Axelopran
Axelopran (TD-1211) is an orally active opioid receptor antagonist. Axelopran binds to human μ-, δ-, and κ-opioid receptors with pKi values of 9.8, 8.8, and 9.9, respectively. Axelopran (sulfate) blocks μ-opioid receptor agonist signaling, reverses opioid-induced gastrointestinal inhibition, and inhibits agonist-induced opioid receptor G protein activation. Axelopran can be used for research on opioid-induced constipation.
For research use only. We do not sell to patients.
- CAS No.: 949904-48-7
- Formula: C26H39N3O4
- Molecular Weight:457.61
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All Opioid Receptor Isoforms
More
Biological Activity
Description
|
μ Opioid Receptor/MOR |
κ Opioid Receptor/KOR |
δ Opioid Receptor/DOR |
In Vitro
Axelopran acts as a potent antagonist in agonist-induced GTPγS binding assays at recombinant μ, δ, and κ opioid receptors (pKb = 9.6, 8.8, and 9.5, respectively)[1].
Axelopran is a P-gp substrate in Caco-2 and MDR1-MDCK cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Axelopran (0.24 mg/kg; p.o.) reverses Loperamide (HY-156131)-induced delayed gastric emptying in rats[1].
Axelopran (0.01 mg/kg; p.o.) inhibits Castor oil (HY-107799)-induced diarrhea in rats[1].
Axelopran (3 mg/kg) inhibits non-productive gastrointestinal circular smooth muscle contractility in dogs[1].
Axelopran (0.03-10 mg/kg; p.o.; single administration) reverses Loperamide-induced delayed gastric emptying in rats, with an oral ED50 of 0.24 mg/kg[2].
Axelopran (0.001-0.3 mg/kg; p.o.; single administration) reverses loperamide-induced antidiarrheal activity in the rat Castor oil model, with an oral ED50 of 0.01 mg/kg[2].
Axelopran (0.03-3 mg/kg; p.o.; single administration) attenuates Loperamide-induced gastrointestinal hypermotility in dogs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Rat[1]
-
Dosage:ID50 0.24 mg/kg
-
Administration:p.o.
-
Result:Reversed loperamide-induced delay in gastric emptying with an ID50 of 0.24 mg/kg.
-
Animal Model:Rat[1]
-
Dosage:ID50 0.01 mg/kg
-
Administration:p.o.
-
Result:Inhibited castor oil-induced diarrhea with an ID50 of 0.01 mg/kg.
-
Animal Model:Sprague-Dawley (male, 150-350 g)[2]
-
Dosage:0.03-10 mg/kg
-
Administration:p.o.; single dose
-
Result:Produced dose-dependent reversal of loperamide-induced inhibition of gastric emptying.
The oral dose producing 50% reversal was 0.24 mg/kg.
The hot plate/gastric emptying peripheral selectivity index was >250.
-
Animal Model:Sprague-Dawley (male, 150-350 g)[2]
-
Dosage:0.001-0.3 mg/kg
-
Administration:p.o.; single dose
-
Result:Produced dose-dependent reversal of loperamide’s antidiarrheal activity.
The oral dose producing 50% reversal was 0.01 mg/kg.
The hot plate/castor oil peripheral selectivity index was >6,000.
-
Animal Model:Beagle (female, 6.5-8.5 kg)[2]
-
Dosage:0.03, 0.3, and 3 mg/kg
-
Administration:p.o.; single dose
-
Result:Attenuated Loperamide-induced increased contractility in the antrum, duodenum, and jejunum.
The inhibitory effect was dose-dependent.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 949904-48-7
-
Molecular Weight 457.61
-
Formula C26H39N3O4
-
SMILES
O=C([C@@H](O)CO)N(CC1CCCCC1)CCN2[C@H]3C[C@H](C4=CC(C(N)=O)=CC=C4)C[C@@H]2CC3
-
Synonyms
TD-1211
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Axelopran Related Classifications
HY-16765 Related Classifications
Powered by Bioz