Effects of Benzoctamine and Chlordiazepoxide on Turnover and Uptake of 5‐hydroxytryptamine in the Brain

Abstract

Benzoctamine, a new psychoactive drug, known to exert in man an anti‐anxiety effect resembling that of chlordiazepoxide, decreased the disappearance of intraventricularly‐injected [14C]‐5‐hydroxytryptamine (5‐HT) from rat brain, as did chlordiazepoxide. Both drugs partially inhibited the α‐ethyl‐3‐hydroxy‐4‐methylphenylethylamine‐induced depletion of rat brain 5‐HT. It is concluded that benzoctamine, like chlordiazepoxide, decreases 5‐HT turnover in the brain and that this action may play a role in the anti‐anxiety effect of these drugs observed in man.

General Pharmacology and Neuropharmacology of Benzodiazepine Derivatives

“…(1970) reported that diazepam markedly retarded the decline of 14C-5-HT and 14C-5-HIAA in the rat brain; in addition the efflux of intracisternally injected 14C-5-HIAA was retarded. Very similar results were obtained by LIPPMANN and PUGSLEY (1974) and PUGSLEY and LIPPMANN (1975 with 20 mg' kg-I chlordiazepoxide i.p. STEIN et ai.…”

“…a-Ethyl-3-hydroxy-4-methylphenethylamine (H 75/ 12) is an amine which is selectively taken up into 5-HT neurons and displaces 5-HT. Neither diazepam nor the thienodiazepine, Y-7131, prevented the 5-HT depletion induced by H 75/12 (LIPPMANN and PUGSLEY, 1974).…”

Asymmetric [4+2]‐Cycloaddition of Anthracene Derivatives via Hydrazone Activation

“…Anthracene and its derivatives constitute an important class of molecules belonging to the family of a polycyclic aromatic compounds, which are widely used in organic synthesis, biological research and in the production of dyes or other materials with interesting photochemical and photophysical properties [1–3] . Notably, the carbocyclic scaffold of anthracene cycloadducts is present in bioactive molecules, especially with antidepressant activity with maprotiline, [4] benzoctamine [4b–5] and oxaprotiline [6] being representative examples of tricyclic antidepressants (TCAs, Figure 1).…”

Catalytic asymmetric [4 + 2] dearomative photocycloadditions of anthracene and its derivatives with alkenylazaarenes

“…Among the established [4 + 2] cycloaddition reactions, anthracene derivatives are of particular synthetic interest owing to the convenient availability of these feedstocks and the attractive bioactivities of the resulting cycloadducts (e.g., molecules I-IV, Fig. 1B) [60][61][62][63] . In order to break the inherent aromatic stability of anthracene, activated functional groups are typically required to assemble on the anthracene ring (Fig.…”