Alentemol
Alentemol (U-66444B (free base)) is a blood-brain barrier-permeable dopamine receptor D1, D2, D3, and D4 agonist. Alentemol inhibits dopamine release, reduces dopamine synthesis, regulates dopamine metabolism, suppresses the impulse activity of dopaminergic neurons, and decreases the impulse frequency of dopaminergic neurons in the substantia nigra pars compacta and ventral tegmental area. Alentemol is applicable to research related to schizophrenia.
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- CAS No.: 112891-97-1
- Formule: C19H25NO
- Masse moléculaire:283.41
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
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D1 Receptor |
D2 Receptor |
D3 Receptor |
D4 Receptor |
In Vivo
Alentemol (0.001-0.1 mg/kg; s.c.) inhibits dopamine synthesis in healthy male Sprague-Dawley rats, with enhanced efficacy when presynaptic terminals are isolated from postsynaptic feedback via gamma-butyrolactone[1].
Alentemol (3.0 μg/kg; i.v.; single dose; 6 mg/kg; daily; 14 days) acts as a potent dopaminergic autoreceptor agonist with an ED50 of 3.0 μg/kg i.v. for inhibiting SNPC neurons, three times more potent than Apomorphine (HY-12723), and shows weak tolerance development following 14 days of daily 6 mg/kg administration[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CF-1 (male, 18-22 g; 25-35 g for striatal 3-methoxytyramine studies)[1]
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Dosage:10.0 mg/kg (hypothermia testing); 0.001-10.0 mg/kg (locomotor activity inhibition); 0.0001-0.1 mg/kg (d-amphetamine-stimulated locomotor activity antagonism); 0.0001-0.1 mg/kg (striatal 3-methoxytyramine measurement); 1.0 mg/kg (brain concentration analysis)
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Administration:i.p. (hypothermia testing); s.c. (locomotor activity inhibition, d-amphetamine-stimulated locomotor activity antagonism, striatal 3-methoxytyramine measurement, single dose for brain concentration analysis); p.o. (single dose for brain concentration analysis)
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Result:Induced hypothermia, an effect blocked by haloperidol but not yohimbine.
Inhibited locomotor activity by 24% at 10.0 mg/kg, 25% at 3.0 mg/kg, 50% at 1.0 mg/kg, 33% at 0.3 mg/kg, 63% at 0.1 mg/kg, 62% at 0.03 mg/kg, 56% at 0.01 mg/kg, 54% at 0.003 mg/kg, and 28% at 0.001 mg/kg; this inhibition was blocked by haloperidol at 0.02 mg/kg.
Antagonized d-amphetamine-stimulated locomotor activity by 82% at 0.1 mg/kg, 69% at 0.01 mg/kg, 52% at 0.003 mg/kg, 26% at 0.001 mg/kg, and 48% at 0.0003 mg/kg.
Reduced striatal 3-methoxytyramine (an index of dopamine release) to 26% of control at 0.1 mg/kg, 52% of control at 0.01 mg/kg, and 70% of control at 0.001 mg/kg.
Achieved brain concentrations of 116 ng/g at 30 minutes, 40 ng/g at 60 minutes, and 13 ng/g at 120 minutes after 1.0 mg/kg s.c. administration; achieved a brain concentration of 27 ng/g at 60 minutes after 1.0 mg/kg p.o. administration.
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Animal Model:Sprague-Dawley (male, approximately 150 g)[1]
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Dosage:0.001-0.1 mg/kg
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Administration:s.c.
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Result:Reduced striatal DOPA concentration (an index of dopamine synthesis) to 34% of control at 0.1 mg/kg and 62% of control at 0.01 mg/kg; 0.001 mg/kg resulted in striatal DOPA levels at 74% of control.
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Animal Model:Sprague-Dawley (male, 300-400 g, chloral hydrate-anesthetized)[2]
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Dosage:3.0 μg/kg (acute electrophysiology); 6 mg/kg (chronic tolerance assessment)
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Administration:i.v.; single dose (acute electrophysiology); daily; 14 days (chronic tolerance assessment)
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Result:Depressed dopaminergic neurons in SNPC and VTA with three times the potency of Apomorphine.
Inhibited SNPC neurons with an ED50 of 3.0 μg/kg i.v.
Induced similar responses in dopaminergic cells in the VTA.
Had its induced inhibition of SNPC and VTA cells reversed by haloperidol.
Showed weak propensity to produce tolerance, as chronically treated rats still responded to its potent dopaminergic autoreceptor agonist effects.
Chemical Information
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CAS No. 112891-97-1
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Masse moléculaire 283.41
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Formule C19H25NO
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SMILES
OC1=CC2=C3C(CC(N(CCC)CCC)C2)=CC=CC3=C1
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Synonyms
U-66444B free base
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Alentemol Related Classifications
HY-124524 Related Classifications
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