| Identification | Back Directory | [Name]
5-Amino-3,4-dimethyl-thieno[2,3-c]pyridazine-6-carboxylic acid 4-trifluoromethanesulfonyl-benzylamide | [CAS]
1451993-15-9 | [Synonyms]
VU0467154
VU0467154, VU-0467154, VU 0467154
5-Amino-3,4-dimethyl-thieno[2,3-c]pyridazine-6-carboxylic acid 4-trifluoromethanesulfonyl-benzylamide
Thieno[2,3-c]pyridazine-6-carboxamide, 5-amino-3,4-dimethyl-N-[[4-[(trifluoromethyl)sulfonyl]phenyl]methyl]- | [Molecular Formula]
C17H15F3N4O3S2 | [MOL File]
1451993-15-9.mol | [Molecular Weight]
444.45 |
| Chemical Properties | Back Directory | [density ]
1.514±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: Soluble | [form ]
A solid | [pka]
11.80±0.46(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor that potentiates acetylcholine responses in CHO cells expressing M4 receptors (EC50s = 17.7, 630, and 1,000 nM for rat, human, and cynomolgus monkey receptors, respectively).1 It is selective for M4 over M1-3 and M5 receptors and a panel of receptors, transporters, and cation channels when used at a concentration of 10 μM. In vivo, VU0467154 (3-56.6 mg/kg, p.o.) reverses amphetamine-induced hyperlocomotion in rats. It reverses MK-801-induced hyperlocomotion, deficits in a pairwise visual discrimination task, and impairments in the acquisition of contextual fear conditioning in wild-type, but not M4 knockout, mice. VU0467154 (3-30 mg/kg) also increases freezing behavior in contextual and tone fear conditioning tests in wild-type mice when administered prior to the conditioning session. Chronic administration of VU0467154 (10 mg/kg once daily) reduces motor incoordination and prevents decreases in locomotion in the YAC128 transgenic mouse model of Huntington''s disease.2 | [Uses]
VU 0467154, is a positive allosteric modulators of the M4 muscarinic acetylcholine receptor (mAChR), robustly potentiates the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey (cyno) M4 receptor, respectively. |
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InvivoChem
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