Category: 93835-05-3

尾-Carboline-3-carboxylate-tert-butyl ester: a selective BZ₁ benzodiazepine receptor antagonist was written by Shannon, H. E.;Guzman, F.;Cook, J. M.. And the article was included in Life Sciences in 1984.Formula: C16H16N2O2 This article mentions the following:

The effectiveness of 尾-carboline-3-carboxylate-tert-Bu聽ester (尾CCtB) [93835-05-3] in antagonizing the anticonvulsant, ataxic, and antipunishment effects of diazepam were evaluated. The mice, 尾CCtB at doses of 3 and 10 mg/kg produced a dose-related antagonism of the anticonvulsant effects of diazepam against pentylenetetrazole (80 mg/kg). A dose of 30 mg/kg of BCCtB did not produce a further shift in the diazepam dose-effect curve, apparently because 尾CCtB failed to block the muscle-relaxant effects of diazepam. Further, 尾CCtB (30 mg/kg) failed to antagonize the ataxic effects of diazepam in an inverted screen test. Rats responded under a multiple schedule where in one component every twentieth response (FR20) resulted in water presentation (unpunished component) and in another component every twentieth response (FR20) resulted in both shock and water presentation (punished component). Diazepam orally (0.1 to 10 mg/kg) first increased and then decreased rates in the punished component but only decreased rates in the unpunished component. 尾CCtB had no effect on response rates when administered alone, but antagonized the rate-increasing effects of diazepam in the punished component. 尾CCtB did not alter the rate-decreasing effects of diazepam in either component. Thus, 尾CCtB selectively antagonized the effects of diazepam on punished behavior as well as the anticonvulsant effects of diazepam, but 尾CCtB failed to antagonize the rate-decreasing and ataxic effects of diazepam. These results are consistent with the interpretation that 尾CCtB is a selective BZ₁ benzodiazepine receptor antagonist. In the experiment, the researchers used many compounds, for example, tert-Butyl 9H-pyrido[3,4-b]indole-3-carboxylate (cas: 93835-05-3Formula: C16H16N2O2).

tert-Butyl 9H-pyrido[3,4-b]indole-3-carboxylate (cas: 93835-05-3) belongs to indole derivatives. Indole, also called Benzopyrrole, a heterocyclic organic compound occurring in some flower oils, such as jasmine and orange blossom, in coal tar, and in fecal matter. It is used in perfumery and in making tryptophan, an essential amino acid, and indoleacetic acid (heteroauxin), a hormone that promotes the development of roots in plant cuttings.Formula: C16H16N2O2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Behavioral effects of benzodiazepine antagonists in chlordiazepoxide tolerant and non-tolerant rats was written by Takada, K.;Suzuki, T.;Hagen, T.;Cook, J. M.;Katz, J. L.. And the article was included in Life Sciences in 1989.COA of Formula: C16H16N2O2 This article mentions the following:

Rats were trained to respond under 3-min fixed-interval schedules of food presentation, and effects of the benzodiazepine-receptor ligands, flumazenil, 2-(4-methoxyphenyl)pyrazolo[4,3-c]quinolin-3(5H)-one (CGS 9895), 3-carbo-t-butoxy-尾-carboline (尾-CCtB), and 尾-carboline-3-carboxylic acid Et ester (尾-CCE) were assessed before and after the induction of tolerance to chlordiazepoxide. Before daily administration of chlordiazepoxide, none of the antagonists produced appreciable effects on rates of responding up to doses of 32.0 mg/kg i.p. 尾-CCE was the only antagonist studied at a higher dose (100.0 mg/kg i.p.), which decreased response rates. After 23 days of daily chlordiazepoxide administration (oral doses started at 10 and increased to 100 mg/kg/day by the 17th day), dose-effect curves for chlordiazepoxide were shifted to the right by about one-half log unit. Subjects were also more sensitive to the flumazenil, CGS 9895, and 尾-CCtB; however, since these drugs produced only small effects in non-tolerant subjects, precise estimates of the degree of the shift in dose-effect curves could not be estimated However, there were differences in the changes in the dose-effect curves induced by chlordiazepoxide tolerance. These results suggest differences in mechanism of action of antagonists in tolerant and non-tolerant subjects, and further that the sensitivity that is induced to antagonists in tolerant subjects is not conferred equally to all drugs having benzodiazepine antagonist activity. In the experiment, the researchers used many compounds, for example, tert-Butyl 9H-pyrido[3,4-b]indole-3-carboxylate (cas: 93835-05-3COA of Formula: C16H16N2O2).

tert-Butyl 9H-pyrido[3,4-b]indole-3-carboxylate (cas: 93835-05-3) belongs to indole derivatives. The indole subunit is an almost ubiquitous component of biologically active natural products, and its study has been the focus of research for decades. In addition to indole, the strain-release chemistry worked for numerous substrates including amines, alcohols, thiols, carboxylic acids, imidazoles, and pyrazoles.COA of Formula: C16H16N2O2

Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles