Pharmacological differentiation of metabotropic glutamate receptors coupled to potentiation of cyclic adenosine monophosphate responses and phosphoinositide hydrolysis. 1993

D G Winder, and T Smith, and P J Conn
Department of Pharmacology, Emory University, Atlanta, Georgia.

Activation of metabotropic glutamate receptors (mGluRs) results in multiple second messenger responses in rat hippocampal slices, including stimulation of phosphoinositide hydrolysis and potentiation of cyclic AMP responses induced by agonists of other receptors that are directly coupled to adenylate cyclase. Alpha 1 adrenergic receptors and H1-histaminergic receptors are similar to mGluRs in that agonists of these receptors also induce both phosphoinositide hydrolysis and potentiation of cyclic AMP responses to other agonists. In each of these cases, it is not clear whether activation of phosphoinositide hydrolysis and potentiation of cyclic AMP responses are mediated by the same or different receptor subtypes. In the present studies, the pharmacological profiles of mGluR-mediated potentiation of cyclic AMP responses and mGluR-mediated activation of phosphoinositide hydrolysis were compared to determine whether these responses are mediated by the same or distinct receptor subtypes. In addition, the authors determined the effect of mGluR activation on cyclic AMP responses in various regions of the rat brain and at different stages of postnatal development. It was found that the rank order of efficacies and potencies of mGluR agonists for potentiating cyclic AMP responses is distinct from the rank order of efficacies and potencies of the same compounds at stimulating phosphoinositide hydrolysis. Furthermore, L-serine-O-phosphate competitively blocked mGluR-mediated potentiation of cyclic AMP responses but had little or no effect on activation of phosphoinositide hydrolysis by the active isomer of trans-1-aminocyclopentane-1,3-dicarboxylic acid. These data are consistent with the hypothesis that these two responses are mediated by distinct mGluR subtypes.

UI MeSH Term Description Entries
D008297 Male Males
D010716 Phosphatidylinositols Derivatives of phosphatidic acids in which the phosphoric acid is bound in ester linkage to the hexahydroxy alcohol, myo-inositol. Complete hydrolysis yields 1 mole of glycerol, phosphoric acid, myo-inositol, and 2 moles of fatty acids. Inositide Phospholipid,Inositol Phosphoglyceride,Inositol Phosphoglycerides,Inositol Phospholipid,Phosphoinositide,Phosphoinositides,PtdIns,Inositide Phospholipids,Inositol Phospholipids,Phosphatidyl Inositol,Phosphatidylinositol,Inositol, Phosphatidyl,Phosphoglyceride, Inositol,Phosphoglycerides, Inositol,Phospholipid, Inositide,Phospholipid, Inositol,Phospholipids, Inositide,Phospholipids, Inositol
D010768 Phosphoserine The phosphoric acid ester of serine. Serine Phosphate,Phosphorylserine,Seryl Phosphate,Phosphate, Serine,Phosphate, Seryl
D001921 Brain The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM. Encephalon
D003515 Cycloleucine An amino acid formed by cyclization of leucine. It has cytostatic, immunosuppressive and antineoplastic activities. 1-Aminocyclopentanecarboxylic Acid,Aminocyclopentanecarboxylic Acid,NSC 1026,1 Aminocyclopentanecarboxylic Acid,Acid, 1-Aminocyclopentanecarboxylic,Acid, Aminocyclopentanecarboxylic
D006868 Hydrolysis The process of cleaving a chemical compound by the addition of a molecule of water.
D000242 Cyclic AMP An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH. Adenosine Cyclic 3',5'-Monophosphate,Adenosine Cyclic 3,5 Monophosphate,Adenosine Cyclic Monophosphate,Adenosine Cyclic-3',5'-Monophosphate,Cyclic AMP, (R)-Isomer,Cyclic AMP, Disodium Salt,Cyclic AMP, Monoammonium Salt,Cyclic AMP, Monopotassium Salt,Cyclic AMP, Monosodium Salt,Cyclic AMP, Sodium Salt,3',5'-Monophosphate, Adenosine Cyclic,AMP, Cyclic,Adenosine Cyclic 3',5' Monophosphate,Cyclic 3',5'-Monophosphate, Adenosine,Cyclic Monophosphate, Adenosine,Cyclic-3',5'-Monophosphate, Adenosine,Monophosphate, Adenosine Cyclic
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D014660 Vasoactive Intestinal Peptide A highly basic, 28 amino acid neuropeptide released from intestinal mucosa. It has a wide range of biological actions affecting the cardiovascular, gastrointestinal, and respiratory systems and is neuroprotective. It binds special receptors (RECEPTORS, VASOACTIVE INTESTINAL PEPTIDE). VIP (Vasoactive Intestinal Peptide),Vasoactive Intestinal Polypeptide,Vasointestinal Peptide,Intestinal Peptide, Vasoactive,Intestinal Polypeptide, Vasoactive,Peptide, Vasoactive Intestinal,Peptide, Vasointestinal,Polypeptide, Vasoactive Intestinal
D017207 Rats, Sprague-Dawley A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company. Holtzman Rat,Rats, Holtzman,Sprague-Dawley Rat,Rats, Sprague Dawley,Holtzman Rats,Rat, Holtzman,Rat, Sprague-Dawley,Sprague Dawley Rat,Sprague Dawley Rats,Sprague-Dawley Rats

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