Norepinephrine hydrochloride - CAS 329-56-6
Catalog number: 329-56-6
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
Adrenal medullary stress hormone, mediator of the fight-or-flight response; and the primary neurotransmitter in the post-ganglionic sympathetic (adrenergic) nervous system.
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L-Arterenol hydrochloride, L-Noradrenaline hydrochloride
1.Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma.
Sturdivant JM1, Royalty SM2, Lin CW2, Moore LA2, Yingling JD2, Laethem CL2, Sherman B2, Heintzelman GR2, Kopczynski CC2, deLong MA2. Bioorg Med Chem Lett. 2016 Apr 1. pii: S0960-894X(16)30337-7. doi: 10.1016/j.bmcl.2016.03.104. [Epub ahead of print]
Inhibition of Rho kinase (ROCK) to improve fluid outflow through the trabecular meshwork and lower intraocular pressure is a strategy for the development of new anti-glaucoma agents. Alpha-aryl-beta-amino isoquinoline analogs were identified as potent ROCK inhibitors. Compounds that provided a longer duration of intraocular pressure reduction in Dutch Belted rabbits also inhibited norepinephrine transporter. Ester 60 improved bioavailability of its parent ROCK inhibitor, 29 (Ki=0.2nM) and demonstrated an effective and sustained IOP reduction for 24h after dosing. From these studies, netarsudil (a.k.a. AR-13324) was discovered and is currently in clinical trials for the treatment of glaucoma and ocular hypertension.
2.Enhanced activity of hormone sensitive lipase (HSL) in mesenteric but not epididymal fat correlates with higher production of epinephrine in mesenteric adipocytes in rat model of cachectic rheumatoid arthritis.
Stofkova A1,2, Krskova K2, Vaculin S1, Jurcovicova J1,2. Autoimmunity. 2016 Apr 12:1-9. [Epub ahead of print]
Cachectic rheumatoid arthritis, the less frequent form of the disease, is associated with loss of fat mass and often more severe course of the disease. Its experimental model represents rat adjuvant arthritis (AA) characterized by edema, lack of appetite, sharp body weight and fat loss. As individual fat depots display functional differences, here we studied lipolytic activity and sensitivity to lipolytic stimuli of nodeless epididymal fat (eWAT) and perinodal mesenteric fat (mWAT) depots at the peak of AA. We also examined changes in catecholamine and cytokine levels involved in lipolysis in plasma and/or isolated adipocytes from both WATs to identify the contribution of local, adipocyte-based processes and/or systemic events to adiposity loss in cachectic rheumatoid arthritis. AA was induced to male Lewis rats by complete Freund's adjuvant. Groups of ad libitum-fed and pair-fed controls were used to distinguish the effects of food restriction from inflammation-induced cachexia.
3.Visualization of conventional outflow tissue responses to netarsudil in living mouse eyes.
Li G1, Mukherjee D2, Navarro I1, Ashpole NE1, Sherwood JM3, Chang J2, Overby DR3, Yuan F2, Gonzalez P1, Kopczynski CC4, Farsiu S5, Stamer WD6. Eur J Pharmacol. 2016 Apr 13. pii: S0014-2999(16)30206-0. doi: 10.1016/j.ejphar.2016.04.002. [Epub ahead of print]
Visual impairment due to glaucoma currently impacts 70 million people worldwide. While disease progression can be slowed or stopped with effective lowering of intraocular pressure, current medical treatments are often inadequate. Fortunately, three new classes of therapeutics that target the diseased conventional outflow tissue responsible for ocular hypertension are in the final stages of human testing. The rho kinase inhibitors have proven particularly efficacious and additive to current therapies. Unfortunately, non-contact technology that monitors the health of outflow tissue and its response to conventional outflow therapy is not available clinically. Using optical coherence tomographic (OCT) imaging and novel segmentation software, we present the first demonstration of drug effects on conventional outflow tissues in living eyes. Topical netarsudil (formerly AR-13324), a rho kinase/ norepinephrine transporter inhibitor, affected both proximal (trabecular meshwork and Schlemm's Canal) and distal portions (intrascleral vessels) of the mouse conventional outflow tract.
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CAS 329-56-6 Norepinephrine hydrochloride

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