Idazoxan

Idazoxan
Clinical data
Routes of; administration	Oral
ATC code	none;
Legal status
Legal status	In general: uncontrolled;
Identifiers
	IUPAC name (±)-2-(2,3-dihydro-1,4-benzodioxin-2-yl)-4,5-dihydro-1H-imidazole;
CAS Number	79944-58-4 ;
PubChem CID	54459;
ChemSpider	49184 ;
UNII	Y310PA316B;
ChEMBL	ChEMBL10316 ;
CompTox Dashboard (EPA)	DTXSID6045161 ;
Chemical and physical data
Formula	C11H12N2O2
Molar mass	204.229 g·mol−1
3D model (JSmol)	Interactive image;
Chirality	Racemic mixture
	SMILES C1CN=C(N1)C2COC3=CC=CC=C3O2;
	InChI InChI=1S/C11H12N2O2/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) ; Key:HPMRFMKYPGXPEP-UHFFFAOYSA-N ;
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Idazoxan (INN) is a drug which is used in scientific research. It acts as both a selective α2 adrenergic receptor antagonist, and an antagonist for the imidazoline receptor.^[1]^[2] Idazoxan has been under investigation as an antidepressant, but it did not reach the market as such. More recently, it is under investigation as an adjunctive treatment in schizophrenia. Due to its alpha-2 receptor antagonism it is capable of enhancing therapeutic effects of antipsychotics, possibly by enhancing dopamine neurotransmission in the prefrontal cortex of the brain, a brain area thought to be involved in the pathogenesis of schizophrenia.

Alzheimer's research

Mice treated with idazoxan, which blocks the α_2A receptor which regulates norepinephrine, behaved similarly to control animals despite still having amyloid-beta plaques in the brain, as a proof-of-concept experiment that dramatically reduced Alzheimer's pathology and symptoms in two mouse models, potentially offering an immediate treatment for this devastating disease.^[3]

References

^ Bousquet P, Bruban V, Schann S, Greney H, Ehrhardt JD, Dontenwill M, Feldman J (June 1999). "Participation of imidazoline receptors and alpha(2-)-adrenoceptors in the central hypotensive effects of imidazoline-like drugs". Annals of the New York Academy of Sciences. 881 (1): 272–8. Bibcode:1999NYASA.881..272B. doi:10.1111/j.1749-6632.1999.tb09369.x. PMID 10415925.
^ Clarke RW, Harris J (2002). "RX 821002 as a tool for physiological investigation of alpha(2)-adrenoceptors". CNS Drug Reviews. 8 (2): 177–92. doi:10.1111/j.1527-3458.2002.tb00222.x. PMC 6741674. PMID 12177687.
^ University of Alabama at Birmingham (January 15, 2020). "Pathogenic Alzheimer's disease cascade is activated by faulty norepinephrine signaling". medicalexpress.com. Retrieved January 15, 2020.

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[1] Bousquet P, Bruban V, Schann S, Greney H, Ehrhardt JD, Dontenwill M, Feldman J (June 1999). "Participation of imidazoline receptors and alpha(2-)-adrenoceptors in the central hypotensive effects of imidazoline-like drugs". Annals of the New York Academy of Sciences. 881 (1): 272–8. Bibcode:1999NYASA.881..272B. doi:10.1111/j.1749-6632.1999.tb09369.x. PMID 10415925.

[2] Clarke RW, Harris J (2002). "RX 821002 as a tool for physiological investigation of alpha(2)-adrenoceptors". CNS Drug Reviews. 8 (2): 177–92. doi:10.1111/j.1527-3458.2002.tb00222.x. PMC 6741674. PMID 12177687.

[3] University of Alabama at Birmingham (January 15, 2020). "Pathogenic Alzheimer's disease cascade is activated by faulty norepinephrine signaling". medicalexpress.com. Retrieved January 15, 2020.

[1]

[2]

[3]

v t e Imidazoline receptor modulators
IRTooltip Imidazoline receptor	Agonists: 2-BFI 7-Me-Marsanidine Agmatine Apraclonidine BU224 Clonidine Clorgyline Harmalas LNP-509 LNP-911 mCPP Moxonidine Rilmenidine S-23515 S-23757 Antagonists: BU99006 Efaroxan Idazoxan Unsorted/unknown: CR-4056 Pargyline
See also: Receptor/signaling modulators

Alzheimer's research

See also

References