ChemInform Abstract: Synthesis of N1-Substituted Analogues of (2R,4R)-4-Aminopyrrolidine-2,4-dicarboxylic Acid as Agonists, Partial Agonists, and Antagonists of Group II Metabotropic Glutamate Receptors.

ChemInform ◽  
2010 ◽  
Vol 32 (45) ◽  
pp. no-no
Author(s):  
Jayanta Kumar Mukhopadhyaya ◽  
Alan P. Kozikowski ◽  
Ewa Grajkowska ◽  
Sergey Pshenichkin ◽  
Jarda T. Wroblewski
Keyword(s):  
Dicarboxylic Acid ◽  
Glutamate Receptors ◽  
Metabotropic Glutamate Receptors ◽  
Metabotropic Glutamate ◽  
Partial Agonists ◽  
Group Ii

scholarly journals Activity-Dependent Activation of Presynaptic Metabotropic Glutamate Receptors in Locus Coeruleus

2000 ◽  
Vol 83 (3) ◽  
pp. 1141-1149 ◽  
Author(s):  
G. R. Dubé ◽  
K. C. Marshall
Keyword(s):  
Dicarboxylic Acid ◽  
Locus Coeruleus ◽  
Glutamate Receptors ◽  
Metabotropic Glutamate Receptors ◽  
Excitatory Amino Acid ◽  
Synaptic Activity ◽  
Group Iii ◽  
Metabotropic Glutamate ◽  
Group Ii ◽  
Activity Dependent

Synaptic activation of metabotropic glutamate receptors (mGluRs) in the locus coeruleus (LC) was investigated in adult rat brain slice preparations. Evoked excitatory postsynaptic potentials (EPSPs) resulting from stimulation of LC afferents were measured with current clamp from intracellularly recorded LC neurons. In this preparation, mGluR agonists (±)-1-aminocyclopentane- trans-1,3-dicarboxylic acid ( t-ACPD) and L(+)-2-amino-4-phosphonobutyric acid (L-AP4) activate distinct presynaptic mGluRs, resulting in an inhibition of EPSPs. When two stimuli were applied to afferents at intervals >200 ms, the amplitude of the second [test (T)] EPSP was identical in amplitude to the first [control(C)]. However, when a stimulation volley was delivered before T, the amplitude of the latter EPSP was consistently smaller than C. The activity-dependent depression (ADD) was dependent on the frequency and duration of the train and the interval between the train and T. ADD was potentiated in the presence of an excitatory amino acid (EAA) uptake inhibitorL- trans-pyrrolidine-2,4-dicarboxylic acid ( t-PDC, 100 μM), changing the T/C ratio from 0.84 ± 0.05 (mean ± SE) in control to 0.69 ± 0.04 in t-PDC ( n = 9). In the presence of t-PDC, the depolarizing response of LC neurons to focally applied glutamate was also increased. Together, these results suggest that accumulation of EAA after synaptic stimulation may be responsible for ADD. To test if ADD is a result of the activation of presynaptic mGluRs, the effect of selective mGluR antagonists on ADD was assessed. In the presence of t-PDC, bath applied (S)-amino-2-methyl-4-phosphonobutanoic acid (MAP4, 500 μM), a mGluR group III antagonist, significantly reversed the decrease in T/C ratio after a train stimulation [from 0.66 ± 0.04 to 0.81 ± 0.02 (mean ± SE), n = 5]. The T/C ratio in the presence of MAP4 was not different from that measured in the absence of a stimulation volley. Conversely, ethyl glutamic acid (EGLU, 500 μM), a mGluR group II antagonist, failed to alter the T/C ratio. Together, these results suggest that, in LC, group III presynaptic mGluR activation provides a feedback mechanism by which excitatory synaptic transmission can be negatively modulated during high-frequency synaptic activity. Furthermore, this study provides functional differentiation between presynaptic groups II and III mGluR in LC and suggests that the group II mGluR may be involved in functions distinct from those of group III mGluRs.

scholarly journals HDAC and HAT Inhibitors Differently Affect Analgesia Mediated by Group II Metabotropic Glutamate Receptors

2014 ◽  
Vol 10 ◽  
pp. 1744-8069-10-68 ◽  
Author(s):  
Magda Zammataro ◽  
Maria Angela Sortino ◽  
Carmela Parenti ◽  
Robert W Gereau ◽  
Santina Chiechio
Keyword(s):  
Glutamate Receptors ◽  
Metabotropic Glutamate Receptors ◽  
Metabotropic Glutamate ◽  
Group Ii

Potentiation of Morphine's Antinociception by Group II and Group III Metabotropic Glutamate Receptors Agonists on a Rat Incisional Pain

2006 ◽  
Vol 19 (2) ◽  
pp. 131 ◽  
Author(s):  
Chang Mo Kim ◽  
Jeong Il Choi ◽  
Hong Beom Bae ◽  
Seok Jai Kim ◽  
Sung Tae Chung ◽  
...  
Keyword(s):  
Glutamate Receptors ◽  
Metabotropic Glutamate Receptors ◽  
Group Iii ◽  
Metabotropic Glutamate ◽  
Group Ii ◽  
Incisional Pain
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