[CAS NO. 102394-31-0] Otenzepad
PRODUCTS SPECIFICATIONS [102394-31-0]
DESCRIPTION [102394-31-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 421.54 |
| Molecular Formula | C24H31N5O2 |
| SMILES | O=C1NC2=CC=CN=C2N(C(CN3C(CN(CC)CC)CCCC3)=O)C4=CC=CC=C14 |
Summary
Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC 50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively [1] .
IC50 & Target
640 nM (M2 muscarinic acetylcholine receptor in rabbit peripheral lung), 386 nM (M2 muscarinic acetylcholine receptor in rat heart) [1] .
In Vivo
Otenzepad (0.5, 1 mg/kg, s.c., in rats) significantly improved win-stay acquisition relative to vehicle-injected controls
[2]
.
Otenzepad (2 mg/kg, s.c., in rats) significantly improved retention relative to vehicle controls
[2]
.
Otenzepad (0.3, 1.0, or 3.0 mg/kg, ip, in mice) potentiates the effects of glucose and reverses the effects of insulin on memory
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Forty-eight male Long-Evans rats (325-350 g) [2] . |
| Dosage: | 0.25, 0.5, 1.0 and 2.0 mg/kg. |
| Administration: | S.C. on the dorsum of the neck once. |
| Result: | Doses of 0.5 and 1.0 mg/kg significantly improved acquisition relative to vehicle controls, while doses of 0.25 and 2.0 mg/kg had no effect. |
| Animal Model: | Adult male Swiss mice (age 60–70 days; weight 25-30 g) [3] . |
| Dosage: | 0.3, 1.0, or 3.0 mg/kg. |
| Administration: | IP once. |
| Result: | Enhanced retention in an inverted-U dose–response manner, with significant enhancement seen at 1.0 mg/kg (U 15,15 = 49, p < 0.02, compared with saline-saline-injected control group). |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 25 mg/mL ( 59.31 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3723 mL | 11.8613 mL | 23.7225 mL |
| 5 mM | 0.4745 mL | 2.3723 mL | 4.7445 mL |
| 10 mM | 0.2372 mL | 1.1861 mL | 2.3723 mL |
References
- [1] Bloom JW, et al. Heterogeneity of the M1 muscarinic receptor subtype between peripheral lung and cerebral cortex demonstrated by the selective antagonist AF-DX 116. Life Sci. 1987 Jul 27;41(4):491-6.
- [2] Packard MG, et al. Post-training injection of the acetylcholine M2 receptor antagonist AF-DX 116 improves memory. Brain Res. 1990 Jul 30;524(1):72-6.
- [3] Kopf SR, et al. AF-DX 116, a presynaptic muscarinic receptor antagonist, potentiates the effects of glucose and reverses the effects of insulin on memory. Neurobiol Learn Mem. 1998 Nov;70(3):305-13.
Synonyms