1207440-88-7
Chemical Structure
ADX71441
- CAS No.: 1207440-88-7
- Formula:C19H15ClF2N4O4
- Molecular Weight:436.80
IUPAC Name: N-(5-(4-(4-chloro-3-fluorobenzyl)-6-methoxy-3,5-dioxo-4,5-dihydro-1,2,4-triazin-2(3H)-yl)-2-fluorophenyl)acetamide
InChIKey: BQDMEJYNGXEHSW-UHFFFAOYSA-N
SMILES: O=C(N(C1=O)CC2=CC=C(C(F)=C2)Cl)C(OC)=NN1C3=CC=C(C(NC(C)=O)=C3)F
Biological Activity: ADX71441 is an orally active, blood-brain barrier penetrant positive allosteric modulator of GABAB receptor. ADX71441 potentiates the activity of endogenous GABA at GABAB receptor, with an EC50 of 96 nM. ADX71441 functionally inhibits adenosine transporters and 5-HT2B receptor. ADX71441 produces anxiolytic-like, analgesic, muscle relaxant, hypothermic and overactive bladder inhibitory effects, reduces acute locomotor activity levels, decreases voluntary intake of alcohol and saccharin, attenuates stress-induced neuronal activation, and exhibits anti-hyperalgesic activity[1][2][3][4].
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ADX71441 | 98.63% | ADX71441 is an orally active, blood-brain barrier penetrant positive allosteric modulator of GABAB receptor. ADX71441 potentiates the activity of endogenous GABA at GABAB receptor, with an EC50 of 96 nM. ADX71441 functionally inhibits adenosine transporters and 5-HT2B receptor. ADX71441 produces anxiolytic-like, analgesic, muscle relaxant, hypothermic and overactive bladder inhibitory effects, reduces acute locomotor activity levels, decreases voluntary intake of alcohol and saccharin, attenuates stress-induced neuronal activation, and exhibits anti-hyperalgesic activity. | ||||||||||||||||||||
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[1]. Kalinichev M, et al. The drug candidate, ADX71441, is a novel, potent and selective positive allosteric modulator of the GABAB receptor with a potential for treatment of anxiety, pain and spasticity. Neuropharmacology. 2017 Mar 1;114:34-47.
- [2]. Kalinichev M, et al. ADX71441, a novel, potent and selective positive allosteric modulator of the GABA(B) receptor, shows efficacy in rodent models of overactive bladder. Br J Pharmacol. 2014;171(4):995-1006. [Content Brief]
- [3]. Augier E, et al. The GABAB Positive Allosteric Modulator ADX71441 Attenuates Alcohol Self-Administration and Relapse to Alcohol Seeking in Rats. Neuropsychopharmacology. 2017;42(9):1789-1799. [Content Brief]
- [4]. Kalinichev M, et al. ADX71943 and ADX71441, novel positive allosteric modulators of the GABAB receptor with distinct central/peripheral profiles, show efficacy in the monosodium iodoacetate model of chronic osteoarthritis pain in the rat. Eur J Pharmacol. 2017;795:43-49. [Content Brief]
Keywords
