Jump to content
 







Main menu
    


Navigation  


●Main page
 ●Contents
 ●Current events
 ●Random article
 ●About Wikipedia
 ●Contact us
 ●Donate
  



Contribute  


●Help
 ●Learn to edit
 ●Community portal
 ●Recent changes
 ●Upload file
  







Search  

































●Create account

●Log in
 









●Create account
 ● Log in
  



Pages for logged out editors learn more  


●Contributions
 ●Talk
  


















Contents

   



(Top)
  


1 Pharmacodynamics  




2 See also  




3 References  













Otenzepad






●فارسی
  
Edit links
  








●Article
 ●Talk
  
















●Read
 ●Edit
 ●View history
  







Tools
    


Actions  


●Read
 ●Edit
 ●View history
  



General  


●What links here
 ●Related changes
 ●Upload file
 ●Special pages
 ●Permanent link
 ●Page information
 ●Cite this page
 ●Get shortened URL
 ●Download QR code
 ●Wikidata item
  



Print/export  


●Download as PDF
 ●Printable version
  















Appearance
    

 





From Wikipedia, the free encyclopedia
  

Otenzepad
Structure of Otenzepad
Clinical data
Routes of
administration		oral
Pharmacokinetic data
Bioavailability45% (oral)[1]
Elimination half-life2.5h
Identifiers

  • 11-[2-[2-(diethylaminomethyl)piperidin-1-yl]acetyl]-5H-pyrido[2,3-b][1,4]benzodiazepin-6-one

CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.220.541 Edit this at Wikidata
Chemical and physical data
FormulaC24H31N5O2
Molar mass421.545 g·mol−1
3D model (JSmol)

  • CCN(CC)CC1CCCCN1CC(=O)N2C3=CC=CC=C3C(=O)NC4=C2N=CC=C4

  • InChI=1S/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)

  • Key:UBRKDAVQCKZSPO-UHFFFAOYSA-N

Otenzepad is a competitive muscarinic receptor antagonist that is relatively selective at the M2 receptor. It was investigated as a treatment for arrhythmia and bradycardia due to its cardioselectivity but research ceased after stage III clinical trials. The drug was originally developed by the German pharmaceutical company, Boehringer Ingelheim Pharma KG.[1]

Pharmacodynamics[edit]

The (+)-enantiomer has 8 times greater potency at the M2 receptor than the (-)-enantiomer.[1]

Potency of Otenzepad at muscarinic receptor isoforms[1]
mAChR isoform Dissociation constant (Ki)
M1 537.0 - 1300nM[1][2]
M2 81.0 - 186nM[1][2]
M3 838 - 2089.0nM[2][1]
M4 407.0 - 1800nM[1][2]
M5 2800nM[2]


See also[edit]

References[edit]

  1. ^ a b c d e f g h "Otenzepad". National Centre for Advancing Translational Sciences. Retrieved 10 June 2021.
  • ^ a b c d e Buckley NJ, Bonner TI, Buckley CM, Brann MR (1989). "Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells". Mol. Pharmacol. 35 (4): 469–76. PMID 2704370.

    • Retrieved from "https://en.wikipedia.org/w/index.php?title=Otenzepad&oldid=1108875742"
    Categories: 
    ●Pyridobenzodiazepines
     ●Piperidines
     ●Tertiary amines
     Hidden categories: 
    ●Articles with short description
     ●Short description is different from Wikidata
     ●ECHA InfoCard ID from Wikidata
     ●Chemical pages without DrugBank identifier
     ●Articles without KEGG source
     ●Drugs missing an ATC code
     ●Drugs with no legal status
     ●Articles containing unverified chemical infoboxes
      


    ●This page was last edited on 6 September 2022, at 18:54 (UTC).
    ●Text is available under the Creative Commons Attribution-ShareAlike License 4.0; additional terms may apply. By using this site, you agree to the Terms of Use and Privacy Policy. Wikipedia® is a registered trademark of the Wikimedia Foundation, Inc., a non-profit organization.


    ●Privacy policy
    ●About Wikipedia
    ●Disclaimers
    ●Contact Wikipedia
    ●Code of Conduct
    ●Developers
    ●Statistics
    ●Cookie statement
    ●Mobile view


    Wikimedia Foundation
    Powered by MediaWiki