Topic
Benzoctamine
About: Benzoctamine is a research topic. Over the lifetime, 32 publications have been published within this topic receiving 593 citations. The topic is also known as: N-Methyl-9,10-ethanoanthracene-9(10H)-methanamine & Benzoctamine.
Papers
TL;DR: Blood pressure reduction more closely paralleled the in vitro and in vivo potency of these agents toward vascular alpha rather than 5HT2 receptors.
Abstract: In vitro affinity for vascular 5HT2 and alpha receptors was determined for several compounds (spiperone, ketanserin, mianserin, trazodone, mepiprazole, benzoctamine, m-trifluoro-methylphenylpiperazine, m-chlorophenylpiperazine, and 1-(1-naphthyl)piperazine) known to interact with serotonin receptors. All compounds competitively inhibited 5HT2 and alpha receptors with differing degrees of selectively. Based on these observations, ketanserin, benzoctamine, and 1(1-naphthyl)piperazine were evaluated as antihypertensive agents in spontaneously hypertensive rats (SHR). Of these compounds, 1-(1-naphthyl)piperazine was a highly selective 5HT2 receptor antagonist with a ratio of 5HT2 to alpha receptor affinity of greater than 2000. The ratio of 5HT2 to alpha receptor affinity for ketanserin and benzoctamine was 63 and 16, respectively. However, the order of affinity toward 5HT2 receptors was ketanserin greater than 1-(1-naphthyl)piperazine greater than benzoctamine whereas the order of affinity toward alpha receptors was ketanserin greater than benzoctamine greater than 1-(1-naphthyl)piperazine. A similar order of potency toward both 5HT2 and alpha receptors was found in pithed SHR based on antagonism of the pressor response to serotonin and methoxamine, respectively. In the SHR, maximum blood pressure reduction at a dose of 10 mg/kg i.p. was approximately 65 and 30 mm Hg for ketanserin and benzoctamine, respectively; 1-(1-naphthyl)piperazine did not affect blood pressure. Thus, blood pressure reduction more closely paralleled the in vitro and in vivo potency of these agents toward vascular alpha rather than 5HT2 receptors.(ABSTRACT TRUNCATED AT 250 WORDS)
71 citations
TL;DR: It is suggested that interactions with benzodiazepine receptors may account for the anxiolytic and anticonvulsive side effects of this drug.
Abstract: The interaction of several non-benzodia-zepine drugs with [3H] diazepam binding to benzodiazepine receptors in rat brain synaptosomal membranes was investigated. Baclofen, benzoctamine, hydroxyzine, chlorpromazin, haloperidol, imipramine, and amitriptyline displace specific [3H] diazepam binding, but the concentrations needed are too high to explain pharmacological effects of these drugs by an interaction with benzodiazepine receptors. The most potent non-benzodiazepine drug for inhibiting specific [3H] diazepam binding was methaqualone (IC50 value of 150 μM). It is suggested that interactions with benzodiazepine receptors may account for the anxiolytic and anticonvulsive side effects of this drug. The analeptic drug pentylenetetrazole interacts with benzodiazepine receptor binding with an IC50 value of about 1 mM, which is possibly too high to explain its convulsive properties by an antagonism at the benzodiazepine receptor.
29 citations
TL;DR: It is suggested that oral drugs given for premedication need to be administered at least 2 hr before operation to obtain maximum sedative effects at a time when respiratory effects are returning to normal.
Abstract: SUMMARY A double-blind trial has been performed to investigate the respiratory effects of low oral doses of benzoctamine, and to compare them with diazepam and a placebo. The displacement of the carbon dioxide response curves indicated that whilst diazepam caused respiratory depression, benzoctamine had a variable effect. Some volunteers showed depression, but most showed stimulation. Peak respiratory effects were seen 1 hr after oral administration, returning to normal 2–3 hr after administration. It is suggested that oral drugs given for premedication need to be administered at least 2 hr before operation to obtain maximum sedative effects at a time when respiratory effects are returning to normal. In animal experiments it has been shown that the analgesic actions of morphine are diminished by concurrent administration of benzoctamine, and that the depression of respiratory rate caused by morphine is enhanced.
21 citations
TL;DR: 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.
Abstract: 1 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
2 Both drugs partially inhibited the α-ethyl-3-hydroxy-4-methylphenylethylamine-induced depletion of rat brain 5-HT
3 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
19 citations
1 Jan 1971
TL;DR: The results suggest a qualitative difference between benzodiazepines and barbiturates in depressing the intralimbic response, and show that the benzod rescinds the amplitude of the evoked potential and increases its latency.
Abstract: In unanesthetized curarized cats, the amplitude and the latency of the potential in the hippocampus evoked by stimulation of the baso-lateral nucleus of the amygdala was studied under the influence of cumulative doses of intravenously injected benzodiazepines (nitrazepam, diazepam, chlordiazepoxide and medazepam), sodium hexobarbitone, meprobamate, chlorpromazine, amitriptyline and benzoctamine.
11 citations
Related Topics (5)
Performance Metrics
| Year | Papers |
|---|---|
| 2016 | 1 |
| 1985 | 1 |
| 1983 | 2 |
| 1980 | 2 |
| 1978 | 2 |
| 1976 | 1 |