Synonym
ARL-15896AR; AZD-6765 dihydrochloride; FPL-15896AR; Lanicemine dihydrochloride; Lanicemine 2HCl
IUPAC/Chemical Name
2-Pyridineethanamine, alpha-phenyl-, (alphaS)-, dihydrochloride
InChi Key
KHJHFYAGQZYCLC-GXKRWWSZSA-N
InChi Code
InChI=1S/C13H14N2.2ClH/c14-13(11-6-2-1-3-7-11)10-12-8-4-5-9-15-12;;/h1-9,13H,10,14H2;2*1H/t13-;;/m0../s1
SMILES Code
Cl.Cl.N[C@@H](Cc1ccccn1)c2ccccc2
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
>3 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
Biological target:
Lanicemine (AZD6765) dihydrochloride 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 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 |
| DMSO |
240.0 |
885.00 |
| Water |
100.0 |
368.75 |
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
271.19
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 vivo 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.
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.
