Lanicemine |CAS#153322-05-5 |CAS#153322-06-6 |NMDA receptor antagonist

MedKoo Cat#: 525425 | Name: Lanicemine (free base)

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Description:

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

Lanicemine (free base) is a low-trapping NMDA receptor antagonist. Lanicemine is used the management of severe and treatment-resistant depression. Lanicemine was originally developed as a neuroprotective agent, but was redeveloped as an antidepressant.

Chemical Structure

Lanicemine (free base)

CAS#153322-05-5

Theoretical Analysis

MedKoo Cat#: 525425

Name: Lanicemine (free base)

CAS#: 153322-05-5

Chemical Formula: C13H14N2

Exact Mass: 198.1157

Molecular Weight: 198.27

Elemental Analysis: C, 78.75; H, 7.12; N, 14.13

Price and Availability

Size	Price	Availability
10mg	USD 300.00	2 Weeks
25mg	USD 550.00	2 Weeks
50mg	USD 810.00

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Related CAS #

No Data

Synonym

Lanicemine(free base); Lanicemine(2HCl) ARL-15896; ARL-15896AR; ARR-15896; ARR-15896AR; FPL-15896; FPL-15896AR ARL15896; ARL15896AR; ARR15896; ARR15896AR; FPL15896; FPL15896AR ARL 15896; ARL 15896AR; ARR 15896; ARR 15896AR; FPL 15896; FPL 15896AR

IUPAC/Chemical Name

(S)-1-phenyl-2-(pyridin-2-yl)ethanamine

InChi Key

FWUQWDCOOWEXRY-ZDUSSCGKSA-N

InChi Code

InChI=1S/C13H14N2/c14-13(11-6-2-1-3-7-11)10-12-8-4-5-9-15-12/h1-9,13H,10,14H2/t13-/m0/s1

SMILES Code

N[C@H](c1ccccc1)Cc2ncccc2

Appearance

Liquid

Purity

>95% (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

Related CAS# 153322-05-5(Lanicemine free base) 153322-06-6(Lanicemine dihydrochloride)

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#C9M07C19

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

Lanicemine (AZD6765) is a low-trapping NMDA channel blocker (Ki of 0.56-2.1 μM for NMDA receptor; IC50s of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively).

In vitro activity:

TBD

In vivo activity:

A single administration of AZD6765 (1 mg/kg, i.p.) was able to induce an antidepressant-like effect in mice submitted to tail suspension test (TST), an effect reversed by LY294002 (a reversible PI3K inhibitor, 10 nmol/site, i.c.v.), wortmannin (an irreversible PI3K inhibitor, 0.1 μg/site, i.c.v.) and rapamycin (a selective mTOR inhibitor, 0.2 nmol/site, i.c.v.). Reference: Pharmacol Biochem Behav. 2020 Nov;198:173020. https://pubmed.ncbi.nlm.nih.gov/32861641/

	Solvent	mg/mL	mM
Solubility
	DMF	5.0	25.22
	DMSO	30.0	151.31
	Ethanol	20.0	100.87
	PBS (pH 7.2)	3.0	15.13

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 198.27 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

Formulation protocol:

1. Neis VB, Moretti M, Rosa PB, Dalsenter YO, Werle I, Platt N, Kaufmann FN, Rosado AF, Besen MH, Rodrigues ALS. The involvement of PI3K/Akt/mTOR/GSK3β signaling pathways in the antidepressant-like effect of AZD6765. Pharmacol Biochem Behav. 2020 Nov;198:173020. doi: 10.1016/j.pbb.2020.173020. Epub 2020 Aug 28. PMID: 32861641.

In vitro protocol:

TBD

In vivo protocol:

1: Wallach J, Kang H, Colestock T, Morris H, Bortolotto ZA, Collingridge GL, Lodge D, Halberstadt AL, Brandt SD, Adejare A. Pharmacological Investigations of the Dissociative 'Legal Highs' Diphenidine, Methoxphenidine and Analogues. PLoS One. 2016 Jun 17;11(6):e0157021. doi: 10.1371/journal.pone.0157021. eCollection 2016. PubMed PMID: 27314670; PubMed Central PMCID: PMC4912077. 2: Downey D, Dutta A, McKie S, Dawson GR, Dourish CT, Craig K, Smith MA, McCarthy DJ, Harmer CJ, Goodwin GM, Williams S, Deakin JF. Comparing the actions of lanicemine and ketamine in depression: key role of the anterior cingulate. Eur Neuropsychopharmacol. 2016 Jun;26(6):994-1003. doi: 10.1016/j.euroneuro.2016.03.006. Epub 2016 Apr 28. PubMed PMID: 27133029. 3: Keavy D, Bristow LJ, Sivarao DV, Batchelder M, King D, Thangathirupathy S, Macor JE, Weed MR. The qEEG Signature of Selective NMDA NR2B Negative Allosteric Modulators; A Potential Translational Biomarker for Drug Development. PLoS One. 2016 Apr 1;11(4):e0152729. doi: 10.1371/journal.pone.0152729. eCollection 2016. PubMed PMID: 27035340; PubMed Central PMCID: PMC4817977. 4: Cooper MD, Rosenblat JD, Cha DS, Lee Y, Kakar R, McIntyre RS. Strategies to mitigate dissociative and psychotomimetic effects of ketamine in the treatment of major depressive episodes: a narrative review. World J Biol Psychiatry. 2016 Mar 16:1-14. [Epub ahead of print] PubMed PMID: 26752601. 5: Fernandes A, Wojcik T, Baireddy P, Pieschl R, Newton A, Tian Y, Hong Y, Bristow L, Li YW. Inhibition of in vivo [(3)H]MK-801 binding by NMDA receptor open channel blockers and GluN2B antagonists in rats and mice. Eur J Pharmacol. 2015 Nov 5;766:1-8. doi: 10.1016/j.ejphar.2015.08.044. Epub 2015 Aug 29. PubMed PMID: 26325093. 6: Rajkumar R, Fam J, Yeo EY, Dawe GS. Ketamine and suicidal ideation in depression: Jumping the gun? Pharmacol Res. 2015 Sep;99:23-35. doi: 10.1016/j.phrs.2015.05.003. Epub 2015 May 15. Review. PubMed PMID: 25982932. 7: Bui KH, Zhou D, Agbo F, Guo J. Effect of multiple intravenous doses of lanicemine (AZD6765) on the pharmacokinetics of midazolam in healthy subjects. J Clin Pharmacol. 2015 Sep;55(9):1024-30. doi: 10.1002/jcph.515. Epub 2015 Jun 2. PubMed PMID: 25880724. 8: Skolnick P, Kos T, Czekaj J, Popik P. Effect of NMDAR antagonists in the tetrabenazine test for antidepressants: comparison with the tail suspension test. Acta Neuropsychiatr. 2015 Aug;27(4):228-34. doi: 10.1017/neu.2015.14. Epub 2015 Apr 10. PubMed PMID: 25858023. 9: Solé B, Jiménez E, Martinez-Aran A, Vieta E. Cognition as a target in major depression: new developments. Eur Neuropsychopharmacol. 2015 Feb;25(2):231-47. doi: 10.1016/j.euroneuro.2014.12.004. Epub 2015 Jan 19. Review. PubMed PMID: 25640673. 10: Guo J, Zhou D, Grimm SW, Bui KH. Pharmacokinetics, metabolism and excretion of [(14)C]-lanicemine (AZD6765), a novel low-trapping N-methyl-d-aspartic acid receptor channel blocker, in healthy subjects. Xenobiotica. 2015 Mar;45(3):244-55. doi: 10.3109/00498254.2014.966175. Epub 2014 Sep 26. PubMed PMID: 25259653. 11: Sanacora G, Smith MA, Pathak S, Su HL, Boeijinga PH, McCarthy DJ, Quirk MC. Lanicemine: a low-trapping NMDA channel blocker produces sustained antidepressant efficacy with minimal psychotomimetic adverse effects. Mol Psychiatry. 2014 Sep;19(9):978-85. doi: 10.1038/mp.2013.130. Epub 2013 Oct 15. PubMed PMID: 24126931; PubMed Central PMCID: PMC4195977. 12: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jan-Feb;25(1):53-76. PubMed PMID: 12690708.