Levocabastine hydrochloride

Modify Date: 2024-01-06 16:53:14

Levocabastine hydrochloride Structure
Levocabastine hydrochloride structure
Common Name Levocabastine hydrochloride
CAS Number 79547-78-7 Molecular Weight 456.98000
Density N/A Boiling Point 611ºC at 760 mmHg
Molecular Formula C26H30ClFN2O2 Melting Point N/A
MSDS Chinese USA Flash Point 323.3ºC
Symbol GHS07
GHS07
Signal Word Warning

 Use of Levocabastine hydrochloride


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].

 Names

Name (3S,4R)-1-[4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenylpiperidine-4-carboxylic acid,hydrochloride
Synonym More Synonyms

 Levocabastine hydrochloride 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
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

 Safety Information

Symbol GHS07
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

 Articles31

More 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...

 Synonyms

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