A marine sponge alkaloid; an agonist of δ- and μ-opioid receptors (EC50s = 5.1 and 10.1 μM

Aaptamine – 1 mg

Brand:
Cayman
CAS:
85547-22-4
Storage:
-80
UN-No:
Non-Hazardous - /

Aaptamine is a marine sponge alkaloid originally isolated from A. aaptos with diverse biological activities, including antiproliferative and antidepressant properties.{47125,47126,47127,47128} It is an agonist of δ- and μ-opioid receptors (EC50s = 5.1 and 10.1 μM, respectively, in HEK293 cells expressing human recombinant receptors) and a competitive antagonist of α-adrenergic receptors (α-ARs; pA2s = 4.88 and 5.43, respectively, in isolated rabbit aorta and renal artery).{47125,47128} Aaptamine inhibits growth of HeLa cervical cancer (IC50 = 15 μg/ml) and K562 leukemia (GI50 = 10 μM) cells and induces cell cycle arrest in the G2/M phase in K562 leukemia and MG63 osteosarcoma cells.{47126,47127,47129} It is a proteasome inhibitor that inhibits chymotrypsin-, caspase-, and trypsin-like activity in a partially purified rat liver proteasome preparation (IC50s = 1.6, 2.7, and 18 μg/ml, respectively) and dose-dependently activates p21 independent of p53 in MG63 cells when used at concentrations ranging from 20 to 50 μM.{47126,47129} Aaptamine (40 mg/kg, i.p.) decreases immobility time in the forced swim test in mice, indicating antidepressant-like activity.{47128}  

 

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Description

A marine sponge alkaloid; an agonist of δ- and μ-opioid receptors (EC50s = 5.1 and 10.1 μM, respectively, in HEK293 cells expressing human recombinant receptors); a competitive antagonist of α-ARs (pA2s = 4.88 and 5.43, respectively, in isolated rabbit aorta and renal artery); inhibits growth of HeLa cervical cancer (IC50 = 15 μg/ml) and K562 leukemia (GI50 = 10 μM) cells; induces cell cycle arrest in the G2/M phase in K562 leukemia and MG63 osteosarcoma cells; inhibits chymotrypsin-, caspase-, and trypsin-like activity in a partially purified rat liver proteasome preparation (IC50s = 1.6, 2.7, and 18 μg/ml, respectively); dose-dependently activates p21 independent of p53 in MG63 cells from 20-50 μM; decreases immobility time in the forced swim test in mice at 40 mg/kg

Formal name: 8,9-dimethoxy-1H-benzo[de][1,6]naphthyridine

Synonyms: 

Molecular weight: 228.3

CAS: 85547-22-4

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Natural Products||Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Neuroscience|Behavioral Neuroscience|Depression

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