913064-47-8 Usage
Biological Activity
eln441958 is a novel, potent and selective bradykinin b1 receptor antagonist with ki value of 0.26 nm [1].the bradykinin b1 receptor is a g-protein coupled receptor with principal ligand of bradykinin and plays an important role in chronic pain and inflammation [1].eln441958 is a novel, potent and selective bradykinin b1 receptor antagonist. in imr-90 lung fibroblast cell membranes, eln441958 competitively inhibited the binding of the agonist [3h]dakd to the human b1 receptor with ki value of 0.26 nm. in imr-90 cells expressing the native human b1 receptor, eln441958 concentration-dependently antagonized calcium mobilization induced by dakd with kb value of 0.12 nm. eln441958 is highly selective for b1 over b2 receptors. eln441958 failed to inhibit the calcium mobilization induced by b2-receptor agonist bk. eln441958 also inhibited human μ-, δ-, κ- opioid receptors and muscarinic m1 receptor with ki values of 0.13, 0.69, 1.5 and 0.37 μm, respectively. eln441958 is also an agonist at the δ-opioid receptor (ec50 = 0.76 μm) and μ-opioid receptor. in vitro, eln441958 exhibited good permeability and metabolic stability [1].in rats and rhesus monkeys, eln441958 exhibited high oral bioavailability and moderate plasma half-lives. in rhesus monkeys, eln441958 dose-dependently reduced the thermal hyperalgesia induced by carrageenan with ed50 value of ~3 mg/kg s.c [1].
references
[1]. hawkinson je, szoke bg, garofalo aw, et al. pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin b1 receptor antagonist eln441958, j pharmacol exp ther, 2007, 322(2): 619-630.
Check Digit Verification of cas no
The CAS Registry Mumber 913064-47-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,1,3,0,6 and 4 respectively; the second part has 2 digits, 4 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 913064-47:
(8*9)+(7*1)+(6*3)+(5*0)+(4*6)+(3*4)+(2*4)+(1*7)=148
148 % 10 = 8
So 913064-47-8 is a valid CAS Registry Number.
913064-47-8Relevant academic research and scientific papers
Pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin B1 receptor antagonist ELN441958
Hawkinson, Jon E.,Szoke, Balazs G.,Garofalo, Albert W.,Hom, Dennis S.,Zhang, Hongbing,Dreyer, Mark,Fukuda, Juri Y.,Chen, Linda,Samant, Bhushan,Simmonds, Stellanie,Zeitz, Karla P.,Wadsworth, Angie,Liao, Anna,Chavez, Raymond A.,Zmolek, Wes,Ruslim, Lany,Bova, Michael P.,Holcomb, Ryan,Butelman, Eduardo R.,Ko, Mei-Chuan,Malmberg, Annika B.
, p. 619 - 630 (2008/03/12)
The bradykinin B1 receptor plays a critical role in chronic pain and inflammation, although efforts to demonstrate efficacy of receptor antagonists have been hampered by species-dependent potency differences, metabolic instability, and low oral
Novel compounds useful for bradykinin B1 receptor antagonism
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Page/Page column 45, (2010/11/25)
Disclosed are compounds that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor.
