CAS 59803-98-4|Brimonidine
| 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 | ChineseUSA | Flash Point | 215.4±31.5 °C |
| Symbol | GHS06 | Signal Word | Danger |
Names
| Name | brimonidine |
|---|---|
| Synonym | More Synonyms |
Brimonidine BiologicalActivity
| Description | Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist. |
|---|---|
| Related Catalog | Signaling Pathways >>GPCR/G Protein >>Adrenergic ReceptorResearch Areas >>Others |
| 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 |
| InChIKey | XYLJNLCSTIOKRM-UHFFFAOYSA-N |
| SMILES | Brc1c(NC2=NCCN2)ccc2nccnc12 |
| Storage condition | Store at RT |
| Water Solubility | 45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: <0.8 mg/mL |
Toxicological Information
CHEMICAL IDENTIFICATION |
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 |
|---|---|
| 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 |
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
More Articles| 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 |
