Nisoxetine

Orders received during 11/25~11/29 will be shipped in 11/30/2020 due to Thanksgiving holiday.

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

MedKoo CAT#: 584876

CAS#: 53179-07-0

Description: Nisoxetine is a potent inhibitor for norepinephrine uptake into rat brain synaptosomes and brain.


Price and Availability

Size Price Shipping out time Quantity
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Pricing updated 2020-11-25. Prices are subject to change without notice.

Nisoxetine 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#: 584876
Name: Nisoxetine
CAS#: 53179-07-0
Chemical Formula: C17H21NO2
Exact Mass: 271.1572
Molecular Weight: 271.36
Elemental Analysis: C, 75.25; H, 7.80; N, 5.16; O, 11.79


Synonym: Nisoxetine

IUPAC/Chemical Name: Benzenepropanamine, gamma-(2-methoxyphenoxy)-N-methyl-

InChi Key: ITJNARMNRKSWTA-UHFFFAOYSA-N

InChi Code: InChI=1S/C17H21NO2/c1-18-13-12-15(14-8-4-3-5-9-14)20-17-11-7-6-10-16(17)19-2/h3-11,15,18H,12-13H2,1-2H3

SMILES Code: CNCCC(OC1=CC=CC=C1OC)C2=CC=CC=C2


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:
>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


References

1: Leung YM, Chu CC, Kuo CS, Chen YW, Wang JJ. Nisoxetine blocks sodium currents and elicits spinal anesthesia in rats. Pharmacol Rep. 2013;65(2):350-7. PubMed PMID: 23744419.

2: Leung YM, Chu CC, Kuo CS, Chen YW, Hung CH, Wang JJ. Isobolographic analysis of interaction between nisoxetine- and mepivacaine-induced spinal blockades in rats. Fundam Clin Pharmacol. 2014 Feb;28(1):88-94. doi: 10.1111/j.1472-8206.2012.01070.x. Epub 2012 Aug 14. PubMed PMID: 22889000.

3: Tejani-Butt SM. [3H]nisoxetine: a radioligand for quantitation of norepinephrine uptake sites by autoradiography or by homogenate binding. J Pharmacol Exp Ther. 1992 Jan;260(1):427-36. PubMed PMID: 1731049.

4: Bello NT, Walters AL, Verpeut JL, Cunha PP. High-fat diet-induced alterations in the feeding suppression of low-dose nisoxetine, a selective norepinephrine reuptake inhibitor. J Obes. 2013;2013:457047. doi: 10.1155/2013/457047. Epub 2013 Jan 30. PubMed PMID: 23431425; PubMed Central PMCID: PMC3570928.

5: Bermingham DP, Hardaway JA, Snarrenberg CL, Robinson SB, Folkes OM, Salimando GJ, Jinnah H, Blakely RD. Acute blockade of the Caenorhabditis elegans dopamine transporter DAT-1 by the mammalian norepinephrine transporter inhibitor nisoxetine reveals the influence of genetic modifications of dopamine signaling in vivo. Neurochem Int. 2016 Sep;98:122-8. doi: 10.1016/j.neuint.2016.01.008. Epub 2016 Feb 3. PubMed PMID: 26850478; PubMed Central PMCID: PMC4969213.

6: Cheetham SC, Viggers JA, Butler SA, Prow MR, Heal DJ. [3H]nisoxetine--a radioligand for noradrenaline reuptake sites: correlation with inhibition of [3H]noradrenaline uptake and effect of DSP-4 lesioning and antidepressant treatments. Neuropharmacology. 1996 Jan;35(1):63-70. PubMed PMID: 8684598.

7: Chen YW, Chu CC, Chen YC, Wang JJ, Hung CH, Shao DZ. Nisoxetine produces local but not systemic analgesia against cutaneous nociceptive stimuli in the rat. Eur J Pharmacol. 2012 Jan 30;675(1-3):22-5. doi: 10.1016/j.ejphar.2011.11.042. Epub 2011 Dec 7. PubMed PMID: 22166377.

8: Penmatsa A, Wang KH, Gouaux E. X-ray structures of Drosophila dopamine transporter in complex with nisoxetine and reboxetine. Nat Struct Mol Biol. 2015 Jun;22(6):506-508. doi: 10.1038/nsmb.3029. Epub 2015 May 11. PubMed PMID: 25961798; PubMed Central PMCID: PMC4608549.

9: Tejani-Butt SM, Ordway GA. Effect of age on [3H]nisoxetine binding to uptake sites for norepinephrine in the locus coeruleus of humans. Brain Res. 1992 Jun 26;583(1-2):312-5. PubMed PMID: 1504838.

10: Snoddy AM, Tessel RE. Nisoxetine and amphetamine share discriminative stimulus properties in mice. Pharmacol Biochem Behav. 1983 Aug;19(2):205-10. PubMed PMID: 6605539.

11: Bello NT, Yeh CY, Verpeut JL, Walters AL. Binge-like eating attenuates nisoxetine feeding suppression, stress activation, and brain norepinephrine activity. PLoS One. 2014 Apr 2;9(4):e93610. doi: 10.1371/journal.pone.0093610. eCollection 2014. PubMed PMID: 24695494; PubMed Central PMCID: PMC3973562.

12: Tejani-Butt SM, Brunswick DJ, Frazer A. [3H]nisoxetine: a new radioligand for norepinephrine uptake sites in brain. Eur J Pharmacol. 1990 Nov 27;191(2):239-43. PubMed PMID: 2086242.

13: Shearman LP, Meyer JS. Norepinephrine transporters in rat placenta labeled with [3H]nisoxetine. J Pharmacol Exp Ther. 1998 Feb;284(2):736-43. PubMed PMID: 9454822.

14: Gehlert DR, Schober DA, Gackenheimer SL. Comparison of (R)-[3H]tomoxetine and (R/S)-[3H]nisoxetine binding in rat brain. J Neurochem. 1995 Jun;64(6):2792-800. PubMed PMID: 7760060.

15: Shang Y, Dluzen DE. Nisoxetine infusion into the olfactory bulb enhances the capacity for male rats to identify conspecifics. Neuroscience. 2001;104(4):957-64. PubMed PMID: 11457583.

16: Zhen J, Ali S, Dutta AK, Reith ME. Characterization of [³H]CFT binding to the norepinephrine transporter suggests that binding of CFT and nisoxetine is not mutually exclusive. J Neurosci Methods. 2012 Jan 15;203(1):19-27. doi: 10.1016/j.jneumeth.2011.08.044. Epub 2011 Sep 12. PubMed PMID: 21933682; PubMed Central PMCID: PMC3221803.

17: Borbély Z, Csomó BK, Kittel Á, Gerber G, Varga G, Vizi ES. Effect of rat spinal cord injury (hemisection) on the ex vivo uptake and release of [(3)H]noradrenaline from a slice preparation. Brain Res Bull. 2017 May;131:150-155. doi: 10.1016/j.brainresbull.2017.04.007. Epub 2017 Apr 20. PubMed PMID: 28434993.

18: Kung MP, Choi SR, Hou C, Zhuang ZP, Foulon C, Kung HF. Selective binding of 2-[125I]iodo-nisoxetine to norepinephrine transporters in the brain. Nucl Med Biol. 2004 Jul;31(5):533-41. PubMed PMID: 15219270.

19: Arime Y, Kasahara Y, Hall FS, Uhl GR, Sora I. Cortico-subcortical neuromodulation involved in the amelioration of prepulse inhibition deficits in dopamine transporter knockout mice. Neuropsychopharmacology. 2012 Oct;37(11):2522-30. doi: 10.1038/npp.2012.114. Epub 2012 Jul 11. PubMed PMID: 22781838; PubMed Central PMCID: PMC3442347.

20: Lemberger L, Terman S, Rowe H, Billings R. The effect of nisoxetine (Lilly compound 94939), a potential antidepressant, on biogenic amine uptake in man. Br J Clin Pharmacol. 1976 Apr;3(2):215-20. PubMed PMID: 788744; PubMed Central PMCID: PMC1428886.