Biomaterial Database

Agonists of cyclic AMP-coupled metabotropic glutamate receptors in adult rat cortical slices. 1996

M C Kemp, and D E Jane, and H W Tse, and P J Roberts

Department of Pharmacology, School of Medical Sciences, University of Bristol, UK.

A number of potential Group 2 and Group 3 metabotropic glutamate receptor (mGlu receptor) agonists were investigated in adult rat brain cerebrocortical slices. The rank order of their potency in inhibiting forskolin-stimulated adenylyl cyclase was found to be: (S)-2-amino-2-methyl-4-phosphonobutyric acid (MAP4) > (2S,1'S,2'S)-2-(2-carboxycyclopropyl)glycine (L-CCG-I) > (1S,3S)-1-aminocyclopentane-1,3-dicarboxylic acid (1S,3S-ACPD) > (1S,3R)-1-aminocyclopentane-1, 3-dicarboxylic acid (1S,3R)-ACPD) > (2S,1'R,2'R,3'R)-2-(2,3-dicarboxycyclopropyl)glycine (DCG-IV) > (S) -2-methylglutamate ((S)-MG) > L-glutamate > (2S,1'S, 2'S)-2-(2-carboxycyclopropyl)alanine (MCCG) > L-2-amino-4-phosphonobutyric acid (L-AP4) > L-serine-O-phosphate (SOP). The finding that (S)-2-amino-2-methyl-4-phosphonobutyric acid was the most potent agonist at these metabotropic glutamate receptors is in contrast to its observed potent mGlu receptor antagonist action in the neonatal rat spinal cord.

UI	MeSH Term	Description	Entries
D002540	Cerebral Cortex	The thin layer of GRAY MATTER on the surface of the CEREBRAL HEMISPHERES that develops from the TELENCEPHALON and folds into gyri and sulci. It reaches its highest development in humans and is responsible for intellectual faculties and higher mental functions.	Allocortex,Archipallium,Cortex Cerebri,Cortical Plate,Paleocortex,Periallocortex,Allocortices,Archipalliums,Cerebral Cortices,Cortex Cerebrus,Cortex, Cerebral,Cortical Plates,Paleocortices,Periallocortices,Plate, Cortical
D004305	Dose-Response Relationship, Drug	The relationship between the dose of an administered drug and the response of the organism to the drug.	Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D005576	Colforsin	Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.	Coleonol,Forskolin,N,N-Dimethyl-beta-alanine-5-(acetyloxy)-3-ethenyldodecahydro-10,10b-dihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-1H-naphtho(2,1-b)pyran-6-yl Ester HCl,NKH 477,NKH-477,NKH477
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
D051381	Rats	The common name for the genus Rattus.	Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus
D018094	Receptors, Metabotropic Glutamate	Cell surface proteins that bind glutamate and act through G-proteins to influence second messenger systems. Several types of metabotropic glutamate receptors have been cloned. They differ in pharmacology, distribution, and mechanisms of action.	Glutamate Receptors, Metabotropic,Metabotropic Glutamate Receptors,Receptors, Glutamate, Metabotropic,Metabotropic Glutamate Receptor,Glutamate Receptor, Metabotropic,Receptor, Metabotropic Glutamate