Cirazoline hydrochloride

Names

[ Name ]:
Cirazoline hydrochloride

[Synonym ]:
2-[(2-Cyclopropylphenoxy)methyl]-4,5-dihydro-1H-imidazole hydrochloride
Cirazoline HCl
Phenserine
EINECS 254-995-3
Cirazoline hydrochloride
MFCD00274034

Biological Activity

[Description]:

Cirazoline hydrochloride (LD 3098 hydrochloride) is a potent competitive full α1A-adrenergic receptor (α1A-AR) agonist (Ki=120 nM) and only a partial agonist at α1B-AR (Ki= 960 nM) and α1D-AR (Ki=660 nM)[1].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor

[In Vitro]

Cirazoline hydrochloride (5-10 μM; 24 hours) does not alter GIC survival and counteracted only poorly prazosin‐induced GIC death[1]. Cell Viability Assay[1] Cell Line: Glioblastoma‐initiating cells Concentration: 5 μM; 10 μM Incubation Time: 24 hours Result: Did not effect GIC cell survival.

[In Vivo]

Cirazoline hydrochloride (drinking water; 40 μM; 9 month) exhibits significantly decreased immobility in the TST and enhances neurogenesis in the mouse[1]. Animal Model: B6/CBA mice[1] Dosage: 40 μM Administration: Drinking water; 40 μM; 9 month Result: Reversed antidepressant-like phenotype of CAM α1A-AR Mice .

[References]

[1]. Doze VA, et al. alpha(1A)- and alpha(1B)-adrenergic receptors differentially modulate antidepressant-like behaviorin the mouse.Brain Res. 2009 Aug 18;1285:148-57.

[2]. Suzana Assad Kahn , et al. The Anti-Hypertensive Drug Prazosin Inhibits Glioblastoma Growth via the PKCδ-dependent Inhibition of the AKT Pathway. EMBO Mol Med. 2016 May 2;8(5):511-26.

Chemical & Physical Properties

[ Density]:
1.25g/cm3

[ Boiling Point ]:
409.5ºC at 760mmHg

[ Molecular Formula ]:
C₁₃H₁₇ClN₂O

[ Molecular Weight ]:
252.74000

[ Flash Point ]:
201.4ºC

[ Exact Mass ]:
252.10300

[ PSA ]:
33.62000

[ LogP ]:
2.51090

[ Storage condition ]:
2-8°C

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Safety Phrases ]:
S22-S24/25

[ RIDADR ]:
NONH for all modes of transport

Articles

The contribution of d-tubocurarine-sensitive and apamin-sensitive K-channels to EDHF-mediated relaxation of mesenteric arteries from eNOS-/- mice.

J. Cardiovasc. Pharmacol. 59(5) , 413-25, (2012)

The nature of the potassium channels involved in determining endothelium-derived hyperpolarizing factor-mediated relaxation was investigated in first-order small mesenteric arteries from male endothel...

Different response of ANP secretion to adrenoceptor stimulation in renal hypertensive rat atria.

Peptides 29(7) , 1207-15, (2008)

Sympathetic nervous system and atrial natriuretic peptide (ANP) system play fundamental roles in the regulation of cardiovascular functions. Overactivity of sympathetic nervous system can lead into ca...

Attenuation of store-operated Ca2+ entry and enhanced expression of TRPC channels in caudal artery smooth muscle from Type 2 diabetic Goto-Kakizaki rats.

Clin. Exp. Pharmacol. Physiol. 37(7) , 670-8, (2010)

1. Previously, we found that Ca(2+) entry from the extracellular space via alpha(1)-adrenoceptor-activated, Ca(2+)-permeable channels, but not voltage-gated Ca(2+) channels, is impaired in endothelium...