VU0152100 | CAS# 409351-28-6 | M4-PAM

MedKoo Cat#: 530354 | Name: VU0152100

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

VU0152100 is a highly selective M4 positive allosteric modulator (PAM) that exerts central effects after systemic administration. VU0152100 dose-dependently reverses amphetamine-induced hyperlocomotion in rats and wild-type mice, but not in M4 KO mice. VU0152100 also blocks amphetamine-induced disruption of the acquisition of contextual fear conditioning and prepulse inhibition of the acoustic startle reflex.

Chemical Structure

VU0152100

CAS#409351-28-6

Theoretical Analysis

MedKoo Cat#: 530354

Name: VU0152100

CAS#: 409351-28-6

Chemical Formula: C18H19N3O2S

Exact Mass: 341.1198

Molecular Weight: 341.43

Elemental Analysis: C, 63.32; H, 5.61; N, 12.31; O, 9.37; S, 9.39

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 450.00

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Synonym

VU0152100, VU-0152100, VU 0152100, VU152100, VU 152100, VU-152100

IUPAC/Chemical Name

3-amino-N-(4-methoxybenzyl)-4,6-dimethylthieno(2,3-b)pyridine-2-carboxamide

InChi Key

MDNWGCQSCGNTKH-UHFFFAOYSA-N

InChi Code

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)

SMILES Code

O=C(C1=C(N)C2=C(C)C=C(C)N=C2S1)NCC3=CC=C(OC)C=C3

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 341.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Balakrishnan AS, Johansen LBE, Lindsley CW, Conn PJ, Thomsen M. Co- stimulation of muscarinic M1 and M4 acetylcholine receptors prevents later cocaine reinforcement in male and female mice, but not place-conditioning. Prog Neuropsychopharmacol Biol Psychiatry. 2024 Aug 30;134:111079. doi: 10.1016/j.pnpbp.2024.111079. Epub 2024 Jun 29. PMID: 38950842; PMCID: PMC11578924. 2: Cieślik P, Rafało-Ulińska A, Wierońska JM. Prevention of MK-801-induced amnestic effect with combined activation of 5-HT1A and muscarinic receptors in mice. Pharmacol Biochem Behav. 2024 May;238:173749. doi: 10.1016/j.pbb.2024.173749. Epub 2024 Mar 9. PMID: 38462045. 3: Wierońska JM, Cieślik P, Burnat G, Kalinowski L. Activation of Metabotropic Glutamate Receptor (mGlu2) and Muscarinic Receptors (M1, M4, and M5), Alone or in Combination, and Its Impact on the Acquisition and Retention of Learning in the Morris Water Maze, NMDA Expression and cGMP Synthesis. Biomolecules. 2023 Jun 30;13(7):1064. doi: 10.3390/biom13071064. PMID: 37509100; PMCID: PMC10377483. 4: Thomsen M, Crittenden JR, Lindsley CW, Graybiel AM. Effects of acute and repeated administration of the selective M4 PAM VU0152099 on cocaine versus food choice in male rats. Addict Biol. 2022 Mar;27(2):e13145. doi: 10.1111/adb.13145. PMID: 35229940; PMCID: PMC9162150. 5: Cieślik P, Radulska A, Burnat G, Kalinowski L, Wierońska JM. Serotonergic- Muscarinic Interaction within the Prefrontal Cortex as a Novel Target to Reverse Schizophrenia-Related Cognitive Symptoms. Int J Mol Sci. 2021 Aug 10;22(16):8612. doi: 10.3390/ijms22168612. PMID: 34445318; PMCID: PMC8395335. 6: Brugnoli A, Pisanò CA, Morari M. Striatal and nigral muscarinic type 1 and type 4 receptors modulate levodopa-induced dyskinesia and striato-nigral pathway activation in 6-hydroxydopamine hemilesioned rats. Neurobiol Dis. 2020 Oct;144:105044. doi: 10.1016/j.nbd.2020.105044. Epub 2020 Aug 13. PMID: 32798726. 7: Nair AG, Castro LRV, El Khoury M, Gorgievski V, Giros B, Tzavara ET, Hellgren-Kotaleski J, Vincent P. The high efficacy of muscarinic M4 receptor in D1 medium spiny neurons reverses striatal hyperdopaminergia. Neuropharmacology. 2019 Mar 1;146:74-83. doi: 10.1016/j.neuropharm.2018.11.029. Epub 2018 Nov 22. PMID: 30468798. 8: Cieślik P, Woźniak M, Tokarski K, Kusek M, Pilc A, Płoska A, Radulska A, Pelikant-Małecka I, Żołnowska B, Sławiński J, Kalinowski L, Wierońska JM. Simultaneous activation of muscarinic and GABAB receptors as a bidirectional target for novel antipsychotics. Behav Brain Res. 2019 Feb 1;359:671-685. doi: 10.1016/j.bbr.2018.09.019. Epub 2018 Sep 26. PMID: 30267715. 9: Stoll K, Hart R, Lindsley CW, Thomsen M. Effects of muscarinic M1 and M4 acetylcholine receptor stimulation on extinction and reinstatement of cocaine seeking in male mice, independent of extinction learning. Psychopharmacology (Berl). 2018 Mar;235(3):815-827. doi: 10.1007/s00213-017-4797-0. Epub 2017 Dec 18. PMID: 29250738; PMCID: PMC6472894. 10: Xue B, Mao LM, Jin DZ, Wang JQ. Pharmacological modulation of AMPA receptor phosphorylation by dopamine and muscarinic receptor agents in the rat medial prefrontal cortex. Eur J Pharmacol. 2018 Feb 5;820:45-52. doi: 10.1016/j.ejphar.2017.12.022. Epub 2017 Dec 11. PMID: 29242119; PMCID: PMC5767128. 11: Hamann M, Plank J, Richter F, Bode C, Smiljanic S, Creed M, Nobrega JN, Richter A. Alterations of M1 and M4 acetylcholine receptors in the genetically dystonic (dtsz) hamster and moderate antidystonic efficacy of M1 and M4 anticholinergics. Neuroscience. 2017 Aug 15;357:84-98. doi: 10.1016/j.neuroscience.2017.05.051. Epub 2017 Jun 9. PMID: 28596119. 12: Dall C, Weikop P, Dencker D, Molander AC, Wörtwein G, Conn PJ, Fink-Jensen A, Thomsen M. Muscarinic receptor M4 positive allosteric modulators attenuate central effects of cocaine. Drug Alcohol Depend. 2017 Jul 1;176:154-161. doi: 10.1016/j.drugalcdep.2017.03.014. Epub 2017 May 16. PMID: 28544993; PMCID: PMC6423356. 13: Xue B, Chen EC, He N, Jin DZ, Mao LM, Wang JQ. Integrated regulation of AMPA glutamate receptor phosphorylation in the striatum by dopamine and acetylcholine. Neuropharmacology. 2017 Jan;112(Pt A):57-65. doi: 10.1016/j.neuropharm.2016.04.005. Epub 2016 Apr 7. PMID: 27060412; PMCID: PMC5055431. 14: Jørgensen KB, Krogh-Jensen K, Pickering DS, Kanui TI, Abelson KS. 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. 2016 Jan;202(1):7-15. doi: 10.1007/s00359-015-1048-x. Epub 2015 Oct 31. PMID: 26520141; PMCID: PMC4698283. 15: Mao LM, Wang JQ. Dopaminergic and cholinergic regulation of Fyn tyrosine kinase phosphorylation in the rat striatum in vivo. Neuropharmacology. 2015 Dec;99:491-9. doi: 10.1016/j.neuropharm.2015.08.017. Epub 2015 Aug 13. PMID: 26277342; PMCID: PMC4655164. 16: Xue B, Mao LM, Jin DZ, Wang JQ. Regulation of synaptic MAPK/ERK phosphorylation in the rat striatum and medial prefrontal cortex by dopamine and muscarinic acetylcholine receptors. J Neurosci Res. 2015 Oct;93(10):1592-9. doi: 10.1002/jnr.23622. Epub 2015 Jul 8. PMID: 26153447; PMCID: PMC4545715. 17: Bubser M, Bridges TM, Dencker D, Gould RW, Grannan M, Noetzel MJ, Lamsal A, Niswender CM, Daniels JS, Poslusney MS, Melancon BJ, Tarr JC, Byers FW, Wess J, Duggan ME, Dunlop J, Wood MW, Brandon NJ, Wood MR, Lindsley CW, Conn PJ, Jones CK. Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents. ACS Chem Neurosci. 2014 Oct 15;5(10):920-42. doi: 10.1021/cn500128b. Epub 2014 Aug 19. PMID: 25137629; PMCID: PMC4324418. 18: Pancani T, Bolarinwa C, Smith Y, Lindsley CW, Conn PJ, Xiang Z. M4 mAChR- mediated modulation of glutamatergic transmission at corticostriatal synapses. ACS Chem Neurosci. 2014 Apr 16;5(4):318-24. doi: 10.1021/cn500003z. Epub 2014 Feb 27. PMID: 24528004; PMCID: PMC3990947. 19: Galloway CR, Lebois EP, Shagarabi SL, Hernandez NA, Manns JR. Effects of selective activation of M1 and M4 muscarinic receptors on object recognition memory performance in rats. Pharmacology. 2014;93(1-2):57-64. doi: 10.1159/000357682. Epub 2014 Jan 25. PMID: 24480931. 20: Byun NE, Grannan M, Bubser M, Barry RL, Thompson A, Rosanelli J, Gowrishankar R, Kelm ND, Damon S, Bridges TM, Melancon BJ, Tarr JC, Brogan JT, Avison MJ, Deutch AY, Wess J, Wood MR, Lindsley CW, Gore JC, Conn PJ, Jones CK. Antipsychotic drug-like effects of the selective M4 muscarinic acetylcholine receptor positive allosteric modulator VU0152100. Neuropsychopharmacology. 2014 Jun;39(7):1578-93. doi: 10.1038/npp.2014.2. Epub 2014 Jan 20. PMID: 24442096; PMCID: PMC4023154.