Abstract:
:1. In order to investigate the modulatory effects of adenosine on excitatory amino acid projections onto striatal medium spiny neurons, whole-cell patch clamp experiments were carried out in rat brain slices. The effects of various agonists for P1 (adenosine) and P2 (ATP) purinoceptors and their antagonists were investigated. The A2A receptor agonist 2-p-(2-carboxyethyl)phenythylamino-5'-N-ethylcarboxamidoadenosine (CGS 21680; 0.1 microM), the A1 receptor agonist 2-chloro-N6-cyclcopentyladenosine (CCPA; 10 microM) and the non-selective P1 purinoceptor antagonist 8-(p sulphophenyl)-theophylline (8-SPT; 100 microM) did not alter the resting membrane potential, the threshold current necessary to elicit an action potential, the amplitude of spikes, their rise time, the amplitude of the afterhyperpolarization (AHP) and the time to peak of the AHP. 2. N-methyl-D-aspartate (NMDA; 1-1000 microM) caused a concentration-dependent inward current which was larger in the absence than in the presence of Mg2+ (1.3 mM). In a subset of striatal neurones, the current response to NMDA (10 microM) and the accompanying increase in conductance were both inhibited by CGS 21680 (0.01-1 microM). The effect of CGS 21680 (0.1 microM) persisted in the presence of tetrodotoxin (0.5 microM) or in a Ca(2+)-free medium, under conditions when synaptically mediated influences may be negligible. 3. The A3 receptor agonist N6-2-(4-aminophenyl)ethyladenosine (APNEA; 0.1-10 microM) also diminished the effect of NMDA (10 microM), while the A1 receptor agonists CCPA (0.1-10 microM) and (2S)-N6-[2-endonorbornyl] adenosine [S(-)-ENBA; 10 microM] as well as the endogenous, non-selective P1 purinoceptor agonist adenosine (100 microM) were inactive. The endogenous non-selective P2 purinoceptor agonist ATP (1000 microM) also failed to alter the current response to NMDA (10 microM). Adenosine (100 microM), but not ATP (1000 microM) became inhibitory after blockade of nucleoside uptake by S[4-nitrobenzyl)-6-thioguanosine (NBTG; 30 microM). 4. 8-(p-Sulphophenyl)-theophylline (8-SPT; 100 microM), as well as the A2A receptor antagonist 8-(3-chlorostyryl) caffeine (CSC; 1 microM) and the A1 receptor antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX) at 0.03, but not 0.003 microM abolished the inhibitory action of CGS 21,680 (0.1 microM). None of these compounds altered the effect of NMDA (10 microM) by itself. DPCPX (0.03 microM) prevented the inhibition of APNEA (10 microM). 5. There was no effect of CGS 21,680 (0.1 microM), when guanosine 5'-O-(3-thiodiphosphate (GDP-beta-S; 300 microM) was included in the pipette solution in order to block G protein-mediated reactions. 6. In conclusion, adenosine receptors, probably of the A2A-subtype, inhibit the conductance of NMDA receptor channels in a subset of medium spiny neurones of the rat striatum by a transduction mechanism which involves a G protein.
journal_name
Br J Pharmacoljournal_title
British journal of pharmacologyauthors
Nörenberg W,Wirkner K,Illes Pdoi
10.1038/sj.bjp.0701347subject
Has Abstractpub_date
1997-09-01 00:00:00pages
71-80issue
1eissn
0007-1188issn
1476-5381journal_volume
122pub_type
杂志文章abstract::1. The effects of a rat brain extract containing clonidine-displacing substance (CDS), a putative endogenous imidazoline receptor ligand, on insulin release from rat and human isolated islets of Langerhans were investigated. 2. CDS was able to potentiate the insulin secretory response of rat islets incubated at 6 mM g...
journal_title:British journal of pharmacology
pub_type: 杂志文章
doi:10.1038/sj.bjp.0700964
更新日期:1997-03-01 00:00:00
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doi:10.1038/sj.bjp.0702726
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abstract::1. The stimulatory effect of neuropeptide Y (NPY) on food intake is well established but the roles of the receptor subtypes Y(1) and Y(5) have been difficult to define. We have studied the effects of two novel Y(1)-preferring and two Y(5)-preferring agonists on feeding in guinea pigs. 2. The Y(1)-preferring receptor a...
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journal_title:British journal of pharmacology
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doi:
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更新日期:2013-03-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
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journal_title:British journal of pharmacology
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更新日期:2011-04-01 00:00:00
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journal_title:British journal of pharmacology
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更新日期:2003-04-01 00:00:00
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journal_title:British journal of pharmacology
pub_type: 杂志文章
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更新日期:2013-04-01 00:00:00
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