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1.
Figure 4

Figure 4. From: The orthosteric agonist 2-chloro-5-hydroxyphenylglycine activates mGluR5 and mGluR1 with similar efficacy and potency.

Efficacy and potency of CHPG were similar for SCG calcium current modulation in cells expressing mGluR5b, mGluR1a, and mGluR1b. Calcium current inhibition by each concentration of CHPG was normalized to that by 100 μM Glu in each cell, and plotted here. Neither efficacy nor potency of CHPG’s effects on mGluR1a, 1b or 5b were statistically distinguishable.

Paul J Kammermeier. BMC Pharmacol. 2012;12:6-6.
2.
Figure 2

Figure 2. From: The orthosteric agonist 2-chloro-5-hydroxyphenylglycine activates mGluR5 and mGluR1 with similar efficacy and potency.

CHPG does not activate group II or III mGluRs. Average (± SEM) calcium current inhibition by 100 μM Glu and 1 mM CHPG in SCG neurons expressing mGluR2 (left) or mGluR4 (right). Both Glu and CHPG were applied to each cell. Number of cells in each group shown in parentheses.

Paul J Kammermeier. BMC Pharmacol. 2012;12:6-6.
3.
Figure 8

Figure 8. From: The orthosteric agonist 2-chloro-5-hydroxyphenylglycine activates mGluR5 and mGluR1 with similar efficacy and potency.

Relative strength of Gqactivation by CHPG is not well correlated with apparent mGluR1 expression level. Relative strength of the Gq inhibitory pathway, expressed as the Post/Pre inhibition ratio vs. apparent mGluR1 expression level, expressed as magnitude of inhibition by 100 μM Glu in each cell. Note that all of the mGluR1 expressing cells recorded are shown, not just those with strong Gq components, as in Figure 7.

Paul J Kammermeier. BMC Pharmacol. 2012;12:6-6.
4.
Figure 5

Figure 5. From: The orthosteric agonist 2-chloro-5-hydroxyphenylglycine activates mGluR5 and mGluR1 with similar efficacy and potency.

Effect of selective inhibitors on CHPG effects in mGluR5b and 1a expressing cells. Average (± SEM) calcium current inhibition produced by application of 1 mM CHPG alone (black) or in the presence of 1 μM MPEP (gray) or 50 μM LY367385 (white) in SCG neurons expressing the indicated receptor. Number of cells in each group shown in parentheses.

Paul J Kammermeier. BMC Pharmacol. 2012;12:6-6.
5.
Figure 7

Figure 7. From: The orthosteric agonist 2-chloro-5-hydroxyphenylglycine activates mGluR5 and mGluR1 with similar efficacy and potency.

DIfferential mechanism of calcium current modulation by Glu and CHPG in cells expressing mGluR1a.A, Sample calcium current traces elicited with the voltage protocol shown (below) illustrating control and Glu (upper) or CHPG (lower) inhibited currents in cells expressing either mGluR5b (left) or mGluR1a (right). Inhibited traces shown in gray. Note that the Gq-mediated component of inhibition is not reversed by the depolarizing step, and is therefore similar in both “Pre” and “Post.” Scale bars represent 0.4 nA and 10 msec. B, Summary of the Gq-mediated, voltage independent component of inhibition (expressed as the Post/Pre inhibition ratio) for Glu and CHPG (paired measurements in each cell) from mGluR5 (left) and mGluR1 (right) expressing cells. Number of cells in each group shown in parentheses.

Paul J Kammermeier. BMC Pharmacol. 2012;12:6-6.
6.
Figure 3

Figure 3. From: The orthosteric agonist 2-chloro-5-hydroxyphenylglycine activates mGluR5 and mGluR1 with similar efficacy and potency.

CHPG induces strong calcium current modulation in SCG neurons expressing mGluR1a and 1b.A, Time course and sample current traces (inset) illustrating the magnitude of calcium currents in a representative mGluR1a expressing SCG neuron and inhibition by various concentrations of CHPG and by 100 μM Glu, as indicated. Cells were held at −80 mV and current was elicited by a 25 msec step to +10 mV. Scale bars represent 0.5 nA and 10 msec. B, Dose response curves for CHPG in cells expressing mGluR1a (open circles) or mGluR1b (open diamonds, as indicated. For mGluR1a, n = 12 at all concentrations. For mGluR1b (30–3000 μM), n = 5, 6, 7 and 7, respectively.

Paul J Kammermeier. BMC Pharmacol. 2012;12:6-6.
7.
Figure 1

Figure 1. From: The orthosteric agonist 2-chloro-5-hydroxyphenylglycine activates mGluR5 and mGluR1 with similar efficacy and potency.

CHPG induces strong calcium current modulation in SCG neurons expressing mGluR5.A, Time course and sample current traces (inset) illustrating the magnitude of calcium currents in a representative SCG neuron and inhibition by various concentrations of CHPG and Glu, as indicated. Voltage protocol consisted of a 25 msec step to +10 mV from a holding potential of −80 mV. Scale bars in inset represent 1 nA and 10 msec. B, Average (±SEM) calcium current inhibition at a range of CHPG concentrations (for [CHPG] ranging from 10 μM to 3 mM, n = 6, 3, 8, 4, 11, and 7, respectively).

Paul J Kammermeier. BMC Pharmacol. 2012;12:6-6.
8.
Figure 6

Figure 6. From: The orthosteric agonist 2-chloro-5-hydroxyphenylglycine activates mGluR5 and mGluR1 with similar efficacy and potency.

Modulation of M-current by CHPG in SCG neurons expressing either mGluR5b or mGluR1a.A, Left, Average (±SEM) calcium current by 1 mM CHPG (open) and 100 μM Glu (filled), in SCG neurons expressing mGluR5b or mGluR1a, as indicated. Number of cells in each group is shown in parentheses. Right, Average (±SEM) ratio of CHPG/Glu inhibition of calcium current in the same cells as in Left. Asterisk indicates p < 0.05, T-test. Note that since ratios are non-linearly distributed around unity, statistical tests were performed on the natural log of the ratio (CHPG/Glu inhibition) from each individual cell. B, Sample current traces illustrating M-current inhibition in an mGluR1a expressing cell. In this cell, CHPG had little effect while Glu strongly inhibited the current. M-currents were measured as the tail current deactivating during a hyperpolarizing step to −60 mV from a holding potential of −30 mV (to inactivate other K+ channels). Voltage protocol is shown below. C, Distribution of percent inhibition by CHPG plotted against the inhibition by Glu in each cell.

Paul J Kammermeier. BMC Pharmacol. 2012;12:6-6.

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