Synthesis and pharmacologic properties of 6-succinylcodeine.

In our search for a ligand to be used for affinity chromatography in the separation of putative, codeine-specific receptors, we have synthesized a pharmacologically active codeine derivative, 6-succinylcodeine (Ib). The structure of the compound has been confirmed. It is markedly less toxic than the parent compound, codeine (Ia), and has significantly weaker antitussive properties in the cat.

Induction of experimental myasthenia gravis in rhesus monkeys: a model for the study of the human disease.

Experimental autoimmune myasthenia gravis (EAMG) was induced in rhesus monkeys using purified acetylcholine receptor (AChR) from Torpedo california. A single dose of 80 micrograms induced antibody formation two weeks after injection. Two subsequent doses at two-week intervals caused clinical signs (anorexia, fatigability, weight loss, ptosis and dysphagia) which initially responded to treatment with neostigmine.

Binding of [3H]phenycyclidine to rat and human blood constituents.

The binding of [3H]phencyclidine (PCP) to rat serum and human plasma was studied using equilibrium dialysis. [3H]PCP bound with a relatively low affinity to both rat serum (KD = 1.5 X 10(-5) M) and human plasma (KD = 6.

Induction of allergic neuritis in rhesus monkeys.

Experimental allergic neuritis (EAN) was induced in rhesus monkey (Macaca mulatta) following sensitization with rabbit nerve (PNS) myelin in complete Freund's adjuvant (CFA) or with bovine P2 protein complexed with phosphatidyl serine (P2-lipid) in CFA. The response of monkeys receiving PNS myelin in CFA differed from the previous studies where monkeys developed clinical signs of fatal EAN within 15-20 days following sensitization. The monkeys in this study (6) showed a much longer delay (40-114 days) before the appearance of severe clinical signs, and 4 of the 6 animals survived without further attack (1 year).

Cardiolipins are 'in vitro' inhibitors of rat brain (Na+ + K+)-dependent ATPases. A probable mechanism of action.

Cardiolipins were found to potentiate the 'in vitro' inhibitory activity of (-)-delta 9-tetrahydrocannabinol on (Na+ + K+)-dependent rat brain ATPases. The compounds were found to be powerful inhibitors by themselves. At optimal concentrations of cations (Na+, K+, Mg2+), the compounds were found to be noncompetitive inhibitors of ATP (Ki = 3.