3-Amino-N-(4-methoxybenzyl)-4,6-dimethylthieno[2,3-b]pyridinecarboxamide

Product Name3-Amino-N-(4-methoxybenzyl)-4,6-dimethylthieno[2,3-b]pyridinecarboxamide
CAS409351-28-6
MFC18H19N3O2S
MW341.43
EINECS
MOL File409351-28-6.mol

Chemical Properties

Boiling point	600.037±55.00 °C(Press: 760.00 Torr)(predicted)
Density	1.282
storage temp.	Store at RT
solubility	DMSO: >50mg/mL
form	powder
pka	13.103±0.46(predicted)
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 Information

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

Usage And Synthesis

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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