Idazoxan Hydrochloride

Names

[ Name ]:
Idazoxan Hydrochloride

[Synonym ]:
Idazoxan Hydrochloride
Melanotan II
IdazoxanHCl

Biological Activity

[Description]:

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[1][2].

[Related Catalog]:

Research Areas >> Endocrinology

[Target]

α2-adrenoceptor[1]; Imidazoline receptors (IRs)[2]

[In Vivo]

Idazoxan (0.16-5 mg/kg; subcutaneous injection; for 1 hour; male CD-COBS rats) treatment potently reverses haloperidol-induced catalepsy with an ED50 of 0.25 mg/kg. Idazoxan (0.3 and 2.5 mg/kg) has no effect on extracellular DA and do not modify the rise of extracellular DA induced by haloperidol[1]. Animal Model: Male CD-COBS rats injected with 1 mg/kg haloperidol[1] Dosage: 0.16 mg/kg, 0.31 mg/kg, 0.63 mg/kg, 1.25 mg/kg, 2.5 mg/kg, and 5.0 mg/kg Administration: Subcutaneous injection; for 1 hour Result: Potently reversed haloperidol-induced catalepsy with an ED50 of 0.25 mg/kg.

[References]

[1]. Roberto W Invernizzi, et al. The α2-Adrenoceptor Antagonist Idazoxan Reverses Catalepsy Induced by Haloperidol in Rats Independent of Striatal Dopamine Release: Role of Serotonergic Mechanisms. Neuropsychopharmacology volume 28, pages872-879 (2003).

[2]. Bousquet P, et al. Participation of imidazoline receptors and alpha(2-)-adrenoceptors in the central hypotensive effects of imidazoline-like drugs. Ann N Y Acad Sci. 1999 Jun 21;881:272-8.

Chemical & Physical Properties

[ Boiling Point ]:
397ºC at 760 mmHg

[ Molecular Formula ]:
C₁₁H₁₃ClN₂O₂

[ Molecular Weight ]:
240.68600

[ Flash Point ]:
193.9ºC

[ Exact Mass ]:
240.06700

[ PSA ]:
42.85000

[ LogP ]:
1.39450

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ Hazard Codes ]:
Xn: Harmful;

[ Risk Phrases ]:
22

[ Safety Phrases ]:
7

[ RIDADR ]:
UN 2811 6.1/PG 3

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

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