Idazoxan HCl |CAS#79944-56-2 |CAS#79944-58-4 | alpha2-adrenoceptor antagonist

MedKoo Cat#: 530009 | Name: Idazoxan HCl

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Description:

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

An alpha2-adrenoceptor antagonist potentially for the treatment of schizophrenia.

Chemical Structure

Idazoxan HCl

CAS#79944-56-2 (HCl)

Theoretical Analysis

MedKoo Cat#: 530009

Name: Idazoxan HCl

CAS#: 79944-56-2 (HCl)

Chemical Formula: C11H13ClN2O2

Exact Mass:

Molecular Weight: 240.69

Elemental Analysis: C, 54.89; H, 5.44; Cl, 14.73; N, 11.64; O, 13.29

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 300.00	2 Weeks
25mg	USD 550.00	2 Weeks

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Related CAS #

79944-56-2 (HCl) 79944-58-4 (free base)

Synonym

RX 781094A; RX-781094A; RX781094A; RX-781094; RX781094; RX 781094; Idazoxan HCl; Idazoxan hydrochloride;

IUPAC/Chemical Name

2-(2,3-dihydrobenzo[b][1,4]dioxin-2-yl)-4,5-dihydro-1H-imidazole hydrochloride

InChi Key

MYUBYOVCLMEAOH-UHFFFAOYSA-N

InChi Code

InChI=1S/C11H12N2O2.ClH/c1-2-4-9-8(3-1)14-7-10(15-9)11-12-5-6-13-11;/h1-4,10H,5-7H2,(H,12,13);1H

SMILES Code

[H]Cl.C1(C2OC3=CC=CC=C3OC2)=NCCN1

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).

HS Tariff Code

2934.99.9001

More Info

Related CAS# 79944-58-4(Idazoxan free base) 79944-56-2(Idazoxan HCl)

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Idazoxan hydrochloride (RX 781094 hydrochloride) is an α2-adrenoceptor antagonist and is also a imidazoline receptors (IRs) antagonist competitively antagonized the centrally induced hypotensive effect of imidazoline-like drugs (IMs). Idazoxan hydrochloride also improves motor symptoms in Parkinson’s disease, L-DOPA-induced dyskinesias, and experimental Parkinsonism.

In vitro activity:

The results showed that IDA (idazoxan) increased the expression of HO-1 and NQO-1, improved the enzyme activities of SOD and GPx, and inhibited the levels of p-Smad2, p-Smad3, α-SMA and Col1 in control shRNA group, while all these effects of IDA were abolished in Nrf2 shRNA group (Figure 6A–6D). Thus, this study concluded that IDA inhibited TGF-β/Smad signaling in LX2 cells via the activation of Nrf2 pathway. Reference: Oncotarget. 2017 Mar 28;8(13):21015-21030. https://pubmed.ncbi.nlm.nih.gov/28423499/

In vivo activity:

Results showed that only 50% of nicotine-withdrawing rats treated with idazoxan exhibited increased number of somatic signs compared to 100% of nicotine-withdrawing rats treated with saline, indicating attenuation of somatic aspects of nicotine withdrawal with idazoxan treatment (Fisher's exact test, p < 0.05). In both control groups, 25% of saline-“withdrawing” rats treated with either saline or idazoxan exhibited somatic signs. This pattern of results reflects partial efficacy of idazoxan treatment on the expression of somatic signs during nicotine withdrawal. Reference: Eur Neuropsychopharmacol. 2010 Oct;20(10):731-46. https://pubmed.ncbi.nlm.nih.gov/20627663/

	Solvent	mg/mL	mM
Solubility
	Water	62.0	257.74

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 240.69 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. Xuanfei L, Hao C, Zhujun Y, Yanming L, Jianping G. Imidazoline I2 receptor inhibitor idazoxan regulates the progression of hepatic fibrosis via Akt-Nrf2-Smad2/3 signaling pathway. Oncotarget. 2017 Mar 28;8(13):21015-21030. doi: 10.18632/oncotarget.15472. PMID: 28423499; PMCID: PMC5400562. 2. Semenova S, Markou A. The alpha2 adrenergic receptor antagonist idazoxan, but not the serotonin-2A receptor antagonist M100907, partially attenuated reward deficits associated with nicotine, but not amphetamine, withdrawal in rats. Eur Neuropsychopharmacol. 2010 Oct;20(10):731-46. doi: 10.1016/j.euroneuro.2010.05.003. Epub 2010 Jun 3. PMID: 20627663; PMCID: PMC3545706. 3. Buck K, Voehringer P, Ferger B. The alpha(2) adrenoceptor antagonist idazoxan alleviates L-DOPA-induced dyskinesia by reduction of striatal dopamine levels: an in vivo microdialysis study in 6-hydroxydopamine-lesioned rats. J Neurochem. 2010 Jan;112(2):444-52. doi: 10.1111/j.1471-4159.2009.06482.x. Epub 2009 Nov 6. PMID: 19895663.

In vitro protocol:

In vivo protocol:

1. Semenova S, Markou A. The alpha2 adrenergic receptor antagonist idazoxan, but not the serotonin-2A receptor antagonist M100907, partially attenuated reward deficits associated with nicotine, but not amphetamine, withdrawal in rats. Eur Neuropsychopharmacol. 2010 Oct;20(10):731-46. doi: 10.1016/j.euroneuro.2010.05.003. Epub 2010 Jun 3. PMID: 20627663; PMCID: PMC3545706. 2. Buck K, Voehringer P, Ferger B. The alpha(2) adrenoceptor antagonist idazoxan alleviates L-DOPA-induced dyskinesia by reduction of striatal dopamine levels: an in vivo microdialysis study in 6-hydroxydopamine-lesioned rats. J Neurochem. 2010 Jan;112(2):444-52. doi: 10.1111/j.1471-4159.2009.06482.x. Epub 2009 Nov 6. PMID: 19895663.

1: Haass-Koffler CL, Leggio L, Davidson D, Swift RM. Effects of idazoxan on alcohol pharmacokinetics and intoxication: a preliminary human laboratory study. Alcohol Clin Exp Res. 2015 Apr;39(4):594-602. doi: 10.1111/acer.12658. PubMed PMID: 25833022; PubMed Central PMCID: PMC4384190. 2: Gentile L, Arianna M, Roberta L, Franco M, Luca R. IMMOBILIZING THE VULNERABLE APENNINE CHAMOIS (RUPICAPRA PYRENAICA ORNATA) WITH A LOW-DOSE XYLAZINE-KETAMINE COMBINATION, REVERSED WITH IDAZOXAN OR ATIPAMEZOLE. J Zoo Wildl Med. 2015 Jun;46(2):213-23. doi: 10.1638/2014-0079R.1. PubMed PMID: 26056871. 3: Wang XS, Fang HL, Chen Y, Liang SS, Zhu ZG, Zeng QY, Li J, Xu HQ, Shao B, He JC, Hou ST, Zheng RY. Idazoxan reduces blood-brain barrier damage during experimental autoimmune encephalomyelitis in mouse. Eur J Pharmacol. 2014 Aug 5;736:70-6. doi: 10.1016/j.ejphar.2014.04.034. PubMed PMID: 24797785. 4: Rusu G, Mititelu-Tartau L, Lupusoru CE, Lupusoru RV, Grigoraş I, Popa G, Nechifor M. Imidazoline receptor antagonists idazoxan and efaroxan enhance locomotor functions in rats. Rev Med Chir Soc Med Nat Iasi. 2015 Jan-Mar;119(1):193-200. PubMed PMID: 25970966. 5: Khokhar JY, Chau DT, Dawson R, Green AI. Clozapine reconstructed: Haloperidol's ability to reduce alcohol intake in the Syrian golden hamster can be enhanced through noradrenergic modulation by desipramine and idazoxan. Drug Alcohol Depend. 2015 Jul 1;152:277-81. doi: 10.1016/j.drugalcdep.2015.04.003. PubMed PMID: 25979645; PubMed Central PMCID: PMC4458150. 6: Larrauri JA, Levin ED. The α₂-adrenergic antagonist idazoxan counteracts prepulse inhibition deficits caused by amphetamine or dizocilpine in rats. Psychopharmacology (Berl). 2012 Jan;219(1):99-108. doi: 10.1007/s00213-011-2377-2. PubMed PMID: 21710169. 7: Buck K, Voehringer P, Ferger B. The alpha(2) adrenoceptor antagonist idazoxan alleviates L-DOPA-induced dyskinesia by reduction of striatal dopamine levels: an in vivo microdialysis study in 6-hydroxydopamine-lesioned rats. J Neurochem. 2010 Jan;112(2):444-52. doi: 10.1111/j.1471-4159.2009.06482.x. PubMed PMID: 19895663. 8: Wang XS, Chen YY, Shang XF, Zhu ZG, Chen GQ, Han Z, Shao B, Yang HM, Xu HQ, Chen JF, Zheng RY. Idazoxan attenuates spinal cord injury by enhanced astrocytic activation and reduced microglial activation in rat experimental autoimmune encephalomyelitis. Brain Res. 2009 Feb 9;1253:198-209. doi: 10.1016/j.brainres.2008.11.059. PubMed PMID: 19083996. 9: Gooneratne SR. Effects of clonidine and idazoxan on tetrathiomolybdate-induced copper and lysosomal enzyme excretion into sheep bile. Res Vet Sci. 2012 Jun;92(3):456-61. doi: 10.1016/j.rvsc.2011.04.013. PubMed PMID: 21570700. 10: Semenova S, Markou A. The alpha2 adrenergic receptor antagonist idazoxan, but not the serotonin-2A receptor antagonist M100907, partially attenuated reward deficits associated with nicotine, but not amphetamine, withdrawal in rats. Eur Neuropsychopharmacol. 2010 Oct;20(10):731-46. doi: 10.1016/j.euroneuro.2010.05.003. PubMed PMID: 20627663; PubMed Central PMCID: PMC3545706. 11: Timofeeva OA, Levin ED. Idazoxan blocks the nicotine-induced reversal of the memory impairment caused by the NMDA glutamate receptor antagonist dizocilpine. Pharmacol Biochem Behav. 2008 Sep;90(3):372-81. doi: 10.1016/j.pbb.2008.03.011. PubMed PMID: 18456310. 12: Knight J, Harley CW. Idazoxan increases perforant path-evoked EPSP slope paired pulse inhibition and reduces perforant path-evoked population spike paired pulse facilitation in rat dentate gyrus. Brain Res. 2006 Feb 9;1072(1):36-45. PubMed PMID: 16426582. 13: Fara-On M, Evans JH, Harley CW. Idazoxan activates rat forebrain glycogen phosphorylase in vivo: a histochemical study. Brain Res. 2005 Oct 12;1059(1):83-92. PubMed PMID: 16226229. 14: Srinivasan J, Schmidt WJ. Serotonergic influence on the potentiation of D-amphetamine and apomorphine-induced rotational behavior by the alpha2-adrenoceptor antagonist 2-methoxy idazoxan in hemiparkinsonian rats. J Neural Transm (Vienna). 2005 Sep;112(9):1223-36. PubMed PMID: 15614426. 15: Eilon GF, Weisenthal L, Stupecky M, Landucci G, Slater LM. Antineoplastic activity of idazoxan hydrochloride. Cancer Chemother Pharmacol. 2009 Nov;64(6):1157-63. doi: 10.1007/s00280-009-0978-9. PubMed PMID: 19308411; PubMed Central PMCID: PMC2728905. 16: Serban DN, Serban IL, Nechifor M. Idazoxan effects upon contractile activity in the rat aorta are related to alpha adrenoceptors and L-type channels. Fundam Clin Pharmacol. 2004 Dec;18(6):635-41. PubMed PMID: 15548234. 17: Srinivasan J, Schmidt WJ. Treatment with alpha2-adrenoceptor antagonist, 2-methoxy idazoxan, protects 6-hydroxydopamine-induced Parkinsonian symptoms in rats: neurochemical and behavioral evidence. Behav Brain Res. 2004 Oct 5;154(2):353-63. PubMed PMID: 15313023. 18: Srinivasan J, Schmidt WJ. The effect of the alpha2-adrenoreceptor antagonist idazoxan against 6-hydroxydopamine-induced Parkinsonism in rats: multiple facets of action? Naunyn Schmiedebergs Arch Pharmacol. 2004 Jun;369(6):629-38. PubMed PMID: 15118809. 19: Invernizzi RW, Garavaglia C, Samanin R. The alpha 2-adrenoceptor antagonist idazoxan reverses catalepsy induced by haloperidol in rats independent of striatal dopamine release: role of serotonergic mechanisms. Neuropsychopharmacology. 2003 May;28(5):872-9. PubMed PMID: 12644843. 20: Shouse MN, Scordato JC, Farber PR, de Lanerolle N. The alpha2 adrenoreceptor agonist clonidine suppresses evoked and spontaneous seizures, whereas the alpha2 adrenoreceptor antagonist idazoxan promotes seizures in amygdala-kindled kittens. Brain Res. 2007 Mar 16;1137(1):58-68. PubMed PMID: 17214976.