942436-93-3
Chemical Structure
AZD6280
- CAS No.: 942436-93-3
- Formula:C20H22N4O3
- Molecular Weight:366.41
IUPAC Name: 4-amino-8-(2,5-dimethoxyphenyl)-N-propylcinnoline-3-carboxamide
InChIKey: NVWCZRPXYVDQEE-UHFFFAOYSA-N
SMILES: O=C(C1=NN=C2C(C3=CC(OC)=CC=C3OC)=CC=CC2=C1N)NCCC
Biological Activity: AZD6280 is an orally active, blood-brain barrier-permeable GABAA receptor modulator, with Ki values of 21 nM, 31 nM and 1680 nM against human receptors containing α2, α3 and α5 subtypes, respectively, and subtype-specific Ki values of < 30 nM for α2 and α3 subtypes. AZD6280 selectively potentiates GABAA receptors containing α2/α3 subtypes with higher potency than α1/α5 subtypes, exerts no modulatory effect on receptors containing α1 subtypes, and regulates the tuberoinfundibular dopaminergic pathway. AZD6280 decreases peak saccadic velocity, increases serum and plasma prolactin levels, rescues dendritic abnormalities of cortical neurons induced by DISC1 knockdown. AZD6280 can be used in studies related to anxiety disorders[1][2][3][4][5][6][7].
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AZD6280 | 98.17% | AZD6280 is an orally active, blood-brain barrier-permeable GABAA receptor modulator, with Ki values of 21 nM, 31 nM and 1680 nM against human receptors containing α2, α3 and α5 subtypes, respectively, and subtype-specific Ki values of < 30 nM for α2 and α3 subtypes. AZD6280 selectively potentiates GABAA receptors containing α2/α3 subtypes with higher potency than α1/α5 subtypes, exerts no modulatory effect on receptors containing α1 subtypes, and regulates the tuberoinfundibular dopaminergic pathway. AZD6280 decreases peak saccadic velocity, increases serum and plasma prolactin levels, rescues dendritic abnormalities of cortical neurons induced by DISC1 knockdown. AZD6280 can be used in studies related to anxiety disorders. | ||||||||||||||||||||
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- [1]. Chen X, et al. Human pharmacology of positive GABA-A subtype-selective receptor modulators for the treatment of anxiety. Acta pharmacologica Sinica. 2019 May;40(5):571-582. [Content Brief]
- [2]. Te Beek ET, et al. The effects of the nonselective benzodiazepine lorazepam and the α2 /α3 subunit-selective GABAA receptor modulators AZD7325 and AZD6280 on plasma prolactin levels. Clinical pharmacology in drug development. 2015 Mar;4(2):149-54. [Content Brief]
- [3]. Jucaite A, et al. GABA receptor occupancy by subtype selective GABA modulators: PET studies in humans. Psychopharmacology. 2017 Feb;234(4):707-716. [Content Brief]
- [4]. Jucaite A, er al. P. 1. g. 069 Relationship between dose, plasma concentration and GABA-A receptor occupancy by partial GABA-A receptor modulators. European Neuropsychopharmacology. 2015 Sep 1;25:S274.
- [5]. Chen X, et al. AZD6280, a novel partial γ-aminobutyric acid A receptor modulator, demonstrates a pharmacodynamically selective effect profile in healthy male volunteers. Journal of clinical psychopharmacology. 2015 Feb;35(1):22-33. [Content Brief]
- [6]. Saito A, et al. Early postnatal GABAA receptor modulation reverses deficits in neuronal maturation in a conditional neurodevelopmental mouse model of DISC1. Molecular psychiatry. 2016 Oct;21(10):1449-59. [Content Brief]
- [7]. Guo J, et al. Absorption, excretion, and metabolism of a potential GABA-A α2/3 receptor modulator in rats. Xenobiotica. 2011 May;41(5):385-99.
Keywords
