|Related Categories||A, A-AM, AA to AL, Alphabetical Index of Analytical Standards, Analytical Standards,|
|drug control||USDEA Schedule IV; Home Office Schedule 4.1; psychotrope; kontrollierte Droge in Deutschland; regulated under CDSA - not available from Sigma-Aldrich Canada|
Alprazolam binds the GABAA receptor at the benzodiazepine site, which is different than the ligand-binding site at which GABA binds. Alprazolam has been shown to be an anxiolytic (anti-anxiety agent) as well as having anticonvulsant, muscle relaxant and antidepressant activity.1
Alprazolam is a triazole-containing benzodiazepine that is related to diazepam and other 1,4-benxodiazepines. Like other benzodiazepines, Alprazolam is a GABAergic agonist that modulates GABAA receptors.2 GABAA receptors in the central nervous system are ligand-gated ion channels that are bound by the stimulatory neurotransmitter GABA; binding of this ligand allows ion movement through the channel and results in neurotransmission inhibition.
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GABAA receptors are responsible for the majority of neuronal inhibition in the mammalian CNS. Agonist activation results in the opening of their integral anion channel, generally leading to hyperpola...
Keywords: Anticonvulsants, Central Nervous System, Cloning, Gene expression, Ligands, Neurotransmitters, Phosphorylations, Schizophrenia, Transduction
2. An Overview of the CNS-Pharmacodynamic Profiles of Nonselective and Selective GABA Agonists Chen, X., et al. Adv. Pharmacol. Sci. 2012, 1-10, (2012)
Contribution of alpha1 subunit-containing gamma-aminobutyric acidA (GABAA) receptors to motor-impairing effects of benzodiazepines in squirrel monkeys. Licata SC Psychopharmacology 203(3), 539-46, (2009)
Concentrations of alprazolam in blood from impaired drivers and forensic autopsies were not much different but showed a high prevalence of co-ingested illicit drugs. Jones AW and Holmgren A J. Psychopharmacol. 27(3), 276-81, (2013)
A novel microextraction by packed sorbent-gas chromatography procedure for the simultaneous analysis of antiepileptic drugs in human plasma and urine. Rani S and Malik AK J. Sep. Sci. 35(21), 2970-7, (2012)
Literature based drug interaction prediction with clinical assessment using electronic medical records: novel myopathy associated drug interactions. Duke JD, Han X, Wang Z, et al. PLoS Comput. Biol. 8(8), e1002614, (2012)
Bilateral acute necrosis of the globi pallidi and rhabdomyolysis due to combined methadone and benzodiazepine toxicity. Corliss RF, Mandal R, and Soriano BJ Am. J. Forensic Med. Pathol. 34(1), 1-4, (2013)
Air to lung partition coefficients for volatile organic compounds and blood to lung partition coefficients for volatile organic compounds and drugs. Michael H Abraham et al Eur. J. Med. Chem. 43, 478-85, (2008)
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data. Xiaofan Sui et al Eur. J. Med. Chem. 44, 4455-60, (2009)
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