Date published: 2025-10-2

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VU 152100 (CAS 409351-28-6)

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Alternate Names:
ML 108; VU0152100
Application:
VU 152100 is a positive allosteric modulator of muscarinic choline receptor M4
CAS Number:
409351-28-6
Molecular Weight:
341.43
Molecular Formula:
C18H19N3O2S
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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A selective positive allosteric modulator of M4 muscarinic acetylcholine receptors (mAChRs) (EC50 = 380 nM). Has been shown to induce a 21-fold shift in ACh potency at M4 receptor. Displays no activity at other mAChR subtypes.


VU 152100 (CAS 409351-28-6) References

  1. Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats.  |  Brady, AE., et al. 2008. J Pharmacol Exp Ther. 327: 941-53. PMID: 18772318
  2. A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning.  |  Shirey, JK., et al. 2009. J Neurosci. 29: 14271-86. PMID: 19906975
  3. New technologies enabling the industrialization of allosteric modulator discovery.  |  Lütjens, R., et al. 2013. Drug Discov Today Technol. 10: e253-60. PMID: 24050276
  4. Development of allosteric modulators of GPCRs for treatment of CNS disorders.  |  Nickols, HH. and Conn, PJ. 2014. Neurobiol Dis. 61: 55-71. PMID: 24076101
  5. Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents.  |  Bubser, M., et al. 2014. ACS Chem Neurosci. 5: 920-42. PMID: 25137629
  6. Investigation of the presence and antinociceptive function of muscarinic acetylcholine receptors in the African naked mole-rat (Heterocephalus glaber).  |  Jørgensen, KB., et al. 2016. J Comp Physiol A Neuroethol Sens Neural Behav Physiol. 202: 7-15. PMID: 26520141
  7. Mutual activation of glutamatergic mGlu4 and muscarinic M4 receptors reverses schizophrenia-related changes in rodents.  |  Cieślik, P., et al. 2018. Psychopharmacology (Berl). 235: 2897-2913. PMID: 30054675
  8. Simultaneous activation of muscarinic and GABAB receptors as a bidirectional target for novel antipsychotics.  |  Cieślik, P., et al. 2019. Behav Brain Res. 359: 671-685. PMID: 30267715
  9. Targeting mGlu Receptors for Optimization of Antipsychotic Activity and Disease-Modifying Effect in Schizophrenia.  |  Nicoletti, F., et al. 2019. Front Psychiatry. 10: 49. PMID: 30890967
  10. Reversal of MK-801-Induced Disruptions in Social Interactions and Working Memory with Simultaneous Administration of LY487379 and VU152100 in Mice.  |  Cieślik, P., et al. 2019. Int J Mol Sci. 20: PMID: 31174329
  11. Phenotypic assays in yeast and zebrafish reveal drugs that rescue ATP13A2 deficiency.  |  Heins-Marroquin, U., et al. 2019. Brain Commun. 1: fcz019. PMID: 32954262
  12. Serotonergic-Muscarinic Interaction within the Prefrontal Cortex as a Novel Target to Reverse Schizophrenia-Related Cognitive Symptoms.  |  Cieślik, P., et al. 2021. Int J Mol Sci. 22: PMID: 34445318
  13. Behavioral features and disorganization of oscillatory activity in C57BL/6J mice after acute low dose MK-801 administration.  |  Cui, K., et al. 2022. Front Neurosci. 16: 1001869. PMID: 36188453

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

VU 152100, 5 mg

sc-311554
5 mg
$98.00

VU 152100, 25 mg

sc-311554A
25 mg
$384.00