SSD114 hydrochloride

• CAT Number: I046320
• CAS Number: 2319790-02-6
• Molecular Formula: C18H21ClF3N3O
• Molecular Weight: 387.83
• Purity: ≥95%
• Synonyms: N-cyclohexyl-4-methoxy-6-[4-(trifluoromethyl)phenyl]pyrimidin-2-amine;hydrochloride
• InChI: InChI=1S/C18H20F3N3O.ClH/c1-25-16-11-15(12-7-9-13(10-8-12)18(19,20)21)23-17(24-16)22-14-5-3-2-4-6-14;/h7-11,14H,2-6H2,1H3,(H,22,23,24);1H
• InChIKey: YXQSTPASDICGCA-UHFFFAOYSA-N
• SMILES: COC1=NC(=NC(=C1)C2=CC=C(C=C2)C(F)(F)F)NC3CCCCC3.Cl

SSD114 hydrochloride is a novel GABAB receptor positive allosteric modulator.
In the presence of 10 µM GABA, SSD114 hydrochloride at 25 µM significantly increases (to approximately 170% above basal levels) the [35S]GTPγS stimulation induced by GABA alone. SSD114 hydrochloride, added at 15 and 30 µM, induces a leftward shift of the GABA concentration-response curve with a slight concomitant increase of maximal GABA stimulation at the highest concentration. In the presence of both 15 and 30 µM SSD114 hydrochloride, the EC50 for GABA decreases by 2 and 2.5 fold, respectively, while the maximal stimulation (Emax) is potentiated only at the concentration of 30 µM, reaching 161±5.09% over the basal value[1] .
The onset of loss of righting reflex (LORR) is reduced by pretreatment with SSD114 hydrochloride [F(5,30)=4.55, P<0.005]. Post hoc analysis indicates that the onset of LORR is significantly lower in mouse groups pretreated with doses of SSD114 hydrochloride equal to or higher than 10 mg/kg than in vehicle-treated mice. The duration of LORR is increased by pretreatment with SSD114 hydrochloride [F(5,30)=4.81, P<0.005]. Post hoc analysis indicates that the duration of LORR is significantly longer in mouse groups pretreated with 10 and 100 mg/kg SSD114 hydrochloride than in vehicle-treated mice[1].

Reference

[1]. Porcu A, et al. In vitro and in vivo pharmacological characterization of SSD114, a novel GABAB positive allosteric modulator. Eur J Pharmacol. 2016 Nov 15;791:115-123.
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