Stimulatory effect of cinnamic acid analogues on α1A-adrenoceptors in-vitro

Huang Kuang Chang, Feng Lin Hsu, I. Min Liu, Juei Tang Cheng

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

We have characterized the effects of cinnamic acid and its derivatives on α1A-adrenoceptor subtypes. The cinnamic acid with a methoxyl group and/or a hydroxyl group showed the ability to stimulate radioactive glucose uptake into C2C12 cells, a cell line that specifically expresses the α1A-adrenoceptor subtype of α1-adrenoceptors. However, cinnamic acid without chemical modification diminished the glucose uptake into C2C12 cells. It was shown that methoxylation and/or hydroxylation of cinnamic acid had higher affinities for α1A-adrenoceptors investigated using [3H]prazosin binding experiments in C2C12 cells. The effect of these derivatives on α1A-adrenoceptors was further characterized using the displacement of [3H]prazosin binding in rat prostate. We found that 3,5-dimethoxy-4-hydroxycinnamic acid, the cinnamic acid derivative with two methoxyl groups and hydroxylation at the fourth carbon on the benzene ring, had a higher affinity for the α1A-adrenoceptor subtype, showing a smaller IC50 value (the concentration for production of 50% inhibition) to displace [3H]prazosin-binding in rat prostate. Affinity of these compounds for α1B-adrenoceptors was identified using [3H]prazosin-binding experiments in rat spleen. However, we found no marked differences in the IC50 values between these cinnamic acid analogues to displace the [3H]prazosin binding in rat spleen. In conclusion, our data indicated that methoxylation and/or hydroxylation of cinnamic acid might raise the affinity for α1A-adrenoceptors.

Original languageEnglish
Pages (from-to)833-837
Number of pages5
JournalJournal of Pharmacy and Pharmacology
Volume55
Issue number6
DOIs
Publication statusPublished - Jun 1 2003

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Adrenergic Receptors
Prazosin
Hydroxylation
Inhibitory Concentration 50
Prostate
Spleen
Glucose
cinnamic acid
In Vitro Techniques
Benzene
Hydroxyl Radical
Carbon
Cell Line

ASJC Scopus subject areas

  • Pharmacology
  • Pharmaceutical Science

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Stimulatory effect of cinnamic acid analogues on α1A-adrenoceptors in-vitro. / Chang, Huang Kuang; Hsu, Feng Lin; Liu, I. Min; Cheng, Juei Tang.

In: Journal of Pharmacy and Pharmacology, Vol. 55, No. 6, 01.06.2003, p. 833-837.

Research output: Contribution to journalArticle

Chang, Huang Kuang ; Hsu, Feng Lin ; Liu, I. Min ; Cheng, Juei Tang. / Stimulatory effect of cinnamic acid analogues on α1A-adrenoceptors in-vitro. In: Journal of Pharmacy and Pharmacology. 2003 ; Vol. 55, No. 6. pp. 833-837.
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