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2-Sdbstituted Cyclopropylamines. II 1265 20 hr. The mixture was cooled and filtered and the filtrate was concentrated in vacuo.The residue was refluxed with 50 ml. of acetic anhydride for 1 hr., the solution was concentrated in vacuo and the residue dissolved in water. After extraction with ether, the solution was made alkaline and the mixture was extracted with ether. The ether extracts were dried and concentrated to give a colorless liquid, b.p. 75-83°( 0.3 mm.), which was converted to a hydrochloride.

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A series of piperidylidene derivatives of thioxanthenes, xanthenes, dibenzoxepins, and acridans was prepared and examined for neuropharmacological activity. Several of these compounds having an appropriate substituent, e.g., CF3, C1, SMe, in the 2 position of the tricyclic nucleus were potent neuroleptic agents. For example, in a ptosis production test in rats l-methyl-4-(2-trifluoromethylthioxanthen-9-ylidene)piperidine (11) and its 10-methylacridan congener 17 were seven to eight times more potent than chlorpromazine. In the same test the N-cyclobutylmethyl analog (26) of 11 was the most effective member of the series; it was about 18 times more potent than chlorpromazine. In the piperidylidene derivatives of tricyclic compounds, for which neuroleptic activity has not been reported previously, the spatial relationship between the basic nitrogen and the tricyclic nucleus is more restricted than in their antipsychotic aminopropyl-and aminopropylidene-substituted relatives. Some consequences of this observation on the conformational requirements for potent neuroleptic activity of tricyclic compounds are considered.Cyproheptadine (la), a clinically useful antipruritic

Monoamine oxidase inhibitors markedly enhance the oral pressor potency of tyramine by preventing it from being destroyed by the monoamine oxidase normally present in liver and intestine. Since certain types of cheese contain high concentrations of tyramine, they should not be eaten by patients during treatment with a monoamine oxidase inhibitor.