Swift's father

Use of site-directed mutagenesis to identify valine-573 in the S'1 binding site of rat neutral endopeptidase 24.11 (enkephalinase)

“…In 1980, Roques and co-workers (Roques et al, 1980) showed antinociceptive activity in mice by the NEP inhibitor thiorphan. This observation has been followed by a number of reports on the development and analgesic effects of NEP inhibitors (Carenzi et al, 1983;Schwartz et al, 1985;Ehrenpreis, 1985;Roques et al, 1986;Chipkin, 1986;Rupreht et al, 1983;Dickenson, 1986; Hersh, 1986; Bateman & Hersh, 1987). The mode of action of these compounds is presumably to inhibit inactivation of synaptically released enkephalins by NEP, thereby prolonging the analgesic effect of these opioid peptides.…”