Release of norepinephrine in the central nervous system by theophylline and caffeine

Berkowitz, Barry A.; Tarver, James; Spector, Sydney

doi:10.1016/0014-2999(70)90158-5

Cited by 203 publications

(52 citation statements)

References 13 publications

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“…Caffeine has been reported to increase norepinephrine turnover (Berkowitz et al, 1970;Corrodi et al, 1972;Hadfield and Milio, 1989). A down-regulation of cortical β 1 adrenergic receptors has been previously reported for rats after chronic caffeine (Goldberg et al, 1982;Green and Stiles, 1986) or theophylline (Fredholm et al 1984).…”

Section: Discussionmentioning

confidence: 76%

“…β-Adrenergic receptors appear down-regulated, while α-adrenergic receptors appear unchanged (Goldberg et al, 1982;Green and Stiles, 1986). Caffeine does alter turnover of not only norepinephrine, but also of dopamine and serotonin (Berkowitz et al, 1970;Berkowitz and Spector, 1971;Corrodi et al, 1972;Hadfield and Milio, 1989). The effects of chronic caffeine on levels of dopamine and serotonin receptors do not appear to have been assessed.…”

Section: Introductionmentioning

confidence: 99%

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Chronic caffeine alters the density of adenosine, adrenergic, cholinergic, GABA, and serotonin receptors and calcium channels in mouse brain

et al. 1993

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SUMMARY1. Chronic ingestion of caffeine by male NIH strain mice alters the density of a variety of central receptors.2. The density of cortical A 1 adenosine receptors is increased by 20%, while the density of striatal A 2A adenosine receptors is unaltered.3. The densities of cortical β 1 and cerebellar β 2 adrenergic receptors are reduced by ca. 25%, while the densities of cortical α 1 and α 2 adrenergic receptors are not significantly altered.Densities of striatal D 1 and D 2 dopaminergic receptors are unaltered. The densities of cortical 5 HT 1 and 5 HT 2 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 GABA A 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.

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Section: Discussionmentioning

confidence: 76%

Section: Introductionmentioning

confidence: 99%

Chronic caffeine alters the density of adenosine, adrenergic, cholinergic, GABA, and serotonin receptors and calcium channels in mouse brain

et al. 1993

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“…Theophylline has a number of pharmacological properties including noradrenaline release (Berkowitz et al, 1970;Karasawa etal., 1976), adenosine receptor antagonism (Daly, Bruns & Snyder, 1981), release of Ca2+ (Johnson & Inesi, 1969) and phosphodiesterase inhibition (Amer & Kreighbaum, 1975). Recently, it was demonstrated that agents which decrease catecholamine function (depletors of monoamines and catecholamines, noradrenoceptor and dopamine receptor antagonists) increase the antinociceptive action of baclofen, and that this effect was likely to occur at a supraspinal site (Sawynok, 1982).…”

Section: Discussionmentioning

confidence: 99%

“…Recently, studies in this laboratory indicated that alterations in catecholamine function at supraspinal sites may be involved in this action (Sawynok, 1982). Theophylline has been shown to increase noradrenaline turnover in rat brain (Berkowitz, Tarver & Spector, 1970;Karasawa, Furukawa, Yoshida & Shimizu, 1976) and to antagonize the antinociceptive action of morphine in the tail flick test (Ho, Loh & Way, 1973;Jurna, 1981). In the present study, the effects of theophylline on the antinociceptive action of baclofen were investigated in an attempt to gain further insight into the mechanism(s) by which baclofen produces antinociception.…”

Section: Introductionmentioning

confidence: 99%

Theophylline‐induced potentiation of the antinociceptive action of baclofen

Sawynok

1983

British J Pharmacology

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“…As caffeine is usually consumed in foods or beverages and several medications, the consumed caffeine may cause in some neurochemical changes; because it is known that serotonin release affects sleep onset,9) modulates sensitivity to certain kinds of pain,IO) temperature regulation, 1 I) migraine headache,12) sedation, I 3) and probably memory.14.15) The administration of caffeine also affects the brain catecholamine metabolism such as the stimulation of brainstem norepinephrine synthesis and release of norepinephrine in rat and guinea-pig. 16 ) It is of interest to note that caffeine is used therapeutically alone or for food additives to stimulate the central nervous system. From this experiment, it can be suggested that some of the actions of caffeine may Vertical bars indicate standard errors of the mean (five rats per group).…”

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confidence: 99%