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moxisylyte

Small moleculeexperimental

Clinical trial activity

0 trials · 0 clinical orgs · 0 marketing orgs

Phase 1

0

Phase 2

0

Phase 3

0

Phase 4

0

Mechanism of action

Adrenergic receptor alphaANTAGONIST
Adrenergic receptor alpha antagonist
Moxisylyte reduces or blocks the response to adrenaline. Because of its alpha-blocking properties, it competitively inhibits the effects of noradrenaline without effect on beta and 5-hydroxytriptamine receptors.
Moderate specificity for alpha-1 receptors. IC50 value of 86 nM was obtained for native alpha 1A subtypes from rat submaxillary gland and an IC50 value of 39 nM for native alpha-1B subtypes from rat liver. No affinity for beta adrenoceptors, D1, 5HT1A and 5HT2 receptors and moderate affinity for H1 receptors. On the native receptor subtypes also, deacetylmoxisylyte (DAM), the main active metabolite, had the same affinity as moxisylyte (IC50=25 nM for alpha1A subtypes and 34nM for alpha1B subtypes)

Chemistry & pharmacology

Loading structure…

SMILES

CC(=O)Oc1cc(C(C)C)c(OCCN(C)C)cc1C

Mol. weight: 279.38 g/mol
Lipinski Ro5: Pass
Rule of 3: No
Chirality: Achiral Molecule
Inorganic: No
Polymer: No
Delivery: Oral

Oral

Yes

Parenteral

No

Topical

No

Sources

ChEMBLCHEMBL159226 ↗
ChEMBLCHEMBL1256739 ↗

Also known as