2,5-Bis(3,4-dimethoxybenzyl)cyclopentylamine, a peripheral dopamine blocking agent.
J Med Chem
; 21(12): 1318-20, 1978 Dec.
Article
in En
| MEDLINE
| ID: mdl-569208
ABSTRACT
2,5-Bis(3,4-dimethoxybenzyl)cyclopentylamine hydrochloride has been synthesized. The intermediate 2,5-bis-(3,4-dimethoxybenzyl)cyclopentanone was formed in 91.8% yield using a sodium methoxide catalyzed aldol condensation and catalytic reduction. The oxime of this ketone was catalytically hydrogenated to the amine which was converted to the hydrochloride (76%). The amine hydrochloride was found to be an effective antagonist to the low-dose hypotensive effect of dopamine; the half-life of this effect was 18 min. At dopamine doses of 3 mg/kg in the atropinized and phenoxybenzamine treated dog, the ED50 for blockade was 4--5 mumol/kg. In direct contrast to its peripheral dopamine blocking activity, the compound potentiates apomorphine-induced stereotypy.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Dopamine Antagonists
/
Cyclopentanes
/
Amines
Limits:
Animals
/
Female
/
Humans
/
Male
Language:
En
Journal:
J Med Chem
Journal subject:
QUIMICA
Year:
1978
Document type:
Article