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Chemical Structure| 70359-46-5 Chemical Structure| 70359-46-5

Structure of Brimonidine tartrate
CAS No.: 70359-46-5

Chemical Structure| 70359-46-5

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Brimonidine tartrate is an α-adrenergic receptor agonist with EC50 of 0.45 nM for the α2A adrenoreceptor, used to treat glaucoma through a dual mechanism of action by reducing aqueous humor production and increasing uveoscleral outflow.

Synonyms: AGN190342 tartrate; UK 14304 tartrate; Alphagan P

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Product Details of Brimonidine tartrate

CAS No. :70359-46-5
Formula : C15H16BrN5O6
M.W : 442.22
SMILES Code : BrC1=C2N=CC=NC2=CC=C1NC3=NCCN3.O=C(O)[C@H](O)[C@@H](O)C(O)=O
Synonyms :
AGN190342 tartrate; UK 14304 tartrate; Alphagan P
MDL No. :MFCD07773072

Safety of Brimonidine tartrate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Brimonidine tartrate

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
human trabecular meshwork (HTM) cells 10 μM 6 days To investigate the effects of BRI on the barrier function of TGF-β2-treated HTM cells, BRI significantly inhibited the TGF-β2-induced increase in TEER values and reduction in FITC dextran permeability Bioengineering (Basel). 2022 Jul 12;9(7):310
Rat retinal rod bipolar cells 0.1, 0.3, 1 μM To investigate the inhibitory effect of brimonidine tartrate on presynaptic Ca2+ signals, results showed that brimonidine significantly inhibited presynaptic Ca2+ signals. J Neurosci. 2014 Jul 9;34(28):9432-40
Müller glia 1 μM 3, 6, 12, 24 h To evaluate the effect of brimonidine tartrate on the production of neurotrophic factors in Müller glia. Results showed that brimonidine tartrate significantly increased mRNA expression levels of NGF, BDNF, and bFGF. Cell Death Dis. 2014 Jul 17;5(7):e1341

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice Microbead-induced ocular hypertensive model Topical eye drops 0.15% Twice daily for 2 weeks To evaluate the IOP-lowering effect of brimonidine tartrate and its protective effects on retinal ganglion cells and axons in the microbead-induced ocular hypertensive mouse model. Results showed that brimonidine tartrate significantly reduced IOP and improved the survival of retinal ganglion cells and axons. Invest Ophthalmol Vis Sci. 2012 Jun 20;53(7):3733-41
Mice Optic nerve injury model Eye drops 1.0% Daily for 2 weeks Brimonidine tartrate promotes optic nerve regeneration by inducing Erk1/2 phosphorylation and upregulates TrkB expression while downregulating p75 expression. Cell Death Dis. 2013 Aug 8;4(8):e763
Rats Laser-induced ocular hypertension model Subcutaneous injection 1 mg/kg Continuous for 8 weeks To investigate the protective effects of brimonidine tartrate on retinal ganglion cells under conditions of elevated intraocular pressure. Results showed that brimonidine tartrate significantly improved retinal ganglion cell survival, particularly in the nasal region of the retina. Additionally, brimonidine preserved ganglion cell axon morphology, density, and total number in the optic nerve, and significantly reduced deficits in axonal transport to the superior colliculus associated with elevated ocular pressure. Mol Neurodegener. 2011 Jan 13;6(1):4

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02039765 Hyperemia PHASE1 COMPLETED 2025-04-14 Bausch & Lomb, Incorporated, R... More >>ochester, New York, 14609, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.26mL

0.45mL

0.23mL

11.31mL

2.26mL

1.13mL

22.61mL

4.52mL

2.26mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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