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Log [ANTAGONIST], M

Figure 16 Functional bioassay for hNPY1R in Xenopus melanophores. (A) PYY-in-duced pigment aggregation in a ligand-controlled manner in NPY-Y1 melanophores. The effect of PYY on aggregation reached a maximum within 30 min and remained unchanged thereafter up to 120 min. Mock transfected melanophores (control) did not respond to PYY. (B) Dose-response of PYY on pigment aggregation and 125I-PYY binding in mela-nophores expressing NPY-Y1R transiently. (C) The effect of antagonist on pigment aggregation induced by PYY and 125I-PYY binding. The aggregation induced by 0.1 nM PYY was abolished by the NPY-Y1-specific antagonist in a dose-dependent manner with an IC50 of 0.4 |M. Antagonist also competed 125I-PYY bound with an IC50 of 0.4 |M. Both curves are superimposable, suggesting that the compound is a true antagonist of hNPY1R. (D) Effect of PYY on aggregation and 125I-PYY binding to melanophore stables expressing NPY-Y1R.

Log [ANTAGONIST], M

Figure 16 Functional bioassay for hNPY1R in Xenopus melanophores. (A) PYY-in-duced pigment aggregation in a ligand-controlled manner in NPY-Y1 melanophores. The effect of PYY on aggregation reached a maximum within 30 min and remained unchanged thereafter up to 120 min. Mock transfected melanophores (control) did not respond to PYY. (B) Dose-response of PYY on pigment aggregation and 125I-PYY binding in mela-nophores expressing NPY-Y1R transiently. (C) The effect of antagonist on pigment aggregation induced by PYY and 125I-PYY binding. The aggregation induced by 0.1 nM PYY was abolished by the NPY-Y1-specific antagonist in a dose-dependent manner with an IC50 of 0.4 |M. Antagonist also competed 125I-PYY bound with an IC50 of 0.4 |M. Both curves are superimposable, suggesting that the compound is a true antagonist of hNPY1R. (D) Effect of PYY on aggregation and 125I-PYY binding to melanophore stables expressing NPY-Y1R.

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