(+)-Butaclamol
(+)-Butaclamol ((+)-AY-23,028 free base; d-Butaclamol) is a dopamine receptor antagonist that blocks D2 and D1 receptors. (+)-Butaclamol antagonizes Dopamine (HY-B0451)-induced relaxation with a KB of 2 nM-0.17 µM and a Ki of 0.19-0.37 µM. (+)-Butaclamol inhibits adenylyl cyclase-coupled dopamine receptors, displaces striatal D2 radioligand binding, and acts as a non-selective D2 antagonist to retain D1-NLS and D1-D2 hetero-oligomers on the cell surface. (+)-Butaclamol inhibits the rewarding effects and self-administration behavior of dopaminergic agonists. (+)-Butaclamol can be used in research related to schizophrenia.
For research use only. We do not sell to patients.
- CAS No.: 56245-67-1
- Formula: C25H31NO
- Molecular Weight:361.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
Description
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D2 Receptor |
D1 Receptor |
In Vitro
(+)-Butaclamol antagonizes dopamine-induced relaxation in isolated rabbit splenic artery, with a KB of 4 nM[2].
(+)-Butaclamol (10-30 nM) competitively antagonizes dopamine-induced vasodilation in the isolated perfused rat kidney with a KB of 2 nM[2].
(+)-Butaclamol inhibits 3H-spiroperidol binding in rabbit renal artery and mesenteric artery membranes, with Ki values of 0.19 μM and 0.37 μM, respectively[2].
(+)-Butaclamol (500 nM-1 μM; 48 h) causes D1-NLS to remain on the cell surface in HEK cells, and nuclear translocation can subsequently occur after elution[3].
(+)-Butaclamol (1 μM) causes D1-IC1-NLS to be retained on the cell surface in HEK cells, but does not retain D1-IC3-NLS[3].
(+)-Butaclamol (1 μM; 24 h) causes D1/D1-NLS homooligomers to be retained on the cell surface in HEK cells, and upon removal, allows complete co-translocation to the nucleus[3].
(+)-Butaclamol (1 μM) retains the D1/D1 (S198A/S199A)-NLS complex on the cell surface in HEK cells, but after removal, the oligomer dissociates, D1 (S198A/S199A)-NLS moves to the nucleus, while D1 remains on the cell surface[3].
(+)-Butaclamol (1 μM) retains D1 (S198A/S199A)/D1 (S198A/S199A)-NLS homooligomers on the cell surface in HEK cells, and its removal permits complete nuclear co-translocation[3].
(+)-Butaclamol (1 μM) retains D1 (S199A/S202A)-NLS at the cell surface in HEK cells[3].
(+)-Butaclamol (1 μM) causes the D1/D1 (S199A/S202A)-NLS complex to be retained on the cell surface in HEK cells; after removal, the complex exhibits incomplete dissociation and undergoes nuclear co-translocation[3].
(+)-Butaclamol (10 nM-1 μM; 48 h) produces dose-dependent cell surface retention of HA-tagged D1-NLS in HEK cells[3].
(+)-Butaclamol (500 nM) causes amino-D2-NLS/D1 hetero-oligomers to remain on the cell surface in HEK cells, and upon removal, allows co-translocation to the nucleus[3].
(+)-Butaclamol (500 nM) causes the amino-D2-NLS/D1 (S198A/S199A) complex to transiently remain on the cell surface in HEK cells, but washout leads to dissociation rather than co-internalization[3].
(+)-Butaclamol (500 nM) retains amino-D2-NLS/D1 (S199A/S202A) hetero-oligomers on the cell surface in HEK cells, and after washing allows complete nuclear co-translocation[3].
(+)-Butaclamol (10 nM-100 μM) displaces [3H]SPIRO binding in rat fetal forebrain and striatal membranes, with stereoselectivity appearing around GD 18.5 and becoming fully established by PN day 5[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
(+)-Butaclamol (1.5 mg/kg; i.p.; daily; gestational days 14.5-17.5) reduces striatal [3H]SPIRO/D2 binding sites in PN 21 male offspring, but does not significantly alter striatal [3H]SPIRO/D2 binding parameters in the offspring[4].
(+)-Butaclamol (0.025-0.2 mg/kg; i.p.; single injection) dose-dependently inhibits Apomorphine (HY-12723) self-administration in rats, with higher doses terminating responding more rapidly without increasing response rates[5].
(+)-Butaclamol (0.05-0.1 mg/kg; i.p.; single injection) terminates self-administration of Piribedil (HY-12707) in rats without increasing response rates[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, 60-65 days old)[4]
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Dosage:1.5 mg/kg body wt
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Administration:28 days; 10-day washout
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Result:Striatal [3H]SPIRO binding sites in this compound-treated mature male rats were 352 fmol/mg protein.
Significantly increased the number of these D2 sites.
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Animal Model:Wistar (pregnant dams; male offspring at postnatal day 21)[4]
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Dosage:1.5 mg/kg body wt
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Administration:i.p.; daily; gestational days 14.5-17.5 or 17.5-19.5
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Result:In PN 21 male offspring, prenatal this compound produced striatal [3H]SPIRO binding Bmax 22.90 fmol/mg tissue and 151.3 fmol/mg protein; Kd 0.098 nM.
The Bmax was significantly reduced.
In PN 21 male offspring, prenatal this compound produced striatal [3H]SPIRO binding Bmax 35.45 fmol/mg tissue and 272.3 fmol/mg protein; Kd 0.100 nM.
No significant effect on kinetic parameters was detected.
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Animal Model:Sprague-Dawley[5]
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Dosage:0.025, 0.05, 0.1, and 0.2 mg/kg
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Administration:i.p.; Single dose
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Result:Administration of this compound to the animals responding for apomorphine resulted in a dose-dependent suppression of apomorphine responding.
Higher doses of this compound caused termination of apomorphine responding sooner than lower this compound doses.
No elevation in response rate was observed with this compound in any animals.
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Animal Model:Sprague-Dawley[5]
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Dosage:0.05 and 0.1 mg/kg
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Administration:i.p.; Single dose
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Result:Produced termination of piribedil responding, without a rate increase, in the few animals tested.
Chemical Information
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CAS No. 56245-67-1
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Molecular Weight 361.52
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Formula C25H31NO
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SMILES
CC(C)([C@]1(C[C@@]2([H])C3=CC=CC4=C3[C@](CN2CC1)([H])C5=CC=CC=C5CC4)O)C
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Synonyms
(+)-AY-23,028 free base; d-Butaclamol
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
(+)-Butaclamol Related Classifications
HY-122979A Related Classifications
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