DBO-83

DBO-83 is an agonist of nicotinic acetylcholine receptors (nAChRs) with antinociceptive and anti-amnesic activities.^1,2,3 It binds to nAChRs in rat cortical membranes with a K_i value of 4.1 nM in a radioligand binding assay with the α4β2 nAChR partial agonist and α7 nAChR agonist [³H]cytisine.¹ DBO-83 dose-dependently increases the latency to paw licking in mice in the hot plate test and reduces the number of abdominal constrictions in mice in the acetic acid abdominal constriction test, effects that can be reduced by the nAChR antagonist mecamylamine (Item No. 14602).² DBO-83 also dose-dependently prevents amnesia induced by mecamylamine, the muscarinic receptor antagonist scopolamine, and the nAChR antagonist dihydro-β-erythroidine in mice in the passive avoidance test.³

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1. Barlocco, D., Cignarella, G., Tondi, D., et al. Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: Synthesis, activity, and modeling. J. Med. Chem. 41(5), 674-681 (1998).

2. Ghelardini, C., Galeotti, N., Barlocco, D., et al. Antinociceptive profile of the new nicotinic agonist DBO-83. Drug Dev. Res. 40(3), 251-258 (1997).

3. Ghelardini, C., Galeotti, N., Giuliani, F., et al. Antiamnesic activity of the nicotinic agonist DBO-83 in mice. Drug Dev. Res. 45(2), 45-51 (1998).