WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 530354
CAS#: 409351-28-6
Description: 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.
MedKoo Cat#: 530354
Name: VU0152100
CAS#: 409351-28-6
Chemical Formula: C18H19N3O2S
Exact Mass: 341.1198
Molecular Weight: 341.429
Elemental Analysis: C, 63.32; H, 5.61; N, 12.31; O, 9.37; S, 9.39
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
The following data is based on the product molecular weight 341.429 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: 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. PubMed PMID: 24442096; PubMed Central PMCID: PMC4023154.
2: Dencker D, Weikop P, Sørensen G, Woldbye DP, Wörtwein G, Wess J, Fink-Jensen A. An allosteric enhancer of M₄ muscarinic acetylcholine receptor function inhibits behavioral and neurochemical effects of cocaine. Psychopharmacology (Berl). 2012 Nov;224(2):277-87. doi: 10.1007/s00213-012-2751-8. PubMed PMID: 22648127; PubMed Central PMCID: PMC3914671.
3: 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. PubMed PMID: 24480931.
4: 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. PubMed PMID: 26520141; PubMed Central PMCID: PMC4698283.
5: Brady AE, 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. doi: 10.1124/jpet.108.140350. PubMed PMID: 18772318; PubMed Central PMCID: PMC2745822.
6: Huynh T, Valant C, Crosby IT, Sexton PM, Christopoulos A, Capuano B. Probing structural requirements of positive allosteric modulators of the M4 muscarinic receptor. J Med Chem. 2013 Oct 24;56(20):8196-200. doi: 10.1021/jm401032k. PubMed PMID: 24074052.
7: 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. PubMed PMID: 26277342; PubMed Central PMCID: PMC4655164.
8: 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. PubMed PMID: 27060412; PubMed Central PMCID: PMC5055431.
9: 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. PubMed PMID: 26153447; PubMed Central PMCID: PMC4545715.
10: 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. PubMed PMID: 25137629; PubMed Central PMCID: PMC4324418.
11: 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. PubMed PMID: 24528004; PubMed Central PMCID: PMC3990947.
