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]
 Structure of Otenzepad | |
| Clinical data | |
|---|---|
| Routes of administration | oral |
| Pharmacokinetic data | |
| Bioavailability | 45% (oral)[1] |
| Elimination half-life | 2.5h |
| Identifiers | |
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| IUPHAR/BPS | |
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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.220.541 |
| Chemical and physical data | |
| Formula | C24H31N5O2 |
| Molar mass | 421.545 g·mol−1 |
| 3D model (JSmol) | |
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Pharmacodynamics
editThe (+)-enantiomer has 8 times greater potency at the M2 receptor than the (-)-enantiomer.[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
editReferences
edit- ^ 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.