Detail of "70359-46-5"

CAS Number:
70359-46-5
Name:
Brimonidine D-tartrate
Molecular Structure:
Formula:
C₁₁H₁₀BrN₅^.C₄H₆O₆
Molecular Weight:
442.22
Deleted CAS:
79570-19-7|109826-56-4
Synonyms:
Alphagan P;6-Quinoxalinamine,5-bromo-N-(4,5-dihydro- 1H-imidazol-2-yl)-,(2R,3R)-2,3-dihydroxybutanedioate (1:1);LK 14304-18;Brimonidine tartrate;
Melting Point:
207-208 °C (dec.)
Boiling Point:
432.6 °C at 760 mmHg
Flash Point:
215.4 °C
Appearance:
Off-white crystalline solid

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Reference

Characterization of postjunctional alpha-1 and alpha-2 adrenoceptors activated by exogenous or nerve-released norepinephrine in the canine saphenous vein: Characterization of postjunctional alpha-1 and alpha-2 adrenoceptors activated by exogenous or nerve-released norepinephrine in the canine saphenous vein. Flavahan, Nicholas A.; Rimele, Thomas J.; Cooke, John P.; Vanhoutte, Paul M. (Dep. Physiol. Biophys., Mayo Clin. Mayo Found., Rochester, MN, USA). J. Pharmacol. Exp. Ther., 230(3), 699-705 (English) 1984. CODEN: JPETAB. ISSN: 0022-3565. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 2 Expts. were designed to characterize alpha-1 and alpha-2 adrenoceptor-mediated effects in the canine saphenous vein. Rings of saphenous vein were mounted for isometric tension recording in physiol. saline soln. Contractile responses evoked by alpha-1 adrenoceptor agonists, cirazoline [59939-16-1] or St 587 [15327-38-5] were inhibited by alpha-1 antagonists, prazosin [19216-56-9] or phenoxybenzamine [59-96-1], but were relatively resistant to the alpha-2 adrenoceptor antagonist rauwolscine [131-03-3]. The responses to alpha-2 adrenoceptor agonists, xylazine [7361-61-7] or B-HT 920 [36085-73-1] were relatively resistant to prazosin or phenoxybenzamine but were antagonized by rauwolscine. After phenoxybenzamine, the alpha-2 agonists, M-7 [39478-90-5], guanfacine [29110-47-2], UK 14304 tartrate [70359-46-5], B-HT 920 and xylazine evoked similar maximal increases in tension which were considerably smaller (approx. 50%) than that attained by alpha-1 adrenoceptor stimulation. The different concn.-effect characteristics of these responses were also revealed using norepinephrine bitartrate [51-40-1]. Prazosin produced a biphasic effect on the concn.-response curve of norepinephrine, being more potent against responses above 50% of the max. compared to lower increases in tension. After alpha-1 adrenoceptor blockade with prazosin, rauwolscine was more effective against responses below 50% of the max., compared to higher increases in tension. The results suggest that the alpha-1 and alpha-2 adrenoceptor-mediated concn.-effect curves to norepinephrine are almost coincident and that alpha-2 adrenergic stimulation produces only partial activation of the vascular smooth muscle. Contractile responses produced by sympathetic nerve stimulation or by tyramine [51-67-2] were antagonized more effectively by the combination of prazosin plus rauwolscine than by either blocker given alone, suggesting that alpha-1 and alpha-2 adrenoceptors are both innervated by sympathetic nerves in the canine saphenous vein.

Non-systemic delivery of topical brimonidine to the brain: a neuro-ocular tissue distribution study: All Rights Reserved. Non-systemic delivery of topical brimonidine to the brain: a neuro-ocular tissue distribution study. Tamilvanan, Shunmugaperumal; Abdulrazik, Muhammad; Benita, Simon (Pharmaceutics Department, School of Pharmacy, Hebrew University of Jerusalem, Jerusalem 91120, Israel). Journal of Drug Targeting, 14(10), 670-679 (English) 2006 Informa Healthcare. CODEN: JDTAEH. ISSN: 1061-186X. DOCUMENT TYPE: Journal CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 1 To date, the risks of central nervous system (CNS) side effects of topically administered ophthalmic therapeutic agents are thought to be the consequence of systemic absorption of these drugs.There are some reagents like 70359-46-5 is used in this study. This paper envisions the possibility of drug delivery to the CNS following ocular application through non-systemic routes. After single instillation of 50 ml of 3H-radiolabeled Alphagan soln. (0.2%) in the cul de sac of the right eye, three male albino rabbits (2-2.5 kg) were sacrificed at each time point (5, 15, 30 and 60 min). Both sides (eyes) specimens of aq. humor, cornea, iris, lens, vitreous, conjunctiva, sclera, ciliary body, choroid, retina, optic nerve, optic tract and olfactory bulb were weighed, and blood samples were measured, before combustion in tissue oxidizer and radioactive liq. scintillation counting. Significant 3H-brimonidine levels were found in right and left optic nerves and tracts with extremely low corresponding drug levels in blood. Uveal tract (ciliary body, iris and choroid tissues) brimonidine levels were relatively high in the treated eye, and the highest among contralateral eye tissues. Our data provide the first case of good CNS availability after ocular application of conventional ophthalmic therapeutic agent, through non-systemic routes. Similar neuro-ocular pharmacokinetic studies should be adopted as a routine ocular therapeutics evaluation study. .

Detail of "70359-46-5"

Brimonidine D-tartrate

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CAS No.70359-46-5 Brimonidine D-tartrate

CAS No.70359-46-5 Brimonidine D-tartrate

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CAS No.70359-46-5 Brimonidine D-tartrate

CAS No.70359-46-5 Brimonidine D-tartrate

CAS No.70359-46-5 Brimonidine D-tartrate

CAS No.70359-46-5 Brimonidine D-tartrate

CAS No.70359-46-5 Brimonidine D-tartrate

CAS No.70359-46-5 Brimonidine D-tartrate

CAS No.70359-46-5 Brimonidine D-tartrate

Reference