Posted by Darby on March 4, 2004, at 14:20:18
In reply to Re: COFFEE- augmenting antidepressants???? » Sooshi, posted by btnd on March 3, 2004, at 6:19:14
Adenosine receptors seem to play some role in the regulation of fatigue and mood, among other things...very interesting...
Darby
1: Eur J Pharmacol. 2002 May 10;442(3):215-23. Related Articles, Links
Dicinnamoylquinides in roasted coffee inhibit the human adenosine transporter.de Paulis T, Schmidt DE, Bruchey AK, Kirby MT, McDonald MP, Commers P, Lovinger DM, Martin PR.
Institute for Coffee Studies, Department of Psychiatry, Vanderbilt University School of Medicine, Nashville, TN 37232, USA.
Preliminary screening of a minor, non-xanthine constituent of roasted coffee, 3,4-diferuloyl-1,5-quinolactone (DIFEQ), showed inhibition of the adenosine transporter at low micromolar concentration. DIFEQ is a neutral derivative of the chlorogenic acids, i.e. isomeric mono- and di-substituted coumaroyl-, caffeoyl-, and feruloyl-esters of quinic acid, formed in the roasting process of coffee. Displacement of the adenosine transporter antagonist [(3)H](S)-(nitrobenzyl)-6-thioinosine binding by DIFEQ in cultured U-937 cell preparations, expressing the human adenosine transporter protein (hENT1), showed a K(i) of 0.96+/-0.13 microM. Extracts of regular and decaffeinated coffee showed binding activities equivalent to 30-40 mg DIFEQ per three cups of coffee. Acute administration of a high dose of DIFEQ (100 mg/kg i.p.) reduced open field locomotion in mice for 20 min in correlation with brain levels of DIFEQ. Both 3,4-dicaffeoyl-1,5-quinide and 3,4-dicoumaroyl-1,5-quinide, two close structural analogs of DIFEQ also present in roasted coffee, showed similar affinities for the adenosine transporter, while the corresponding 3- and 4-mono caffeoyl- and feruloyl-quinides were one to two orders of magnitudes less active. This suggests that 3,4-dicinnamoyl-1,5-quinides in coffee could have the potential to raise extra-cellular adenosine levels, thereby counteracting the stimulant effect of caffeine.
poster:Darby
thread:318390
URL: http://www.dr-bob.org/babble/20040304/msgs/320182.html