102394-31-0 Usage
Uses
Used in Pharmaceutical Research:
AF-DX 116 is used as an M2 muscarinic acetylcholine receptor (M2AChR) selective antagonist for investigating the influence of M2AChR in the regulation of both basal and carbachol-stimulated long-term potentiation at the dentate gyrus (DG-LTP) and pro-nerve growth factor (proNGF) secretion in hippocampal cells of young diabetic rats. This application helps researchers understand the role of M2AChR in cognitive function and neurodegenerative diseases, potentially leading to the development of new therapeutic strategies.
Used in Neuroscience:
In the field of neuroscience, AF-DX 116 is used as a research tool to study the role of M2AChR in synaptic plasticity and memory formation. By selectively blocking the M2AChR, researchers can gain insights into the underlying mechanisms of cognitive processes and the potential therapeutic effects of modulating this receptor.
Used in Drug Development:
AF-DX 116 is also used in the development of new drugs targeting the M2 muscarinic acetylcholine receptor. As a selective antagonist, it can be used to test the efficacy and safety of new compounds designed to modulate M2AChR activity, potentially leading to the development of novel treatments for conditions such as Alzheimer's disease, schizophrenia, and other cognitive disorders.
Biological Activity
Selective M 2 muscarinic receptor antagonist. K i values are 64, 417, 786, 211 and 5130 nM for human recombinant M 2 , M 1 , M 3 , M 4 and M 5 muscarinic receptors, respectively.
Biochem/physiol Actions
AF-DX 116 raises blood pressure and heart rate in a rat model of hypotension induced by repeated cold stress. Thus, it may be used as a therapeutic for hypotension related to vagotonia type autonomic dysfunction.
Check Digit Verification of cas no
The CAS Registry Mumber 102394-31-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,0,2,3,9 and 4 respectively; the second part has 2 digits, 3 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 102394-31:
(8*1)+(7*0)+(6*2)+(5*3)+(4*9)+(3*4)+(2*3)+(1*1)=90
90 % 10 = 0
So 102394-31-0 is a valid CAS Registry Number.
InChI:InChI=1/C24H31N5O2/c1-3-27(4-2)16-18-10-7-8-15-28(18)17-22(30)29-21-13-6-5-11-19(21)24(31)26-20-12-9-14-25-23(20)29/h5-6,9,11-14,18H,3-4,7-8,10,15-17H2,1-2H3,(H,26,31)
102394-31-0Relevant articles and documents
Tricyclic Compounds as Selective Muscarinic Receptor Antagonists. 3. Structure-Selectivity Relationships in a Series of Cardioselective (M2) Antimuscarinics
Engel, Wolfhard W.,Eberlein, Wolfgang G.,Mihm, Gerhard,Hammer, Rudolf,Trummlitz, Guenter
, p. 1718 - 1724 (2007/10/02)
On the basis of the cardioselective muscarinic receptor antagonist AF-DX 116 (2), a series of 11-substituted pyridobenzodiazepinones (9-35) was prepared and screened for their binding affinity to muscarinic receptors located in cardiac (M2) and glandular (M3) tissue.The ratio of IC50 values of the test compounds in the two different tissues was taken as a measure of cardiac (M2) receptor selectivity.Qualitative structure-selectivity relationships point to the fact that it is the spartial orientation of the protonated side-chain nitrogen atom in relation to the tricycle that is the main determinant for receptor subtype recognition and hence is important for the achievement of cardiac (M2) selectivity.
CONDENSED DIAZEPINONES, THEIR COMPOSITIONS AND METHODS OF USE AS PHARMACEUTICALS
-
, (2008/06/13)
Disclosed are novel condensed diazepinones of formula I STR1 wherein B is a fused ring selected from STR2 X is--CH--or, when B is ortho-phenylene, X can also be nitrogen; A 1 is C 1-C. sub.2 alkylene; A 2 is C 1-C 2 when it is in the 2-position relative to the saturated heterocyclic ring nitrogen or a single bond or methylene when it is in the 3-or 4-position; R 1 is C 1-C 3 alkyl; R 2 is C. sub.1-C 7 alkyl, optionally hydroxy-substituted on at least one of its second to seventh carbon, or C 3-C 7 cycloalkyl, optionally hydroxy substituted, or C 3-C 7 cycloalkylmethyl; or R 1 and R 2 can, together with the nitrogen therebetween, be a 4-to 7-membered saturated monocyclic, heterocyclic ring which can optionally include an oxygen or N--CH 3 ; R 3 is hydrogen, chlorine, or methyl; R 4 is hydrogen or C 1-C 4 alkyl, R 5 is hydrogen, chlorine or C 1-C 4 alkyl; and Z is a single bond, oxygen, methylene or 1,2-ethylene; and NR 1 R 2--N oxides and nontoxic, pharmaceutically acceptable addition salts thereof. Also disclosed are pyrrolobenzodiazepinone intermediates, pharmaceutical compositions containing the condensed diazepinones and methods of using them to treat cardiovascular disorders, particularly bradycardia and bradyarrhythmia.
