RB 101

RB 101 is an active mixed inhibitor against two enzymes which metabolize the enkephalins neutral endopeptidase and aminopeptidase N. RB 101 has rather long-lasting antinociceptive effects. RB 101 inhibits the in vivo [3H]DPN binding both under basal conditions and after swim stress in mice. RB 101 can be used to determine the precise in vivo localization of enkephalinergic pathways recruited by various stimuli[1][2].

[1] Baamonde A, et al. Antidepressant-type effects of endogenous enkephalins protected by systemic RB 101 are mediated by opioid delta and dopamine D1 receptor stimulation. Eur J Pharmacol. 1992 Jun 5;216(2):157-66. DOI:10.1016/0014-2999(92)90356-9
[2] Ruiz-Gayo M, et al. In vivo occupation of mouse brain opioid receptors by endogenous enkephalins: blockade of enkephalin degrading enzymes by RB 101 inhibits [3H]diprenorphine binding. Brain Res. 1992 Feb 7;571(2):306-12. DOI:10.1016/0006-8993(92)90669-z