1704716-36-8
Chemical Structure
ASP8062
- CAS No.: 1704716-36-8
- Formula:C20H29N3O2S2
- Molecular Weight:407.59
InChIKey: USFNNXLOYXNESM-UHFFFAOYSA-N
SMILES: O=S1(CCN(CC1)CC2=C3C=C(C4CCC(C)(CC4)C)SC3=NC(C)=N2)=O
Biological Activity: ASP8062 is an orally active, blood-brain barrier-permeable selective GABAB receptor positive allosteric modulator. ASP8062 enhances GABA-mediated activation of GABAB receptors and strengthens GABAergic neurotransmission. ASP8062 reverses Reserpine (HY-N0480)-induced myalgia, regulates the sleep-wake cycle, increases delta wave power during non-REM sleep, and impairs motor coordination at high doses. ASP8062 penetrates the central nervous system with a half-life of 40-50 h. ASP8062 can be used in research related to opioid use disorder, fibromyalgia, chronic pain, and alcohol use disorder[1][2][3][4].
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ASP8062 | ASP8062 is an orally active, blood-brain barrier-permeable selective GABAB receptor positive allosteric modulator. ASP8062 enhances GABA-mediated activation of GABAB receptors and strengthens GABAergic neurotransmission. ASP8062 reverses Reserpine (HY-N0480)-induced myalgia, regulates the sleep-wake cycle, increases delta wave power during non-REM sleep, and impairs motor coordination at high doses. ASP8062 penetrates the central nervous system with a half-life of 40-50 h. ASP8062 can be used in research related to opioid use disorder, fibromyalgia, chronic pain, and alcohol use disorder. | |||||||||||||||||||||
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References
- [1]. Akuzawa S, et al. Effect of ASP8062 on morphine self-administration and morphine-induced respiratory suppression in monkeys. Journal of pharmacological sciences. 2023 Apr;151(4):171-176. [Content Brief]
- [2]. Walzer M, et al. Single- and Multiple-Dose Safety, Tolerability, and Pharmacokinetic Profiles of ASP8062: Results From 2 Phase 1 Studies. Clinical pharmacology in drug development. 2020 Apr;9(3):297-306. [Content Brief]
- [3]. Murai N, et al. A novel GABAB receptor positive allosteric modulator, ASP8062, exerts analgesic effects in a rat model of fibromyalgia. European Journal of Pharmacology. 2020;866:172750. [Content Brief]
- [4]. Haile CN, et al. The GABA receptor positive allosteric modulator ASP8062 reduces operant alcohol self-administration in male and female Sprague Dawley rats. Psychopharmacology. 2021 Sep;238(9):2587-2600. [Content Brief]
