Details
| Stereochemistry | UNKNOWN |
| Molecular Formula | C28H33ClN2 |
| Molecular Weight | 433.028 |
| Optical Activity | ( - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)(C)C1=CC=C(CN2CCN(CC2)C(C3=CC=CC=C3)C4=CC=C(Cl)C=C4)C=C1
InChI
InChIKey=MOYGZHXDRJNJEP-UHFFFAOYSA-N
InChI=1S/C28H33ClN2/c1-28(2,3)25-13-9-22(10-14-25)21-30-17-19-31(20-18-30)27(23-7-5-4-6-8-23)24-11-15-26(29)16-12-24/h4-16,27H,17-21H2,1-3H3
| Molecular Formula | C28H33ClN2 |
| Molecular Weight | 433.028 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
DescriptionCurator's Comment: description was created based on several sources, including: https://www.ncbi.nlm.nih.gov/pubmed/22469258 | http://edudrugs.com/B/Bucladin-S.html
Curator's Comment: description was created based on several sources, including: https://www.ncbi.nlm.nih.gov/pubmed/22469258 | http://edudrugs.com/B/Bucladin-S.html
Buclizine, a piperazine derivative, is a sedating antihistamine with antimuscarinic and moderate sedative action. The drug is used mainly for its antiemetic action, particularly in the prevention of motion sickness, and in the treatment of migraine in combination with analgesics. The following side/adverse effects have been selected on the basis of their potential clinical significance: drowsiness; Incidence less frequent; blurred vision; dryness of mouth, nose, and throat; headache; nervousness, restlessness, or trouble in sleeping; upset stomach. The following drug interactions have been selected on the basis of their potential clinical significance: alcohol; anticholinergics or other medications with anticholinergic activity; apomorphine.
CNS Activity
Sources: http://www.pharmacorama.com/en/Sections/Histamin_3.php | https://www.ncbi.nlm.nih.gov/pubmed/20515533
Curator's Comment: Buclizine is the drug of the first antihistamine generation.Firstgeneration histamine H1-receptor antagonists readily penetrate the blood brain barrier and produce histamine blockade at histamine H1-receptors in the central nervous system.
Originator
Sources: https://www.google.com/patents/US2709169
Curator's Comment: https://www.ncbi.nlm.nih.gov/pubmed/22469258
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL231 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Preventing | BUCLADIN-S Approved UseFor prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness and vertigo (dizziness caused by other medical problems). |
|||
Sources: http://edudrugs.com/B/Bucladin-S/more.html |
Preventing | BUCLADIN-S Approved UseFor prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness and vertigo (dizziness caused by other medical problems). |
||
| Palliative | Migraleve pink Approved UseTreating nausea and headache associated with migraine attacks that are not relieved by paracetamol, ibuprofen or aspirin alone. Launch Date2015 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.45 μg/mL |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
BUCLIZINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
5.22 μg × h/mL |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
BUCLIZINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
5.3 h |
25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered: |
BUCLIZINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method. | 2010-12 |
|
| Simultaneous determination of gliquidone, fexofenadine, buclizine, and levocetirizine in dosage formulation and human serum by RP-HPLC. | 2010-06-03 |
|
| Quantitation of buclizine hydrochloride in pharmaceutical formulations and human serum by RP-HPLC. | 2006-10 |
Patents
Sample Use Guides
50 mg thirty minutes before travel. Dose may be repeated every four to six hours as needed. Usual adult prescribing limits - up to 150 mg daily.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26921194
Treatment of MCF-7 cells with different concentrations for 72 h showed that buclizine (IC50: 19.18 ± 5.32 μM) revealed considerable growth inhibition.
| Substance Class |
Chemical
Created
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admin
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Edited
Mon Mar 31 20:52:14 GMT 2025
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Mon Mar 31 20:52:14 GMT 2025
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| Record UNII |
1178B2VD9B
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| Record Status |
Validated (UNII)
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| Record Version |
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