Biomaterial Database

sigma1 Receptors in rat striatum regulate NMDA-stimulated [3H]dopamine release via a presynaptic mechanism. 1995

G M Gonzalez-Alvear, and L L Werling

Department of Pharmacology, The George Washington University Medical Center, Washington DC 20037, USA.

The role of the sigma1 receptor in the regulation of N-methyl-D-aspartate (NMDA)-stimulated [3H]dopamine release from rat striatal slices was examined. The sigma receptor agonist 1S,2R-(--)-N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)cy clohexylamine (BD737) inhibited stimulated release in a concentration-dependent manner. The sigma1 receptor antagonist, 1-(cyclopropylmethyl)-4-(2'-(4"-fluorophenyl)-2'-oxoethyl)piperidi ne HBr (DuP 734), reversed inhibition of release by BD737. Haloperidol, di-o-tolylguanidine (DTG) and N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamine (BD1008) reversed the BD737-mediated inhibition of release. Haloperidol and DTG also antagonized inhibition of stimulated release by (+)-pentazocine. Furthermore, BD737 and (+)-pentazocine inhibited stimulated release in the presence of tetrodotoxin, suggesting that sigma1 receptors regulating dopamine release are located on dopaminergic nerve terminals. These data suggest that sigma1 receptors may be important in the regulation of glutamate-stimulated dopamine release.

UI	MeSH Term	Description	Entries
D008297	Male		Males
D010423	Pentazocine	The first mixed agonist-antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opioid receptors and has a weak antagonist action at the mu receptor. (From AMA Drug Evaluations Annual, 1991, p97)	Fortral,Lexir,Pentazocine Hydrochloride,Pentazocine Lactate,Talwin,Hydrochloride, Pentazocine,Lactate, Pentazocine
D011759	Pyrrolidines	Compounds also known as tetrahydropyridines with general molecular formula (CH2)4NH.	Tetrahydropyridine,Tetrahydropyridines
D003514	Cyclohexylamines	A family of alicyclic hydrocarbons containing an amine group with the general formula R-C6H10NH2.	Cyclohexylamine
D004298	Dopamine	One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.	Hydroxytyramine,3,4-Dihydroxyphenethylamine,4-(2-Aminoethyl)-1,2-benzenediol,Dopamine Hydrochloride,Intropin,3,4 Dihydroxyphenethylamine,Hydrochloride, Dopamine
D005260	Female		Females
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
D016202	N-Methylaspartate	An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).	N-Methyl-D-aspartate,NMDA,N-Methyl-D-aspartic Acid,Acid, N-Methyl-D-aspartic,N Methyl D aspartate,N Methyl D aspartic Acid,N Methylaspartate
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
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