(±)-Butaclamol
(±)-Butaclamol (AY-23,028 free base; dl-Butaclamol) is the racemate of Butaclamol. Butaclamol is an orally active neuroleptic and a dopamine receptor antagonist. Butaclamol specifically blocks postsynaptic dopamine receptors and antagonizes dopaminergic neurotransmission, thereby exerting antipsychotic effects, and has very weak adrenergic receptor blocking activity. Butaclamol can be used in research on schizophrenia.
For research use only. We do not sell to patients.
- CAS No.: 36504-93-5
- Formula: C25H31NO
- Molecular Weight:361.52
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All Dopamine Receptor Isoforms
More
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Astrocyte | EC50 |
13.34 μM
Compound: 4
|
Antiproliferative activity against mouse astrocyte cells by MTT assay
Antiproliferative activity against mouse astrocyte cells by MTT assay
|
[PMID: 17417631] |
| Medulloblastoma cell | EC50 |
0.751 μM
Compound: 4
|
Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay
Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay
|
[PMID: 17417631] |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
-
Animal Model:Sprague-Dawley (male, 160-180 g)[1]
-
Dosage:0.16, 0.31, and 0.62 mg/kg
-
Administration:i.p.; single injection 15 min after d-amphetamine
-
Result:At 0.62 mg/kg i.p., amphetamine-induced stereotyped behavior was abolished within 30 min.
At 0.31 mg/kg, onset was slow and normal behavior occurred by 2 hr.
At 0.16 mg/kg, partial protection occurred.
The minimal effective dose was 0.62 mg/kg i.p.
-
Animal Model:Swiss albino (male, 18-22 g)[1]
-
Dosage:0.31, 0.62, and 1.25 mg/kg
-
Administration:i.p.; single injection 30 min before d-amphetamine
-
Result:Mortality at 24 hr was 60% at 0.31 mg/kg, 20% at 0.62 mg/kg, and 0% at 1.25 mg/kg i.p.
-
Animal Model:Sprague-Dawley (male, 250-400 g)[1]
-
Dosage:0.5 and 1.5 mg/kg
-
Administration:i.p.; single injection 30 min before testing
-
Result:Active avoidance failures were 32% at 0.5 mg/kg and 94% at 1.5 mg/kg.
Escape failures were 0% and 32%.
Discrimination failures were 0% and 2%, respectively.
-
Animal Model:Sprague-Dawley (male, 400-500 g)[1]
-
Dosage:0.05, 0.1, 0.2, and 0.4 mg/kg
-
Administration:i.p.; single injection; retested at 24 and 48 hr at 0.4 mg/kg
-
Result:Lever-pressing rate was reduced and shocks were increased in a dose-dependent manner.
Onset began 60 min after injection, and peak activity was recorded at the end of the 3-hr session.
At 0.4 mg/kg, avoidance remained strongly depressed at 24 hr, with rats avoiding less than 60% of shocks.
At 48 hr, behavior returned toward normal but did not reach pretreatment values.
-
Animal Model:Sprague-Dawley (male, 160-180 g)[1]
-
Dosage:7.5, 15, and 30 mg/kg
-
Administration:i.p.; single injection; evaluated at 1, 2, 4, and 6 hr
-
Result:Onset of catalepsy was dose-dependent, and peak activity occurred at 4 hr in every dose group.
At 6 hr the cataleptic effect declined in the 7.5 and 15 mg/kg groups.
-
Animal Model:albino (male; 23-25 g; Canadian Breeding Laboratories)[4]
-
Dosage:0.5 mg/kg (labelled-amine turnover); 2 mg/kg (labelled-amine turnover); 2 mg/kg (MT series)
-
Administration:i.p.; single dose
-
Result:At 2 mg/kg (i.p.), brain 14C-DA was reduced to 261 dpm/g and 14C-NA to 283 dpm/g (vehicle: 14C-DA 973 dpm/g; 14C-NA 474 dpm/g); brain tyrosine was 11.3 µg/g and tyrosine specific activity was 34 dpm/g.
At 0.5 mg/kg (i.p.), 14C-DA was reduced to 397 dpm/g (vehicle 874 dpm/g) but 14C-NA was not significantly reduced (721 dpm/g vs vehicle 732 dpm/g); brain tyrosine was 15.6 µg/g and tyrosine specific activity was 96 dpm/g.
In the MT series at 2 mg/kg, NA was 90.6% and DA 89.0% of control; with MT, NA was reduced to 44.9% and DA to 19.3% of control (MT alone: NA 57.4%, DA 43.0%; vehicle 100%).
No significant alterations in endogenous levels of NA and DA were observed.
The failure of labelled 14C-NA to fall at 0.5 mg/kg and the significant DA fall at both doses indicate preferential acceleration of DA turnover, with NA turnover affected only at 2 mg/kg.
Chemical Information
-
CAS No. 36504-93-5
-
Molecular Weight 361.52
-
Formula C25H31NO
-
SMILES
CC(C)([C@@]1(C[C@]2([H])C3=CC=CC4=C3[C@@](CN2CC1)([H])C5=CC=CC=C5CC4)O)C
-
Synonyms
AY-23,028 free base; dl-Butaclamol
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
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-165622 Related Classifications
Powered by Bioz
Keywords
- (±)-Butaclamol
- 36504-93-5
- AY-23,028
- dl-Butaclamol
- Dopamine Receptor
- amphetamine-induced stereotyped behavior
- apomorphine-induced emesis
- catalepsy
- conditioned avoidance behavior
- dopamine receptor antagonist
- dopamine turnover
- dopamine-stimulated adenyl cyclase
- postsynaptic dopamine receptors
- psychoses
- schizophrenia
- Inhibitor
- inhibitor
- inhibit