Sabeluzole

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

MedKoo CAT#: 326887

CAS#: 104383-17-7

Description: Sabeluzole, also known as R-58735, is a nootropic and neuroprotective drug which was originally developed for the treatment of Alzheimer's disease, and has subsequently been researched for other applications such as sleep apnoea. It acts primarily as an NMDA antagonist, but other mechanisms of action may also be important. .


Price and Availability

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Sabeluzole is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 326887
Name: Sabeluzole
CAS#: 104383-17-7
Chemical Formula: C22H26FN3O2S
Exact Mass: 415.173
Molecular Weight: 415.5274
Elemental Analysis: C, 63.59; H, 6.31; F, 4.57; N, 10.11; O, 7.70; S, 7.72


Synonym: R-58735; R58735; R 58735; Sabeluzole

IUPAC/Chemical Name: 1-(4-((benzo[d]thiazol-2-ylmethyl)amino)piperidin-1-yl)-3-(4-fluorophenoxy)propan-2-ol

SMILES Code: OC(COC1=CC=C(F)C=C1)CN2CCC(NCC3=NC4=CC=CC=C4S3)CC2


Technical Data

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).

Harmonized System Code:
293490


References

1: Verreck G, Chun I, Li Y, Kataria R, Zhang Q, Rosenblatt J, Decorte A, Heymans K, Adriaensen J, Bruining M, Van Remoortere M, Borghys H, Meert T, Peeters J, Brewster ME. Preparation and physicochemical characterization of biodegradable nerve guides containing the nerve growth agent sabeluzole. Biomaterials. 2005 Apr;26(11):1307-15. PubMed PMID: 15475061.

2: Pageaux GP, Micallef J, Nataf MB, Levron JC, Lacarelle B, Le Moing JP, Bouhours P, Blin O. Pharmacokinetics of sabeluzole and dextromethorphan oxidation capacity in patients with severe hepatic dysfunction and healthy volunteers. Br J Clin Pharmacol. 2001 Feb;51(2):164-8. PubMed PMID: 11259989; PubMed Central PMCID: PMC2014438.

3: Mohr E, Nair NP, Sampson M, Murtha S, Belanger G, Pappas B, Mendis T. Treatment of Alzheimer's disease with sabeluzole: functional and structural correlates. Clin Neuropharmacol. 1997 Aug;20(4):338-45. PubMed PMID: 9260731.

4: Uberti D, Rizzini C, Galli P, Pizzi M, Grilli M, Lesage A, Spano P, Memo M. Priming of cultured neurons with sabeluzole results in long-lasting inhibition of neurotoxin-induced tau expression and cell death. Synapse. 1997 Jun;26(2):95-103. PubMed PMID: 9131769.

5: Geerts H, Nuydens R, De Jong M, Cornelissen F, Nuyens R, Wouters L. Sabeluzole stabilizes the neuronal cytoskeleton. Neurobiol Aging. 1996 Jul-Aug;17(4):573-81. PubMed PMID: 8832632.

6: Domány G, Barta-Szalai G, Matúz J, Ezer E, Schön I. Analogues of sabeluzole with gastric acid secretion inhibitory effect. Pharmazie. 1996 Jun;51(6):427-8. PubMed PMID: 8767854.

7: Hedner J, Grunstein R, Eriksson B, Ejnell H. A double-blind, randomized trial of sabeluzole--a putative glutamate antagonist--in obstructive sleep apnea. Sleep. 1996 May;19(4):287-9. PubMed PMID: 8776785.

8: Aldenkamp AP, Overweg J, Smakman J, Beun AM, Diepman L, Edelbroek P, Gutter T, Mulder OG, vt Slot B, Vledder B. Effect of sabeluzole (R 58,735) on memory functions in patients with epilepsy. Neuropsychobiology. 1995;32(1):37-44. PubMed PMID: 7566521.

9: Zgur T, Vodusek DB, Krzan M, Vrtovec M. Efficiency of the antihypoxic substance sabeluzole in patients with clinically and neurophysiologically evident diabetic polyneuropathy. Acta Neurol Scand. 1993 Nov;88(5):381. PubMed PMID: 8296540.

10: Li JY, Dahlström AB. Sabeluzole administration does not enhance fast axonal transport in normal adult rat sciatic nerve. Pharmacol Toxicol. 1993 Jun;72(6):383-7. PubMed PMID: 7689730.

11: Hlinák Z, Krejcí I. [Sabeluzole and flunarizine in memory processes: animal studies]. Cesk Psychiatr. 1993 Apr;89(2):91-3. Czech. PubMed PMID: 8403029.

12: Vondrácková D. [EMG findings in patients with diabetic polyneuropathy treated with sabeluzole]. Cesk Psychiatr. 1993 Apr;89(2):87-90. Czech. PubMed PMID: 8403028.

13: Van der Valk JB, Vijverberg HP. Chronic sabeluzole treatment of cultured rat cerebellar granule cells reduces N-methyl-D-aspartate-induced inward current. Eur J Pharmacol. 1993 Feb 23;232(1):131-4. PubMed PMID: 8458392.

14: Krejcí I, Hlinák Z, Schuh J. [Flunarizine and sabeluzole improves behavior disorders caused by cold-induced cortical lesions in mice]. Cesk Psychiatr. 1993 Jan;89(1):39-41. Czech. PubMed PMID: 8508463.

15: Krejcová H, Vondrácková D, Egerová Y, Cerný R. [Treatment of polyneuropathy using sabeluzole]. Cesk Psychiatr. 1993 Jan;89(1):35-8. Czech. PubMed PMID: 8508462.

16: Pauwels PJ, Van Assouw HP, Peeters L, Moeremans M, Leysen JE. Chronic treatment with sabeluzole protects cultured rat brain neurons from the neurotoxic effects of excitatory amino acids. Synapse. 1992 Dec;12(4):271-80. PubMed PMID: 1361247.

17: Hendriksen PH, Oey PL, Wieneke GH, Banga JD, van Dam PS. Antihypoxic treatment at an early stage of diabetic neuropathy: an electrophysiological study with sabeluzole. Acta Neurol Scand. 1992 Nov;86(5):506-11. PubMed PMID: 1336292.

18: Geerts H, Nuydens R, Nuyens R, Cornelissen F, De Brabander M, Pauwels P, Janssen PA, Song YH, Mandelkow EM. Sabeluzole, a memory-enhancing molecule, increases fast axonal transport in neuronal cell cultures. Exp Neurol. 1992 Jul;117(1):36-43. PubMed PMID: 1377635.

19: Geerts H, Nuydens R, Nuyens R, Cornelissen F. Sabeluzole accelerates neurite outgrowth in different neuronal cell lines. Restor Neurol Neurosci. 1992 Jan 1;4(1):21-32. doi: 10.3233/RNN-1992-4103. PubMed PMID: 21551650.

20: De Deyn PP, Van de Velde V, Verslegers W, Saerens J, Pickut BA, Clincke B, Woestenborghs R, Van Peer A. Single-dose and steady-state pharmacokinetics of sabeluzole in senile dementia of Alzheimer type patients. Eur J Clin Pharmacol. 1992;43(6):661-2. PubMed PMID: 1493851.