title: Chronic caffeine alters the density of adenosine, adrenergic, cholinergic, GABA, and serotonin receptors and calcium channels in mouse brain.
abstract: 1. Chronic ingestion of caffeine by male NIH strain mice alters the density of a variety of central receptors. 2. The density of cortical A1 adenosine receptors is increased by 20%, while the density of striatal A2A adenosine receptors is unaltered. 3. The densities of cortical beta 1 and cerebellar beta 2 adrenergic receptors are reduced by ca. 25%, while the densities of cortical alpha 1 and alpha 2 adrenergic receptors are not significantly altered. Densities of striatal D1 and D2 dopaminergic receptors are unaltered. The densities of cortical 5 HT1 and 5 HT2 serotonergic receptors are increased by 26-30%. Densities of cortical muscarinic and nicotinic receptors are increased by 40-50%. The density of cortical benzodiazepine-binding sites associated with GABAA receptors is increased by 65%, and the affinity appears slightly decreased. The density of cortical MK-801 sites associated with NMDA-glutaminergic receptors appear unaltered. 4. The density of cortical nitrendipine-binding sites associated with calcium channels is increased by 18%. 5. The results indicate that chronic ingestion of caffeine equivalent to about 100 mg/kg/day in mice causes a wide range of biochemical alterations in the central nervous system.
authors.affiliation: Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892.
authors.forename: D
authors.initials: D
authors.lastname: Shi
authors.forename: O
authors.initials: O
authors.lastname: Nikodijević
authors.forename: K A
authors.initials: KA
authors.lastname: Jacobson
authors.forename: J W
authors.initials: JW
authors.lastname: Daly
mesh_terms: D000818:Animals; D001923:Brain Chemistry / Q000187:drug effects*; D002110:Caffeine / Q000008:administration & dosage / Q000494:pharmacology*; D015220:Calcium Channels / Q000187:drug effects*; D002531:Cerebellum / Q000737:chemistry / Q000187:drug effects; D002540:Cerebral Cortex / Q000737:chemistry / Q000187:drug effects; D003342:Corpus Striatum / Q000737:chemistry / Q000187:drug effects; D008297:Male; D051379:Mice; D011941:Receptors, Adrenergic / Q000145:classification / Q000187:drug effects; D011950:Receptors, Cholinergic / Q000145:classification / Q000187:drug effects; D011954:Receptors, Dopamine / Q000032:analysis; D018079:Receptors, GABA / Q000145:classification / Q000187:drug effects; D017470:Receptors, Glutamate / Q000032:analysis; D017981:Receptors, Neurotransmitter / Q000187:drug effects*; D018047:Receptors, Purinergic P1 / Q000145:classification / Q000187:drug effects; D011985:Receptors, Serotonin / Q000145:classification / Q000187:drug effects
chemical_list: D015220:Calcium Channels; D011941:Receptors, Adrenergic; D011950:Receptors, Cholinergic; D011954:Receptors, Dopamine; D018079:Receptors, GABA; D017470:Receptors, Glutamate; D017981:Receptors, Neurotransmitter; D018047:Receptors, Purinergic P1; D011985:Receptors, Serotonin; D002110:Caffeine