VU0152100
Modify Date: 2024-01-09 11:28:50
VU0152100 structure
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Common Name | VU0152100 | ||
|---|---|---|---|---|
| CAS Number | 409351-28-6 | Molecular Weight | 341.42700 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C18H19N3O2S | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | N/A | |
| Symbol |
GHS06 |
Signal Word | Danger | |
Use of VU0152100VU0152100 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]. |
| Name | 3-amino-N-[(4-methoxyphenyl)methyl]-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide |
|---|---|
| Synonym | More Synonyms |
| 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]. |
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| Related Catalog | |
| References |
| Molecular Formula | C18H19N3O2S |
|---|---|
| Molecular Weight | 341.42700 |
| Exact Mass | 341.12000 |
| PSA | 105.48000 |
| LogP | 4.40600 |
| Storage condition | 2-8℃ |
| Symbol |
GHS06 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H301-H319 |
| Precautionary Statements | P301 + P310-P305 + P351 + P338 |
| RIDADR | UN 2811 6.1 / PGIII |
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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... |
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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... |
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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... |
| ML108 |
| 3-Amino-N-[(4-methoxyphenyl)methyl]-4,6-dimethyl-thieno[2,3-b]pyridine-2-carboxamide |
| Kinome_1269 |
| VU0152100 |