CAS 409351-28-6|VU0152100
| Common Name | VU0152100 | ||
|---|---|---|---|
| CAS Number | 409351-28-6 | Molecular Weight | 341.42700 |
| Density | / | Boiling Point | / |
| Molecular Formula | C18H19N3O2S | Melting Point | / |
| MSDS | ChineseUSA | Flash Point | / |
| Symbol | GHS06 | Signal Word | Danger |
Names
| Name | 3-amino-N-[(4-methoxyphenyl)methyl]-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide |
|---|---|
| Synonym | More Synonyms |
VU0152100 BiologicalActivity
| Description | VU0152100 is a potent and selective allosteric potentiator of M4 mAChR with an EC50 of 380 ± 93 nM.IC50 Value: 380 ± 93 nM (EC50) [1]Target: M4 mAChRin vitro: VU0152100 was selective for M4 relative to M1, M2, M3, and M5. VU0152100 dose-dependently potentiated the response to an EC20 concentration of ACh with EC50 values of 1.9 ± 0.2 μM, and increased the maximal response to ACh to approximately 130%. VU0152100 (10 μM) also enhanced the potency of ACh to induce GIRK-mediated thallium flux, as manifest by a robust (≈30-fold) leftward shift in the ACh CRC from 77 ± 1.2 nM (veh) to 2.35 ± 0.5 nM (VU0152100) [1].in vivo: Systemic administration of VU0152099 and VU0152100 provides robust brain levels of these compounds, the effects of VU0152099 and VU0152100 were evaluated in reversing amphetamine-induced hyperlocomotion in rats using a dose of 56.6 mg/kg i.p. for each compound with a 30-min pretreatment interval [1]. |
|---|---|
| Related Catalog | Signaling Pathways >>GPCR/G Protein >>mAChRSignaling Pathways >>Neuronal Signaling >>mAChRResearch Areas >>Neurological Disease |
| References | [1]. Brady AE, et al. 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. |
Chemical & Physical Properties
| Molecular Formula | C18H19N3O2S |
|---|---|
| Molecular Weight | 341.42700 |
| Exact Mass | 341.12000 |
| PSA | 105.48000 |
| LogP | 4.40600 |
| InChIKey | MDNWGCQSCGNTKH-UHFFFAOYSA-N |
| SMILES | COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)cc1 |
| Storage condition | 2-8℃ |
Safety Information
| Symbol | GHS06 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H301-H319 |
| Precautionary Statements | P301 + P310-P305 + P351 + P338 |
| RIDADR | UN 2811 6.1 / PGIII |
Articles3
More Articles| Regulation of synaptic MAPK/ERK phosphorylation in the rat striatum and medial prefrontal cortex by dopamine and muscarinic acetylcholine receptors. J. Neurosci. Res. 93 , 1592-9, (2015) Dopamine and acetylcholine are two principal transmitters in the striatum and are usually balanced to modulate local neural activity and to maintain striatal homeostasis. This study investigates the r... | |
| Investigation of the presence and antinociceptive function of muscarinic acetylcholine receptors in the African naked mole-rat (Heterocephalus glaber). J. Comp. Physiol. A. Neuroethol. Sens. Neural. Behav. Physiol. 202 , 7-15, (2016) The present study investigated the cholinergic system in the African naked mole-rat (Heterocephalus glaber) with focus on the muscarinic acetylcholine receptor subtypes M1 and M4. The protein sequence... | |
| Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents. ACS Chem. Neurosci. 5(10) , 920-42, (2014) Positive allosteric modulators (PAMs) of the M4 muscarinic acetylcholine receptor (mAChR) represent a novel approach for the treatment of psychotic symptoms associated with schizophrenia and other neu... |
Synonyms
| ML108 |
| 3-Amino-N-[(4-methoxyphenyl)methyl]-4,6-dimethyl-thieno[2,3-b]pyridine-2-carboxamide |
| Kinome_1269 |
| VU0152100 |
