| Identification | Back Directory | [Name]
3-Amino-N-(4-methoxybenzyl)-4,6-dimethylthieno[2,3-b]pyridinecarboxamide | [CAS]
409351-28-6 | [Synonyms]
VU0152100
VU 152100
VU152100;VU 0152100;VU-0152100
3-Amino-N-(4-methoxybenzyl)-4,6-dimethylthieno[2,3-b]pyridinecarboxamide
3-Amino-N-[(4-methoxyphenyl)methyl]-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide
Thieno[2,3-b]pyridine-2-carboxamide, 3-amino-N-[(4-methoxyphenyl)methyl]-4,6-dimethyl- | [Molecular Formula]
C18H19N3O2S | [MDL Number]
MFCD02742972 | [MOL File]
409351-28-6.mol | [Molecular Weight]
341.43 |
| Chemical Properties | Back Directory | [density ]
1.282 | [storage temp. ]
Store at RT | [solubility ]
DMSO: >50mg/mL | [form ]
powder | [color ]
Light yellow to khaki | [InChI]
1S/C18H19N3O2S/c1-10-8-11(2)21-18-14(10)15(19)16(24-18)17(22)20-9-12-4-6-13(23-3)7-5-12/h4-8H,9,19H2,1-3H3,(H,20,22) | [InChIKey]
MDNWGCQSCGNTKH-UHFFFAOYSA-N | [SMILES]
COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)cc1 |
| Safety Data | Back Directory | [Hazard Codes ]
T | [Risk Statements ]
25-36 | [Safety Statements ]
26-45 | [RIDADR ]
UN 2811 6.1 / PGIII | [WGK Germany ]
3 | [Storage Class]
6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects | [Hazard Classifications]
Acute Tox. 3 Oral
Eye Irrit. 2 |
| Hazard Information | Back Directory | [Uses]
VU 152100 is a positive allosteric modulator of muscarinic choline receptor M4. | [Biological Activity]
vu0152100 is a selective and positive allosteric modulators of m4 receptor with the ec50 value of 380±93nm[1].vu0152100 has shown a potent positive allosteric modulators that increase the response of the m4 receptor to the endogenous agonist ach in in vitro study. in addition, vu0152100 has been reported to dese-dependently potentiate the response to the agonist (ach) with the ec50 value of 1.9±0.2μm, and increase the maximal response to ach to approximately 130%. furthermore, vu0152100 has been revealed to enhance receptor activation by increasing the affinity of m4 for acetylcholine. apart from these, vu0152100 has been found to induce a 20 to 25-fold leftward shift in the potency of ach to displace [3h]nms binding to m4 receptor with the ki value from 252±19.7nm to 12.2±0.49nm [1]. | [in vivo]
VU0152100 (10, 30, 56.6 mg/kg; i.p.; single) reverses amphetamine-induced hyperlocomotion in rats[1].
VU0152100 (10, 30, 56.6 mg/kg; i.p.; single) blocks amphetamine-induced disruption of the acquisition of contextual fear conditioning and prepulse inhibition of the acoustic startle reflex in rats[1].
VU0152100 reverses amphetamine-induced increases in extracellular dopamine levels in nucleus accumbens and caudate-putamen[1]. | Animal Model: | Adult male Sprague-Dawley rats (250-275 g; amphetamine-induced hyperlocomotion model)[1]. | | Dosage: | 10, 30, 56.6 mg/kg | | Administration: | Intraperitoneal injection; single (pre-treatment) | | Result: | Produced a robust dose-dependent reversal of amphetamine-induced hyperlocomotion. |
| Animal Model: | Adult male Sprague-Dawley rats (250-275 g; amphetamine-induced)[1]. | | Dosage: | 10, 30, 56.6 mg/kg | | Administration: | Intraperitoneal injection; single (pre-treatment) | | Result: | Blocked amphetamine-induced disruption of prepulse inhibition.
Dose-dependently reversed the disruptive effects of amphetamine on the acquisition of a context-dependent fear.
|
| [IC 50]
mAChR4 | [storage]
Store at RT | [References]
[1] brady ae1, jones ck, bridges tm, kennedy jp, thompson ad, heiman ju, breininger ml, gentry pr, yin h, jadhav sb, shirey jk, conn pj, lindsley cw. centrally active allosteric potentiators of the m4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats. j pharmacol exp ther. 2008 dec;327(3):941-53. |
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SPIRO PHARMA
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www.spiropharma.com.cn |
| Company Name: |
Musechem
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+1-800-259-7612 |
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www.musechem.com |
| Company Name: |
DC Chemicals
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021-58447131 13564518121 |
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www.chemicalbook.com/showsupplierproductslist927327/0_en.htm |
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