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Phe-Met-Arg-Phe amide trifluoroacetate is an activator of K + current, with ED 50 of 23 nM in the peptidergic caudodorsal neurons.
In Vitro
In the molluscan central nervous system, Phe-Met-Arg-Phe amide (FMRFa) acts on K + channels in sensory, motor-, and neuroendocrine neurones. Phe-Met-Arg-Phe amide activates a novel K + current that is characterized by a combined voltage- and receptor-dependent gating mechanism, with both factors being necessary for opening of the channels. Phe-Met-Arg-Phe amide (1 μM) significantly inhibits glucose stimulated (300 mg/dL) insulin release (p<0.005) and somatostatin release (p<0.01) from the isolated perfused pancreas. Phe-Met-Arg-Phe amide (FMRF-NH2) (1 and 10 μM) is without effect on Glukagon secretion, either in low glucose (50 mg/dL), high glucose (300 mg/dL), or during arginine stimulation (5 mM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Phe-Met-Arg-Phe amide (FMRFamide) stimulates growth hormone secretion in conscious OVX rats. The presence of Phe-Met-Arg-Phe amide-like immunoreactivity in neuronal elements in the hypothalamus suggested a role for this in the hypothalamic control of the anterior pituitary function. The injection of 200 ng (313.8 picomoles) of FMRFamide (in 2 uL) produces a significantly increased plasma GH 15 min after injection. The GH-increasing effect of 400-800 ng (627-1255 picomoles) of FMRFamide is already developed after 5 min and lasted up to 30 min. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:ED50: 23 nM (K + current)