82230-53-3
Chemical Structure
Girisopam
- CAS No.: 82230-53-3
- Formula:C18H17ClN2O2
- Molecular Weight:328.79
InChIKey: VQYLGVVODFDFNK-UHFFFAOYSA-N
SMILES: ClC1=CC=CC(C2=NN=C(CC3=C2C=C(OC)C(OC)=C3)C)=C1
Biological Activity: Girisopam is a PDE inhibitor with IC50 values of 3.2, 4.0, and 12.5 μM against PDE4, PDE2, and PDE5, respectively. Girisopam exhibits anxiolytic, antidepressant, anti-aggressive, and antipsychotic activities. The binding sites of Girisopam are enriched exclusively in the basal ganglia of rat brains, and depletion of these sites is associated with damage to the striatonigral pathway. Girisopam enhances the potency of μ-opioid receptor agonists, attenuates the antagonistic effect of low-dose Naloxone (HY-17417A), and synergistically potentiates the anti-fighting effect of Chlorpromazine (HY-12708). Girisopam can be used in studies related to psychiatric disorders such as anxiety and depression[1][2][3][4][5].
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Girisopam | Girisopam is a PDE inhibitor with IC50 values of 3.2, 4.0, and 12.5 μM against PDE4, PDE2, and PDE5, respectively. Girisopam exhibits anxiolytic, antidepressant, anti-aggressive, and antipsychotic activities. The binding sites of Girisopam are enriched exclusively in the basal ganglia of rat brains, and depletion of these sites is associated with damage to the striatonigral pathway. Girisopam enhances the potency of μ-opioid receptor agonists, attenuates the antagonistic effect of low-dose Naloxone (HY-17417A), and synergistically potentiates the anti-fighting effect of Chlorpromazine (HY-12708). Girisopam can be used in studies related to psychiatric disorders such as anxiety and depression. | |||||||||||||||||||||
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- [1]. Bihel FJ, et al. New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam. Bioorganic & medicinal chemistry letters. 2011 Nov 01;21(21):6567-72.
- [2]. Palkovits M, et al. Binding of girisopam (a 2,3-benzodiazepine derivative) to the substantia nigra is prevented by lesioning of the striatonigral pathway. Neuroscience. 1998 Apr;83(3):799-806.
- [3]. Horváth EJ, et al. Changes in specific binding sites of girisopam after chemical and surgical lesions in the striato-nigral system. Brain research. Molecular brain research. 1997 Apr;45(1):141-4.
- [4]. Horváth EJ, et al. A novel specific binding site for homophthalazines in the rat brain. Eur J Pharmacol. 1993 May 12;236(1):151-3.
- [5]. Fekete MI, et al. Selective interaction of homophtalazine derivatives with morphine. European journal of pharmacology. 1997 Jul 23;331(2-3):175-83.
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