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Low IC 50 or high pIC 50 values indicate tighter binding (pIC 50 of 8.0 = IC 50 of 10nM, pIC 50 of 9.0 = IC 50 of 1nM, etc.) These are non subtype selective IC 50 values averaged across all GABA A receptor subtypes , so subtype selective compounds with strong binding at one subtype but weak at others will appear unusually weak due to averaging ...
Nordazepam is a partial agonist at the GABA A receptor, which makes it less potent than other benzodiazepines, particularly in its amnesic and muscle-relaxing effects. [6] Its elimination half life is between 36 and 200 hours, with wide variation among individuals; factors such as age and sex are known to impact it. [2]
Desmethyldiazepam has a half-life of 36–200 hours, and flurazepam, with the main active metabolite of desalkylflurazepam, with a half-life of 40–250 hours. These long-acting metabolites are partial agonists. [6] [145] Short-acting compounds have a median half-life of 1–12 hours.
The half-life of chlordiazepoxide is from 5 to 30 hours but has an active benzodiazepine metabolite, nordiazepam, which has a half-life of 36 to 200 hours. [31] The half-life of chlordiazepoxide increases significantly in the elderly, which may result in prolonged action as well as accumulation of the drug during repeated administration.
Nitrazepam is a long-acting benzodiazepine with an elimination half-life of 15–38 hours (mean elimination half-life 26 hours). [12] Residual "hangover" effects after nighttime administration of nitrazepam such as sleepiness, impaired psychomotor and cognitive functions may persist into the next day, which may impair the ability of users to ...
Flutazolam [1] (Coreminal, MS-4101) is a drug which is a benzodiazepine derivative. It was invented in Japan, and this is the main country in which it has been used medically. It was invented in Japan, and this is the main country in which it has been used medically.
Pyrazolam (SH-I-04) [2] is a benzodiazepine derivative originally developed by a team led by Leo Sternbach at Hoffman-La Roche in the 1970s. [3] It has since been "rediscovered" and sold as a designer drug since 2012.
Medazepam is a drug that is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative, and skeletal muscle relaxant properties. It is known by the following brand names: Azepamid, Nobrium, Tranquirax (mixed with bevonium), Rudotel, Raporan, Ansilan and Mezapam. [2]