Levocabastine hydrochloride

Names

[ Name ]:
Levocabastine hydrochloride

[Synonym ]:
R 50,547
levocabastin
Livostin
LEVOCABASTINE HYDROCHLORIDE
Levocabastine HCl
Levocabastine
Levophta
levocobastine
UNII-124XMA6YEI

Biological Activity

[Description]:

Levocabastine (R 50547) hydrochloride is a long acting, highly potent and selective histamine H1-receptor antagonist with anti-allergic activity. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2[1][2].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

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

Research Areas >> Inflammation/Immunology

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

[Target]

H1 Receptor

NTR2:17 nM (Ki)

[In Vivo]

Levocabastine (0.25 mg/kg; i.p.; twice a day for five successive days; guinea-pigs) inhibits the virus-induced airway hyperresponsiveness, suppresses the influx of broncho-alveolar cells and increase in albumin content, and corrects the reduced chemiluminescence production by broncho-alveolar cells in response to zymosan[1]. In mice that receivedβ-LT, Levocabastine (0.05 mg/kg; i.p.) blocks the anxiolytic effect of β-LT and the number of head-dips decreased[2].

[References]

[1]. Folkerts G, et al. Virus-induced airway hyperresponsiveness in the guinea-pig: possible involvement of histamine and inflammatory cells. Br J Pharmacol. 1993;108(4):1083-1093.

[2]. Yamauchi R, et al. Effect of beta-lactotensin on acute stress and fear memory. Peptides. 2006;27(12):3176-3182.

Chemical & Physical Properties

[ Boiling Point ]:
611ºC at 760 mmHg

[ Molecular Formula ]:
C₂₆H₃₀ClFN₂O₂

[ Molecular Weight ]:
456.98000

[ Flash Point ]:
323.3ºC

[ Exact Mass ]:
456.19800

[ PSA ]:
64.33000

[ LogP ]:
5.63398

[ Appearance of Characters ]:
solid | white

[ Storage condition ]:
2-8°C

[ Water Solubility ]:
DMSO: ~10 mg/mL, soluble

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P305 + P351 + P338

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

[ Hazard Codes ]:
Xi

[ Risk Phrases ]:
36/37/38

[ Safety Phrases ]:
26-36

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

Articles

Treatment of allergic conjunctivitis: results of a 1-month, single-masked randomized study.

Eur. J. Ophthalmol. 20(5) , 811-8, (2010)

To compare the effects of topical antiallergic eyedrops in relieving the signs and symptoms of patients with allergic conjunctival pathology.In this multicenter, single-masked, randomized study, 240 p...

Neurotensin decreases high affinity [3H]-ouabain binding to cerebral cortex membranes.

Regul. Pept. 172(1-3) , 35-40, (2011)

Previous work from this laboratory showed the ability of neurotensin to inhibit synaptosomal membrane Na(+), K(+)-ATPase activity, the effect being blocked by SR 48692, a non-peptidic antagonist for h...

Neurotensin is a regulator of insulin secretion in pancreatic beta-cells.

Int. J. Biochem. Cell Biol. 42(10) , 1681-8, (2010)

Neurotensin (NT) is secreted from neurons and gastrointestinal endocrine cells. We previously reported that the three NT receptors (NTSRs) are expressed in pancreatic islets and beta cell lines on whi...