Bretazenil
Bretazenil structure
|
Common Name | Bretazenil | ||
|---|---|---|---|---|
| CAS Number | 84379-13-5 | Molecular Weight | 418.284 | |
| Density | 1.6±0.1 g/cm3 | Boiling Point | 594.3±50.0 °C at 760 mmHg | |
| Molecular Formula | C19H20BrN3O3 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 313.2±30.1 °C | |
|
A Comparison of the α2/3/5 Selective Positive Allosteric Modulators L-838,417 and TPA023 in Preclinical Models of Inflammatory and Neuropathic Pain.
Adv. Pharmacol. Sci. 2011 , 608912, (2011) GABA(A) receptors containing α2/3 subunits are current targets in the battle to develop new pain medications, as they are expressed in the spinal cord where increasing inhibitory drive should result in analgesia. However, this approach is prone to a range of ... |
|
|
A comparison of chlordiazepoxide, bretazenil, L838,417 and zolpidem in a validated mouse Vogel conflict test.
Psychopharmacology 182(4) , 475-84, (2005) GABAA receptors containing an alpha2 subunit are proposed to mediate the anxiolytic effect of benzodiazepines (BZ) based on studies in transgenic mice using unconditioned models of anxiety. Conditioned models of anxiety were not assessed and are rarely encoun... |
|
|
Contextual fear conditioning and baseline startle responses in the rat fear-potentiated startle test: a comparison of benzodiazepine/gamma-aminobutyric acid-A receptor agonists.
Behav. Pharmacol. 11(6) , 495-504, (2000) In the rat, fear-potentiated startle (FPS) test animals are first trained to associate brief light presentations with a mild electric footshock and then tested for startle responses to acoustic stimuli, delivered either in darkness (i.e. baseline startle) or ... |
|
|
Self-administration of bretazenil under progressive-ratio schedules: behavioral economic analysis of the role intrinsic efficacy plays in the reinforcing effects of benzodiazepines.
Drug Alcohol Depend. 113(2-3) , 157-64, (2011) Previous research suggests that intrinsic efficacy of benzodiazepines is an important determinant of their behavioral effects. We evaluated the reinforcing effects of the benzodiazepine partial agonist bretazenil using behavioral economic models referred to a... |
|
|
Differential behavioral effects of low efficacy positive GABAA modulators in combination with benzodiazepines and a neuroactive steroid in rhesus monkeys.
Br. J. Pharmacol. 147(3) , 260-8, (2006) In the clinic, low efficacy positive GABAA modulators might be preferred to high efficacy positive modulators insofar as low efficacy modulators might have comparatively less abuse and dependence liability. Drug discrimination was used to examine the behavior... |
|
|
Ribozyme-mediated reduction of the GABA(A) receptor alpha1 subunit.
Brain Res. Mol. Brain Res. 92(1-2) , 149-56, (2001) As an approach to understanding the role of the alpha1 subunit of the GABA(A) receptor, ribozymes were designed to reduce expression of this subunit protein by hydrolysis of alpha1 subunit message and antisense inactivation. The ribozyme cleavage sites were s... |
|
|
Selective overexpression of Comt in prefrontal cortex rescues schizophrenia-like phenotypes in a mouse model of 22q11 deletion syndrome.
Transl. Psychiatry 2 , e146, (2012) The 22q11.2 microdeletion is one of the highest genetic risk factors for schizophrenia. It is not well understood which interactions of deleted genes in 22q11.2 regions are responsible for the pathogenesis of schizophrenia, but catechol-O-methytransferase (CO... |
|
|
Bretazenil, a benzodiazepine receptor partial agonist, as an adjunct in the prophylactic treatment of OP poisoning.
J. Appl. Toxicol. 21 Suppl 1 , S115-9, (2001) Benzodiazepines, mainly diazepam, are commonly used as anticonvulsants in the treatment of organophosphate casualties. Although very effective, diazepam usually is not used in prophylactic treatments because of its adverse effects on task performance and its ... |
|
|
Selective labelling of diazepam-insensitive GABAA receptors in vivo using [3H]Ro 15-4513.
Br. J. Pharmacol. 146(6) , 817-25, (2005) Classical benzodiazepines (BZs), such as diazepam, bind to GABAA receptors containing alpha1, alpha2, alpha3 or alpha5 subunits that are therefore described as diazepam-sensitive (DS) receptors. However, the corresponding binding site of GABAA receptors conta... |
|
|
Effects of benzodiazepine receptor ligands and ethanol in rats trained to discriminate pregnanolone.
Pharmacol. Biochem. Behav. 67(3) , 483-7, (2000) Although GABA(A) receptor positive modulators share many behavioral effects, subtle differences have been detected among their discriminative stimulus effects. The purpose of the present study was to determine the extent of shared discriminative stimulus effe... |