73210-73-8 Usage
Description
Different sources of media describe the Description of 73210-73-8 differently. You can refer to the following data:
1. Xamoterol fumarate is a cardioselective partial beta-agonist, the first of its class to be
developed for use in heart failure. The main advantage of xamoterol fumarate as a
cardiotonic lies in the fact that its beta-blocking effect exerted during high sympathetic
drive will protect the heart from overstimulation. It is claimed to be a viable but safer
alternative to digoxin.
2. Xamoterol is a partial agonist of β1-adrenergic receptors (β1-ARs) with an EC50 value of 80 nM for the generation of cyclic AMP (cAMP) in neonatal rat cardiomyocyte cultures. It increases spontaneous contraction of isolated rat right atria (EC50 = 4.67 nM). In vivo, xamoterol increases heart rate in beagle dogs (ED50 = 3.2 μg/kg) and in a rat model of spontaneous heart failure (ED50 = 6 μg/kg), an effect that is reversed by the selective β1-AR antagonist betaxolol but not the selective β2-AR antagonist ICI 118551 . Formulations containing xamoterol have been used in the treatment of heart failure.
Uses
Different sources of media describe the Uses of 73210-73-8 differently. You can refer to the following data:
1. Xamoterol Hemifumarate, is a β1-adrenoceptor-selective partial agonist.
2. Stimulant (cardiac).
Brand name
Corwin
Biological Activity
β 1 -adrenoceptor-selective partial agonist (pA 2 values are 7.4-7.8 and 5.2-6.2 at β 1 - and β 2 -adrenoceptors respectively).
Check Digit Verification of cas no
The CAS Registry Mumber 73210-73-8 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 7,3,2,1 and 0 respectively; the second part has 2 digits, 7 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 73210-73:
(7*7)+(6*3)+(5*2)+(4*1)+(3*0)+(2*7)+(1*3)=98
98 % 10 = 8
So 73210-73-8 is a valid CAS Registry Number.
InChI:InChI=1/C16H25N3O5.C4H4O4/c20-13-1-3-15(4-2-13)24-12-14(21)11-17-5-6-18-16(22)19-7-9-23-10-8-19;5-3(6)1-2-4(7)8/h1-4,14,17,20-21H,5-12H2,(H,18,22);1-2H,(H,5,6)(H,7,8)/b;2-1+
73210-73-8Relevant articles and documents
Discovery of novel brain permeable and G protein-biased beta-1 adrenergic receptor partial agonists for the treatment of neurocognitive disorders
Yi, Bitna,Jahangir, Alam,Evans, Andrew K.,Briggs, Denise,Ravina, Kristine,Ernest, Jacqueline,Farimani, Amir B.,Sun, Wenchao,Rajadas, Jayakumar,Green, Michael,Feinberg, Evan N.,Pande, Vijay S.,Shamloo, Mehrdad
, (2017/08/01)
The beta-1 adrenergic receptor (ADRB1) is a promising therapeutic target intrinsically involved in the cognitive deficits and pathological features associated with Alzheimer’s disease (AD). Evidence indicates that ADRB1 plays an important role in regulating neuroinflammatory processes, and activation of ADRB1 may produce neuroprotective effects in neuroinflammatory diseases. Novel small molecule modulators of ADRB1, engineered to be highly brain permeable and functionally selective for the G protein with partial agonistic activity, could have tremendous value both as pharmacological tools and potential lead molecules for further preclinical development. The present study describes our ongoing efforts toward the discovery of functionally selective partial agonists of ADRB1 that have potential therapeutic value for AD and neuroinflammatory disorders, which has led to the identification of the molecule STD-101-D1. As a functionally selective agonist of ADRB1, STD-101-D1 produces partial agonistic activity on G protein signaling with an EC50 value in the low nanomolar range, but engages very little beta-arrestin recruitment compared to the unbiased agonist isoproterenol. STD-101-D1 also inhibits the tumor necrosis factor α (TNFα) response induced by lipopolysaccharide (LPS) both in vitro and in vivo, and shows high brain penetration. Other than the therapeutic role, this newly identified, functionally selective, partial agonist of ADRB1 is an invaluable research tool to study mechanisms of G protein-coupled receptor signal transduction.
