isoxsuprine
Isoxsuprine (used as isoxsuprine hydrochloride) is a drug used as a vasodilator in humans (under the trade name Duvadilan) and equines. Isoxsuprine is a β2 adrenoreceptor agonist that causes direct relaxation of uterine and vascular smooth muscle via β2 receptors. Isoxsuprine it is used in humans for treatment of premature labor, i.e. a tocolytic, and as a vasodilator for the treatment of cerebral vascular insufficiency, Raynaud's phenomenon, and other conditions. Isoxsuprine may increase the heart rate, cause changes in blood pressure, and irritate the GI tract. It should, therefore, be used with caution if combined with other drugs that affect blood pressure, such as sedatives and anesthetic drugs. Isoxsuprine is most commonly used to treat hoof-related problems in the horse, most commonly for laminitis and navicular disease, as its effects as a vasodilator are thought to increase circulation within the hoof to help counteract the problems associated with these conditions. — NCATS
Clinical trial activity
1 trials · 1 clinical orgs · 0 marketing orgs
Earliest trial started Feb 15, 2019 (NCT03752307)
Timeline
2010s
- Jan 1, 2019
Earliest Phase 1 Sponsor(trial)
Indications
Studied for
Mechanism of action
- Beta-2 adrenergic receptorAGONIST
ADRB2 agonist
Isoxsuprine is a beta-adrenoreceptor agonist and an alpha-adrenoreceptor antagonist, with both characteristics contributing to vasodilation and uterine relaxation.
Isoxsuprine has a higher affinity of ¿1-adrenoreceptors (Kd=59+-15nM, adrenoreceptors in rat vas deferens) than for ß2-adrenoceptors ( Kd=3900+-500nM adrenoreceptors in rat vas deferens).
- Adrenergic receptor alpha-1ANTAGONIST
Adrenergic receptor alpha-1 antagonist
Isoxsuprine is a beta-adrenoreceptor agonist and an alpha-adrenoreceptor antagonist, with both characteristics contributing to vasodilation and uterine relaxation.
Isoxsuprine has a higher affinity of ¿1-adrenoreceptors (Kd=59+-15nM, adrenoreceptors in rat vas deferens) than for ß2-adrenoceptors ( Kd=3900+-500nM adrenoreceptors in rat vas deferens).
Chemistry & pharmacology
SMILES
CC(COc1ccccc1)NC(C)C(O)c1ccc(O)cc1- Mol. weight
- 301.39 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL1197051 ↗
- WikipediaIsoxsuprine ↗
- NCATSR15UI3245N ↗
- ChEMBLCHEMBL559180 ↗
- ChEMBLCHEMBL2103925 ↗
Also known as
- defencin
- dilavase
- duvadilan
- duvadilan
- duvadilan
- duvadilan
- duvadilan
- duvadilan
- duvadilan ret
- isoxsuprine
- isoxsuprine
- isoxsuprine
- isoxsuprine
- isoxsuprine
- isoxsuprine
- isoxsuprine
- isoxsuprine
- isoxsuprine hcl
- isoxsuprine hcl
- isoxsuprine hcl
- isoxsuprine hydrochloride
- isoxuprine
- (r/s) isoxsuprine hydrochloride
- vadosilan
- vasodilan
- vasodilan
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03752307 | Phase 1/Phase 2 (Phase 2) | Feb 15, 2019 | University of New Mexico |
Organizations
Research & Development (1)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| University of New Mexico | Academic/Hospital | 1 | 1 | 1 | 2019 |