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  • Structure-activity relationship of gramine derivatives in Ca(2+) release from sarcoplasmic reticulum.

Structure-activity relationship of gramine derivatives in Ca(2+) release from sarcoplasmic reticulum.

European journal of pharmacology (1999-10-21)
N Nakahata, Y Harada, M Tsuji, K Kon-ya, Y Shizuri, Y Ohizumi
ABSTRACT

5,6-Dibromo-1,2-dimethylgramine evoked Ca(2+) release from skeletal muscle sarcoplasmic reticulum through ryanodine receptors in a concentration-dependent manner with an EC(50) of 22.2 microM. Since the EC(50) of caffeine was 0.885 mM, 5,6-dibromo-1,2-dimethylgramine was 40 times more sensitive than caffeine. Among 14 gramine derivatives having different substituents at N-1, C-2, C-5 or C-6 of the indole skeleton, we found that five derivatives were effective. Study of the structure-activity relationship for Ca(2+) release indicated that 1-methylation and/or both 5- and 6-bromination are important for Ca(2+) release. Thus, gramine derivatives are useful tools for the investigation of Ca(2+) release from sarcoplasmic reticulum.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Gramine, 97.5%