Brimonidine

Modify Date: 2024-01-02 11:35:02

Brimonidine Structure
Brimonidine structure
Common Name Brimonidine
CAS Number 59803-98-4 Molecular Weight 292.135
Density 1.8±0.1 g/cm3 Boiling Point 432.6±55.0 °C at 760 mmHg
Molecular Formula C11H10BrN5 Melting Point 207.5 °C
MSDS Chinese USA Flash Point 215.4±31.5 °C
Symbol GHS06
GHS06
Signal Word Danger

 Use of Brimonidine


Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.

 Names

Name brimonidine
Synonym More Synonyms

 Brimonidine Biological Activity

Description Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
Related Catalog
Target

α2-adrenergic Receptor.

In Vitro [3H]Brimonidine (UK 14304) is a full agonist at alpha 2-adrenergic receptors. [3H]Brimonidine (UK 14304) labels at least 2 specific binding sites in human brain that both have the characteristics of an alpha 2-adrenergic binding site. GTP decreases agonist binding at both of these sites, but with different potencies at each site [1-3].
References

[1]. Andorn, A.C., M.A. Carlson, and R.C. Gilkeson, Specific [3H]UK 14,304 binding in human cortex occurs at multiple high affinity states with alpha 2-adrenergic selectivity and differing affinities for GTP. Life Sci, 1988. 43(22): p. 1805-12.

[2]. Cambridge, D., UK-14,304, a potent and selective alpha2-agonist for the characterisation of alpha-adrenoceptor subtypes. Eur J Pharmacol, 1981. 72(4): p. 413-5.

[3]. Chopin, P., F.C. Colpaert, and M. Marien, Effects of alpha-2 adrenoceptor agonists and antagonists on circling behavior in rats with unilateral 6-hydroxydopamine lesions of the nigrostriatal pathway. J Pharmacol Exp Ther, 1999. 288(2): p. 798-804.

 Chemical & Physical Properties

Density 1.8±0.1 g/cm3
Boiling Point 432.6±55.0 °C at 760 mmHg
Melting Point 207.5 °C
Molecular Formula C11H10BrN5
Molecular Weight 292.135
Flash Point 215.4±31.5 °C
Exact Mass 291.011963
PSA 62.20000
LogP 0.96
Vapour Pressure 0.0±1.0 mmHg at 25°C
Index of Refraction 1.798
Storage condition Store at RT
Water Solubility 45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: <0.8 mg/mL

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
VD1200000
CHEMICAL NAME :
6-Quinoxalinamine, 5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl)-
CAS REGISTRY NUMBER :
59803-98-4
LAST UPDATED :
199612
DATA ITEMS CITED :
1
MOLECULAR FORMULA :
C11-H10-Br-N5

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
160 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JKXXAF Japanese Kokai Tokyo Koho Patents. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #81-02912

 Safety Information

Symbol GHS06
GHS06
Signal Word Danger
Hazard Statements H301
Precautionary Statements P301 + P310
Hazard Codes T:Toxic;
Risk Phrases R25;R36/37/38
Safety Phrases S26-S36-S45
RIDADR UN 2811 6.1/PG 3
WGK Germany -
RTECS VD1200000
Packaging Group III
Hazard Class 6.1
HS Code 2934999090

 Precursor & DownStream

Precursor  0

DownStream  1

 Customs

HS Code 2934999090
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Articles55

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A Comparison of the Anorectic Effect and Safety of the Alpha2-Adrenoceptor Ligands Guanfacine and Yohimbine in Rats with Diet-Induced Obesity.

PLoS ONE 10 , e0141327, (2015)

The search for drugs with anorectic activity, acting within the adrenergic system has attracted the interest of researchers. Partial α2-adrenoceptor agonists might offer the potential for effective an...

Brimonidine reduces TGF-beta-induced extracellular matrix synthesis in human Tenon's fibroblasts.

BMC Ophthalmol. 15 , 54, (2015)

Brimonidine is a highly selective α2 adrenergic agonist that has been widely used in anti-glaucoma eyedrops. The aim of this study was to investigate its putative anti-fibrotic role in the fibrosis ca...

Dilute brimonidine to improve patient comfort and subconjunctival hemorrhage after LASIK.

J. Refract. Surg. 29(7) , 469-75, (2013)

To investigate whether dilute brimonidine (0.025%) reduces patient discomfort, subconjunctival hemorrhage, and injection after LASIK without a significant increase in the rate of flap complications or...

 Synonyms

brimonidinum
5-bromo-6-(imidazolin-2-ylamino)-quinoxaline
MFCD00153878
Brimonidine [INN:BAN]
Bromoxidine
Brimonidine
5-bromo-6-(2-imidazolin-2-ylamino)quinoxaline
UNII-E6GNX3HHTE
[3H]-Brimonidine
5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine
5-Bromo-N-(4,5-dihydro-1H-imidazol-2-yl)-6-quinoxalinamine
6-Quinoxalinamine, 5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl)-
UK 14,304
brimonidina
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