schaefer, Werner J Schmidt, Wojciech Danysz

Behav Pharmacol. 2007 Jul;18(4):273-81.

PMID: 17551319

Abstract:

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. This diminishes its therapeutic potential for the treatment of chronic pain.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP869802584	A-841720		869802-58-4	Price

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