BD1063 HCl
featured

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

MedKoo CAT#: 555158

CAS#: 206996-13-6 (HCl)

Description: BD1063 is a selective sigma receptor antagonist, with a reported binding affinity of Ki = 9 ± 1 nM for the sigma-1 receptor and more than 49 times selectivity over the sigma-2 receptor. Consistent with other reported sigma receptor antagonists, pretreating Swiss Webster mice with BD1063 significantly decreases the convulsivity and lethality of cocaine. In other animal studies, BD1063 blocks the effects of MDMA, and reduces alcohol intake in rodent models of alcoholism.


Price and Availability

Size
Price

10mg
USD 250
Size
Price

Size
Price

BD1063 HCl, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

img

Theoretical Analysis

MedKoo Cat#: 555158
Name: BD1063 HCl
CAS#: 206996-13-6 (HCl)
Chemical Formula: C13H20Cl4N2
Exact Mass:
Molecular Weight: 346.117
Elemental Analysis: C, 45.11; H, 5.82; Cl, 40.97; N, 8.09


Synonym: 206996-13-6 (HCl), 150208-28-9 (free base),

IUPAC/Chemical Name: 1-[2-(3,4-dichlorophenyl)ethyl]-4-methyl-piperazine, dihydrochloride

InChi Key: NXFDBTLQOARIMH-UHFFFAOYSA-N

InChi Code: InChI=1S/C13H18Cl2N2.2ClH/c1-16-6-8-17(9-7-16)5-4-11-2-3-12(14)13(15)10-11;;/h2-3,10H,4-9H2,1H3;2*1H

SMILES Code: CN1CCN(CCC2=CC=C(Cl)C(Cl)=C2)CC1.[H]Cl.[H]Cl


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: Beggiato S, Borelli AC, Borroto-Escuela D, Corbucci I, Tomasini MC, Marti M, Antonelli T, Tanganelli S, Fuxe K, Ferraro L. Cocaine modulates allosteric D(2)-σ(1) receptor-receptor interactions on dopamine and glutamate nerve terminals from rat striatum. Cell Signal. 2017 Dec;40:116-124. doi: 10.1016/j.cellsig.2017.09.007. Epub 2017 Sep 18. PubMed PMID: 28923416.

2: Nguyen L, Scandinaro AL, Matsumoto RR. Deuterated (d6)-dextromethorphan elicits antidepressant-like effects in mice. Pharmacol Biochem Behav. 2017 Oct;161:30-37. doi: 10.1016/j.pbb.2017.09.005. Epub 2017 Sep 12. PubMed PMID: 28916283.

3: Meng B, Li H, Sun X, Qu W, Yang B, Cheng F, Shi L, Yuan H. σ-1 receptor stimulation protects against pressure-induced damage through InsR-MAPK signaling in human trabecular meshwork cells. Mol Med Rep. 2017 Jul;16(1):617-624. doi: 10.3892/mmr.2017.6647. Epub 2017 May 30. PubMed PMID: 28560459; PubMed Central PMCID: PMC5482118.

4: Gasparre G, Abate C, Carlucci R, Berardi F, Cassano G. The σ(1) receptor agonist (+)-pentazocine increases store-operated Ca(2+) entry in MCF7σ(1) and SK-N-SH cell lines. Pharmacol Rep. 2017 Jun;69(3):542-545. doi: 10.1016/j.pharep.2017.01.022. Epub 2017 Jan 28. PubMed PMID: 28364693.

5: Dalwadi DA, Kim S, Schetz JA. Activation of the sigma-1 receptor by haloperidol metabolites facilitates brain-derived neurotrophic factor secretion from human astroglia. Neurochem Int. 2017 May;105:21-31. doi: 10.1016/j.neuint.2017.02.003. Epub 2017 Feb 8. PubMed PMID: 28188803; PubMed Central PMCID: PMC5375023.

6: Wu Z, Li L, Zheng LT, Xu Z, Guo L, Zhen X. Allosteric modulation of sigma-1 receptors by SKF83959 inhibits microglia-mediated inflammation. J Neurochem. 2015 Sep;134(5):904-14. doi: 10.1111/jnc.13182. Epub 2015 Jun 19. PubMed PMID: 26031312.

7: Skuza G, Sadaj W, Kabziński M, Cassano G, Gasparre G, Abate C, Berardi F. The effects of new sigma (σ) receptor ligands, PB190 and PB212, in the models predictive of antidepressant activity. Pharmacol Rep. 2014 Apr;66(2):320-4. doi: 10.1016/j.pharep.2013.12.002. Epub 2014 Mar 4. PubMed PMID: 24911087.

8: Pan B, Guo Y, Kwok WM, Hogan Q, Wu HE. Sigma-1 receptor antagonism restores injury-induced decrease of voltage-gated Ca2+ current in sensory neurons. J Pharmacol Exp Ther. 2014 Aug;350(2):290-300. doi: 10.1124/jpet.114.214320. Epub 2014 Jun 2. PubMed PMID: 24891452; PubMed Central PMCID: PMC4109486.

9: Zhao J, Ha Y, Liou GI, Gonsalvez GB, Smith SB, Bollinger KE. Sigma receptor ligand, (+)-pentazocine, suppresses inflammatory responses of retinal microglia. Invest Ophthalmol Vis Sci. 2014 May 8;55(6):3375-84. doi: 10.1167/iovs.13-12823. PubMed PMID: 24812552; PubMed Central PMCID: PMC4042630.

10: Nguyen L, Robson MJ, Healy JR, Scandinaro AL, Matsumoto RR. Involvement of sigma-1 receptors in the antidepressant-like effects of dextromethorphan. PLoS One. 2014 Feb 28;9(2):e89985. doi: 10.1371/journal.pone.0089985. eCollection 2014. PubMed PMID: 24587167; PubMed Central PMCID: PMC3938562.

11: Sánchez-Blázquez P, Rodríguez-Muñoz M, Herrero-Labrador R, Burgueño J, Zamanillo D, Garzón J. The calcium-sensitive Sigma-1 receptor prevents cannabinoids from provoking glutamate NMDA receptor hypofunction: implications in antinociception and psychotic diseases. Int J Neuropsychopharmacol. 2014 Dec;17(12):1943-55. doi: 10.1017/S1461145714000029. Epub 2014 Jan 31. PubMed PMID: 24485144.

12: Kotagale NR, Shirbhate SH, Shukla P, Ugale RR. Agmatine attenuates neuropathic pain in sciatic nerve ligated rats: modulation by hippocampal sigma receptors. Eur J Pharmacol. 2013 Aug 15;714(1-3):424-31. doi: 10.1016/j.ejphar.2013.07.005. Epub 2013 Jul 16. PubMed PMID: 23872381.

13: Hiranita T, Mereu M, Soto PL, Tanda G, Katz JL. Self-administration of cocaine induces dopamine-independent self-administration of sigma agonists. Neuropsychopharmacology. 2013 Mar;38(4):605-15. doi: 10.1038/npp.2012.224. Epub 2012 Nov 28. PubMed PMID: 23187725; PubMed Central PMCID: PMC3572457.

14: Amer MS, McKeown L, Tumova S, Liu R, Seymour VA, Wilson LA, Naylor J, Greenhalgh K, Hou B, Majeed Y, Turner P, Sedo A, O'Regan DJ, Li J, Bon RS, Porter KE, Beech DJ. Inhibition of endothelial cell Ca²⁺ entry and transient receptor potential channels by Sigma-1 receptor ligands. Br J Pharmacol. 2013 Mar;168(6):1445-55. doi: 10.1111/bph.12041. PubMed PMID: 23121507; PubMed Central PMCID: PMC3596649.

15: Ito K, Hirooka Y, Matsukawa R, Nakano M, Sunagawa K. Decreased brain sigma-1 receptor contributes to the relationship between heart failure and depression. Cardiovasc Res. 2012 Jan 1;93(1):33-40. doi: 10.1093/cvr/cvr255. Epub 2011 Sep 29. PubMed PMID: 21960687.

16: Penas C, Pascual-Font A, Mancuso R, Forés J, Casas C, Navarro X. Sigma receptor agonist 2-(4-morpholinethyl)1 phenylcyclohexanecarboxylate (Pre084) increases GDNF and BiP expression and promotes neuroprotection after root avulsion injury. J Neurotrauma. 2011 May;28(5):831-40. doi: 10.1089/neu.2010.1674. Epub 2011 Apr 12. PubMed PMID: 21332255.

17: Herrera Y, Katnik C, Rodriguez JD, Hall AA, Willing A, Pennypacker KR, Cuevas J. sigma-1 receptor modulation of acid-sensing ion channel a (ASIC1a) and ASIC1a-induced Ca2+ influx in rat cortical neurons. J Pharmacol Exp Ther. 2008 Nov;327(2):491-502. doi: 10.1124/jpet.108.143974. Epub 2008 Aug 22. PubMed PMID: 18723775.

18: Liu Y, Matsumoto RR. Alterations in fos-related antigen 2 and sigma1 receptor gene and protein expression are associated with the development of cocaine-induced behavioral sensitization: time course and regional distribution studies. J Pharmacol Exp Ther. 2008 Oct;327(1):187-95. doi: 10.1124/jpet.108.141051. Epub 2008 Jun 30. PubMed PMID: 18591217.

19: Wu Z, Bowen WD. Role of sigma-1 receptor C-terminal segment in inositol 1,4,5-trisphosphate receptor activation: constitutive enhancement of calcium signaling in MCF-7 tumor cells. J Biol Chem. 2008 Oct 17;283(42):28198-215. doi: 10.1074/jbc.M802099200. Epub 2008 Jun 6. PubMed PMID: 18539593; PubMed Central PMCID: PMC2661391.

20: Schetz JA, Perez E, Liu R, Chen S, Lee I, Simpkins JW. A prototypical Sigma-1 receptor antagonist protects against brain ischemia. Brain Res. 2007 Nov 21;1181:1-9. Epub 2007 Sep 12. PubMed PMID: 17919467; PubMed Central PMCID: PMC4896215.