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I6138

Idazoxan hydrochloride

Name: Idazoxan hydrochloride
Brand: SIGMA

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Synonym(s):

(±)-2-[1,4-Benzodioxan-2-yl]-2-imidazoline hydrochloride, RX 781094

Empirical Formula (Hill Notation):

C₁₁H₁₂N₂O₂ · HCl

CAS Number:

79944-56-2

Molecular Weight:

240.69

MDL number:

MFCD00069293

PubChem Substance ID:

24278493

NACRES:

NA.77

solubility

H₂O: 50 mg/mL

SMILES string

Cl.C1CN=C(N1)C2COc3ccccc3O2

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

InChI key

MYUBYOVCLMEAOH-UHFFFAOYSA-N

Gene Information

human ... ADRA2A(150) , ADRA2B(151) , ADRA2C(152)

Application

Idazoxan hydrochloride has been used to study the efficacy of antidepressant treatments that interact with multiple neurotransmitter systems.

Biochem/physiol Actions

α2-adrenoceptor antagonist; I2 imidazoline receptor agonist; I1 imidazoline receptor antagonist. Idazoxan can antagonize various behaviors generated by ethanol in a preclinical setting. It possesses neuroprotective activity against spinal cord injury, resulted due to experimental autoimmune encephalomyelitis (EAE) in mouse, an animal modal of multiple sclerosis (MS).

Pictograms

GHS06

Signal Word

Danger

Hazard Statements

H301

Precautionary Statements

P301 + P310

Hazard Classifications

Acute Tox. 3 Oral

Storage Class Code

6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

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An increase in spinal cord noradrenaline is a major contributor to the antihyperalgesic effect of antidepressants after peripheral nerve injury in the rat.

Kunie Nakajima et al.

Pain, 153(5), 990-997 (2012-03-20)

Antidepressants are often used for the treatment of neuropathic pain. Clinical studies suggest that the efficacy of serotonin (5-HT) and noradrenaline (NA) reuptake inhibitors (SNRIs) for neuropathic pain is greater than that of selective 5-HT reuptake inhibitors (SSRIs). In the

Spontaneous spiking and synaptic depression underlie noradrenergic control of feed-forward inhibition.

Sidney P Kuo et al.

Neuron, 71(2), 306-318 (2011-07-28)

Inhibitory interneurons across diverse brain regions commonly exhibit spontaneous spiking activity, even in the absence of external stimuli. It is not well understood how stimulus-evoked inhibition can be distinguished from background inhibition arising from spontaneous firing. We found that noradrenaline

Effects of idazoxan on alcohol pharmacokinetics and intoxication: a preliminary human laboratory study

Haass-Koffler C L, et al.

Alcohol, 39(4), 594-602 (2015)

Favourable involvement of α2A-adrenoreceptor antagonism in the I₂-imidazoline binding sites-mediated morphine analgesia enhancement.

Valerio Mammoli et al.

Bioorganic & medicinal chemistry, 20(7), 2259-2265 (2012-03-01)

Aim of the present study was to obtain novel α(2)-adrenoreceptor (α(2)-AR) antagonists, possibly endowed with subtype-selectivity. Therefore, inspired by the non subtype-selective α(2)-AR antagonist idazoxan, we designed 1,4-dioxane derivatives bearing an aromatic area in position 5 or 6 and the

Repetitive treatment with diluted bee venom reduces neuropathic pain via potentiation of locus coeruleus noradrenergic neuronal activity and modulation of spinal NR1 phosphorylation in rats.

Suk-Yun Kang et al.

The journal of pain : official journal of the American Pain Society, 13(2), 155-166 (2012-01-06)

We previously demonstrated that a single injection of diluted bee venom (DBV) temporarily alleviates thermal hyperalgesia, but not mechanical allodynia, in neuropathic rats. The present study was designed to determine whether repetitive injection of DBV produces more potent analgesic effects

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