Biomaterial Database

The effects of sigma ligands on the release of glutamate from rat striatal slices. 1994

Y Ellis, and J A Davies

Department of Pharmacology and Therapeutics, University of Wales College of Medicine, Heath Park, Cardiff, UK.

This study investigated the effects of sigma receptor ligands on the release of endogenous amino acid neurotransmitters from rat striatal slices. The effect of haloperidol on release in slices prepared from 6-hydroxydopamine lesioned animals was also tested. Haloperidol, the (+/-) reduced metabolite of haloperidol, rimcazole and ifenprodil specifically reduced potassium-stimulated release of glutamate with IC50 values between 20-60 microM. The release of aspartate, gamma-aminobutyric acid (GABA) and glycine was not affected. Haloperidol also reduced glutamate release from slices prepared from lesioned animals. The neuroleptic drug alpha-flupenthixol and the putative sigma receptor ligand R(+)3-(3-hydroxyphenyl)-N-(n-propyl) piperidine (3-PPP) had no effect on release. These effects of the sigma ligands show that the inhibition of glutamate release is specific to this amino acid and also that it is not due to dopamine receptor blockade as those ligands which have low affinity for dopamine receptors were also effective in reducing release. A presynaptic location for sigma receptor sites, possibly associated with ion channels, could account for the effects of these ligands on transmitter release.

UI	MeSH Term	Description	Entries
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
D009478	Neuropeptide Y	A 36-amino acid peptide present in many organs and in many sympathetic noradrenergic neurons. It has vasoconstrictor and natriuretic activity and regulates local blood flow, glandular secretion, and smooth muscle activity. The peptide also stimulates feeding and drinking behavior and influences secretion of pituitary hormones.	Neuropeptide Y-Like Immunoreactive Peptide,Neuropeptide Tyrosine,Neuropeptide Y Like Immunoreactive Peptide,Tyrosine, Neuropeptide
D010880	Piperidines	A family of hexahydropyridines.
D011188	Potassium	An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.
D003342	Corpus Striatum	Striped GRAY MATTER and WHITE MATTER consisting of the NEOSTRIATUM and paleostriatum (GLOBUS PALLIDUS). It is located in front of and lateral to the THALAMUS in each cerebral hemisphere. The gray substance is made up of the CAUDATE NUCLEUS and the lentiform nucleus (the latter consisting of the GLOBUS PALLIDUS and PUTAMEN). The WHITE MATTER is the INTERNAL CAPSULE.	Lenticular Nucleus,Lentiform Nucleus,Lentiform Nuclei,Nucleus Lentiformis,Lentiformis, Nucleus,Nuclei, Lentiform,Nucleus, Lenticular,Nucleus, Lentiform,Striatum, Corpus
D005260	Female		Females
D006220	Haloperidol	A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279)	Haldol
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
D017208	Rats, Wistar	A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.	Wistar Rat,Rat, Wistar,Wistar Rats
D017480	Receptors, sigma	A class of cell surface receptors recognized by its pharmacological profile. Sigma receptors were originally considered to be opioid receptors because they bind certain synthetic opioids. However they also interact with a variety of other psychoactive drugs, and their endogenous ligand is not known (although they can react to certain endogenous steroids). Sigma receptors are found in the immune, endocrine, and nervous systems, and in some peripheral tissues.	Opioid Receptors, sigma,Receptors, Opioid, sigma,Receptors, sigma Opioid,sigma Receptors,sigma Receptor,Receptor, sigma,sigma Opioid Receptors