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Low efficacy adenosine A1 agonists inhibit striatal acetylcholine release in rats improving central selectivity of action
| article |
2003
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| Author: |
Bueters, T.J.H.
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Helden, H.P.M. van
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IJzerman, A.P.
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Danhof, M.
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| Keywords: |
Acetylcholine · Adenosine · Adenosine A1 receptor · Low efficacy agonist · Microdialysis · Tissue selectivity · 2' deoxy 6 n cyclopentyladenosine · 3' deoxy 6 n cyclopentyladenosine · 6 n cyclopentyladenosine · 8 butylamino 6 n cyclopentyladenosine · 8 cyclopentyltheophylline · 8 ethylamino 6 n cyclopentyladenosine · Acetylcholine · Adenosine A1 receptor agonist · Unclassified drug · Acetylcholine release · Animal experiment · Animal tissue · Cardiovascular system · Controlled study · Corpus striatum · Dose response · Drug effect · Drug efficacy · Male · Microdialysis · Nonhuman · Rat · Animals · Dose-Response Relationship, Drug · Microdialysis · Neostriatum · Rats, Wistar · Receptor, Adenosine A2B · Receptors, Purinergic P1 · Reproducibility of Results · Sensitivity and Specificity · 6 n cyclopentyladenosine, 41552-82-3 · 8 cyclopentyltheophylline, 35873-49-5 · Acetylcholine, 51-84-3, 60-31-1, 66-23-9 · Adenosine, 58-61-7; · N(6)-cyclopentyladenosine, 41552-82-3 · Receptor, Adenosine A2B · Receptors, Purinergic P1
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The objective of this study was to characterize the effects of the adenosine A1 receptor agonist N6-cyclopentyladenosine (CPA) and its low efficacy derivatives 2′-deoxy-CPA (2DCPA), 3′-deoxy-CPA (3DCPA), 8-ethylamino-CPA (8ECPA) and 8-butylamino-CPA (8BCPA) on the release of acetylcholine (ACh) using intrastriatal microdialysis. These low efficacy agonists exhibited lower effects on the cardiovascular system than CPA. A concentration-dependent inhibition of ACh release was observed with a maximum of 60.5±2.4% for CPA, 42.5±2.3% for 2DCPA, 45.3±5.8% for 3DCPA, 57.1±1.4% for 8ECPA and 93.1±10.9% for 8BCPA, respectively. This effect was counteracted by the adenosine A1 receptor antagonist 8-cyclopentyltheophylline. These findings show that low efficacy adenosine A1 agonists inhibit striatal ACh release equally effective as CPA, suggesting that central nervous system-selective actions can be obtained with these compounds. © 2003 Elsevier Science Ireland Ltd. All rights reserved.
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[Abstract]
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