Biomaterial Database

AMPA (amino-3-hydroxy-5-methylisoxazole-4-propionic acid) receptors in human brain tissues. 1995

D G Sawutz, and D S Krafte, and J J Oleynek, and B Ault

Department of Biochemistry, Sterling Winthrop Pharmaceuticals Research Division, Collegeville, PA 19426, USA.

AMPA receptors may play an important role in acute and chronic neurodegenerative diseases. An assay for the specific binding of [3H]-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) to receptors in membranes from post-mortem human brain is described, which can be used in screening for selective AMPA receptor antagonists. Membranes were prepared from frozen human adult hippocampus and whole fetal brain tissues. [3H]-AMPA binding to human hippocampus was saturable; Scatchard analysis of equilibrium binding data indicated high and low affinity sites with affinity binding constants (KD) of 3.4 +/- 0.5 nM and 65 +/- 9 nM (n = 7) respectively. Biphasic association and dissociation rate constants for [3H]-AMPA binding were consistent with the biphasic Scatchard analysis. Inhibition of [3H]-AMPA binding revealed a rank order of potency as quisqualate = AMPA > BOAA > L-glutamate = DNQX = CNQX > kainate > L-aspartate = NMDA. AMPA receptors in human fetal brain had a comparable pharmacology. AMPA/kainate receptors were expressed in frog oocytes following injection of RNA prepared from human fetal brain. Human brain tissues may therefore be utilized for screening and functional analysis of AMPA receptor antagonists.

UI	MeSH Term	Description	Entries
D007608	Kainic Acid	(2S-(2 alpha,3 beta,4 beta))-2-Carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid. Ascaricide obtained from the red alga Digenea simplex. It is a potent excitatory amino acid agonist at some types of excitatory amino acid receptors and has been used to discriminate among receptor types. Like many excitatory amino acid agonists it can cause neurotoxicity and has been used experimentally for that purpose.	Digenic Acid,Kainate,Acid, Digenic,Acid, Kainic
D007700	Kinetics	The rate dynamics in chemical or physical systems.
D008024	Ligands	A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)	Ligand
D009865	Oocytes	Female germ cells derived from OOGONIA and termed OOCYTES when they enter MEIOSIS. The primary oocytes begin meiosis but are arrested at the diplotene state until OVULATION at PUBERTY to give rise to haploid secondary oocytes or ova (OVUM).	Ovocytes,Oocyte,Ovocyte
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
D005260	Female		Females
D005333	Fetus	The unborn young of a viviparous mammal, in the postembryonic period, after the major structures have been outlined. In humans, the unborn young from the end of the eighth week after CONCEPTION until BIRTH, as distinguished from the earlier EMBRYO, MAMMALIAN.	Fetal Structures,Fetal Tissue,Fetuses,Mummified Fetus,Retained Fetus,Fetal Structure,Fetal Tissues,Fetus, Mummified,Fetus, Retained,Structure, Fetal,Structures, Fetal,Tissue, Fetal,Tissues, Fetal
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000328	Adult	A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available.	Adults
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