Centrally acting emetics. II. Norapomorphine and derivatives

Conversion of Apocodeine to Apomorphine and Norapomorphine in Rats

“…and IV [prepared according to the literature procedure (9)] yielded blue-green-colored spots, presumably due to formation of ortho-quinone-type oxidation products (12). Quantitation of I and IV was by TLC fluorescence quenching (13).…”

“…TLC examination of extracts of hydrolyzed urine4 obtained from animals injected with 11-HC1 revealed the presence of I and IV (Table I). This suggestion is somewhat contradicted by the apparent low order of activity of IV causing compulsive gnawing in mice (9). Quantitative evaluation of these results gave the data indicated in Table 11.…”

Screening Nornuciferine Derivatives for Apomorphine-Like Activity

“…A substantial number of apomorphine analogs and derivatives were examined in an attempt to define the chemorphological requisites for biological activity, notably activity relating to emesis and behavioral stereotypy (1)(2)(3). In a continuing study of apomorphine derivatives having "potential" emetic activity, Vavrek et al (4) prepared a series of I,2-dimethoxylated noraporphines (nornuciferines) for biological evaluation.…”

“…The method for assessing emetic activity was described previously (2) and involves comparison of the threshold emetic dose of a compound with the threshold emetic dose of apomorphine reference standard in the same animals. Compounds that do not provoke emesis in doses 100 times the apomorphine threshold emetic dose are judged to be inactive.…”

“…(2) stated that free films only provide a model for evaluating gross properties of applied films, with limited information in other areas, while Banker et al. (2) stated that free films only provide a model for evaluating gross properties of applied films, with limited information in other areas, while Banker et al.…”