Biomaterial Database

Cocaine self-administration appears to be mediated by dopamine uptake inhibition. 1988

M C Ritz, and R J Lamb, and S R Goldberg, and M J Kuhar

National Institute on Drug Abuse, Addiction Research Center, Baltimore, Maryland.

1. While cocaine binds to several known sites in the brain, the binding site or receptor associated with its reinforcing or addictive properties has not been identified as such. 2. The identification of the pharmacologically relevant receptor(s) requires that an association exist between the potency of a variety of cocaine of cocaine-related drugs in animal models of substance and their potency at a binding site in the brain. 3. Our experiments indicate that the potencies of cocaine-like drugs in animal studies of drug self-administration are correlated with their potencies in inhibiting 3H-mazindol binding to dopamine transporters in the rat striatum. Cocaine binding to several other presynaptic and postsynaptic binding sites does not appear to be associated with the reinforcing effects of the drug. 4. Thus, the cocaine receptor related to substance abuse appears to be the binding site associated with inhibition of dopamine uptake on the dopaminergic nerve terminals.

UI	MeSH Term	Description	Entries
D008454	Mazindol	Tricyclic anorexigenic agent unrelated to and less toxic than AMPHETAMINE, but with some similar side effects. It inhibits uptake of catecholamines and blocks the binding of cocaine to the dopamine uptake transporter.	AN-448,Diestet,Mazanor,Mazindole,Sanjorex,Sanorex,Solucaps,Teronac,Teronak,AN448
D011954	Receptors, Dopamine	Cell-surface proteins that bind dopamine with high affinity and trigger intracellular changes influencing the behavior of cells.	Dopamine Receptors,Dopamine Receptor,Receptor, Dopamine
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
D003042	Cocaine	An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.	Cocaine HCl,Cocaine Hydrochloride,HCl, Cocaine,Hydrochloride, Cocaine
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
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
D012646	Self Administration	Administration of a drug or chemical by the individual under the direction of a physician. It includes administration clinically or experimentally, by human or animal.	Administration, Self,Administrations, Self,Self Administrations