Another chemical called cyclocreatine also blocks the creatine transporter in frog cells, but it takes about 370 millionths of a gram per milliliter to block half of the transporter's activity, which is less potent than beta-guanidinopropionic acid.

Scientific Claim

Cyclocreatine inhibits the human CRT-1 creatine transporter in Xenopus oocytes with an IC50 of approximately 369.8 microM, indicating its relative potency compared to other inhibitors in this experimental system.

Source Excerpt

“The induced uptake was inhibited by beta-guanidinopropionic acid (IC50 approximately 44.4 microM), 2-amino-1-imidazolidineacetic acid (cyclocreatine; IC50 approximately 369.8 microM), gamma-guanidinobutyric acid (IC50 approximately 697.9 microM), gamma-aminobutyric acid (IC50 approximately 6.47 mM), and amiloride (IC50 approximately 2.46 mM).”

Evidence from Studies

Supporting Studies

Molecular characterization of the human CRT-1 creatine transporter expressed in Xenopus oocytes.

In Vitro

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Evidence Assessment

Supported

The study directly measured the inhibition of creatine uptake by cyclocreatine in Xenopus oocytes expressing the human CRT-1 transporter. The IC50 value quantifies the concentration needed for half-maximal inhibition in this specific experimental system.

Source Study

Molecular characterization of the human CRT-1 creatine transporter expressed in Xenopus oocytes.

Score: 2

DOI: 10.1006/abbi.1998.0959

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