Pyrazolam
Pyrazolam Basic information
- Product Name:
- Pyrazolam
- Synonyms:
-
- Pyrazolam
- 8-Bromo-1-methyl-6-(pyridin-2-yl)-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine
- formaty
- Pyrazolam solution
- 4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine, 8-bromo-1-methyl-6-(2-pyridinyl)-
- 8-Bromo-1-methyl-6-(2-pyridinyl)-4H-[1,2,4]triazolo[4,3-a][1,4]be nzodiazepine
- ANTIOXIDANT PUB-380
- Pyrazolam 1
- CAS:
- 39243-02-2
- MF:
- C16H12BrN5
- MW:
- 354.2
- EINECS:
- 200-258-5
- Product Categories:
-
- Pyrazolam
- 39243-02-2
- Mol File:
- 39243-02-2.mol
Pyrazolam Chemical Properties
- Melting point:
- 253-255 °C
- Boiling point:
- 544.4±60.0 °C(Predicted)
- Density
- 1.62±0.1 g/cm3(Predicted)
- storage temp.
- -20°C
- solubility
- DMF: 30 mg/ml; DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml; DMSO: 20 mg/ml; Ethanol: 10 mg/ml; Methanol: 1 mg/ml
- form
- A crystalline solid
- pka
- 2.18±0.40(Predicted)
- InChI
- InChI=1S/C16H12BrN5/c1-10-20-21-15-9-19-16(13-4-2-3-7-18-13)12-8-11(17)5-6-14(12)22(10)15/h2-8H,9H2,1H3
- InChIKey
- BGRWSFIQQPVEML-UHFFFAOYSA-N
- SMILES
- N12C(C)=NN=C1CN=C(C1=NC=CC=C1)C1=CC(Br)=CC=C12
Pyrazolam Usage And Synthesis
Description
Pyrazolam (SH-I-04) is a benzodiazepine derivative originally developed by a team led by Leo Sternbach at Hoffman-La Roche in the 1970s. It has since been "rediscovered" and sold as a designer drug since 2012.
Pyrazolam has structural similarities to alprazolam and bromazepam. Unlike other benzodiazepines, pyrazolam does not appear to undergo metabolism, instead being excreted unchanged in the urine. It is most selective for the α2 and α3 subtypes of the GABAA receptor.
Chemical Properties
Pyrazolam is a benzodiazepine that has been abused recreationally. Like other benzodiazepines, pyrazolam has anxiolytic effects.
Uses
Pyrazolam is a benzodiazepine with an elimination half-life of about 17 hours and no detectable metabolites in human serum and urine; thus pyrazolam may go undetected without instrumental analytical techniques.
Application
Pyrazolam is a designer benzodiazepine that has been sold online as a 'legal high' or 'research chemical'. Since its emergence in Europe a few years ago, pyrazolam, along with other designer benzodiazepines, have increasingly been encountered in forensic case work.
Biological Activity
Pyrazolam has structural similarities to alprazolam and bromazepam. Unlike other benzodiazepines, pyrazolam does not appear to undergo metabolism, instead being excreted unchanged in the urine.It is most selective for the α2 and α3 subtypes of the GABAA receptor.
Pharmacology
Benzodiazepines produce a variety of effects by binding to the benzodiazepine receptor site and magnifying the efficiency and effects of the neurotransmitter gamma aminobutyric acid (GABA) by acting on its receptors. As this site is the most prolific inhibitory receptor set within the brain, its modulation results in the sedating (or calming effects) of pyrazolam on the nervous system.The anticonvulsant properties of benzodiazepines may be, in part or entirely, due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors.Pyrazolam is most selective for the α2 and α3 receptor subtypes. It is excreted by the body unchanged thus not interacting with liver enzymes like other benzodiazepines, meaning that its use in people with reduced liver function may be safer.