ArticleBritish journal of pharmacology1993
Ap4A and ADP-beta-S binding to P2 purinoceptors present on rat brain synaptic terminals.
Article in British journal of pharmacology, 1993. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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17 citing papers in PubMed, 87 citations in OpenAlex.
- Purinergic Signalling in Parkinson's Disease: A Multi-target System to Combat Neurodegeneration.Neurochemical research · 2019Review
- Diadenosine tetraphosphate protects against injuries induced by ischemia and 6-hydroxydopamine in rat brain.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2003Article
- Diadenosine polyphosphates evoke Ca2+ transients in guinea-pig brain via receptors distinct from those for ATP.The Journal of physiology · 1997Article
- Diadenosine polyphosphates induce intracellular Ca2+ mobilization in human neutrophils via a pertussis toxin sensitive G-protein.Immunology · 1997Article
- Desensitization of P2U receptor in neuronal cell line. Different control by the agonists ATP and UTP, as demonstrated by single-cell Ca2+ responses.The Biochemical journal · 1996Article
- Selectivity and activity of adenine dinucleotides at recombinant P2X2 and P2Y1 purinoceptors.British journal of pharmacology · 1996Article
- Evidence for two distinct P2-purinoceptors subserving contraction of the rat anococcygeus smooth muscle.British journal of pharmacology · 1996Article
- Characterization of the binding of diadenosine 5',5'''-P1,P4-tetraphosphate (Ap4A) to rat liver cell membranes.The Biochemical journal · 1996Article
- Cytosolic free Ca2+ oscillations induced by diadenosine 5',5"'-P1,P3-triphosphate and diadenosine 5',5"'-P1,P4-tetraphosphate in single rat hepatocytes are indistinguishable from those induced by ADP and ATP respectively.The Biochemical journal · 1995Article
- Pharmacological selectivity of the cloned human P2U-purinoceptor: potent activation by diadenosine tetraphosphate.British journal of pharmacology · 1995Article
- A novel receptor for diadenosine polyphosphates coupled to calcium increase in rat midbrain synaptosomes.British journal of pharmacology · 1995Article
- Autoradiography of P2x ATP receptors in the rat brain.British journal of pharmacology · 1995Article
- Modulation by nicotinamide adenine dinucleotide of sympathetic and sensory-motor neurotransmission via P1-purinoceptors in the rat mesenteric arterial bed.British journal of pharmacology · 1995Article
- Nomenclature and classification of purinoceptors.Pharmacological reviews · 1994Review
- The use of antagonists to characterize the receptors mediating depolarization of the rat isolated vagus nerve by alpha, beta-methylene adenosine 5'-triphosphate.British journal of pharmacology · 1994Article
- Characterization of purinoceptors mediating depolarization of rat isolated vagus nerve.British journal of pharmacology · 1993Article
- Suso Pintor (1964-2019): The art of making science look easy.Journal of optometryArticle
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. Diadenosine tetraphosphate (Ap4A) a dinucleotide stored and released from rat brain synaptic terminals presents two types of affinity binding sites in synaptosomes. When [3H]-Ap4A was used for binding studies a Kd value of 0.10 +/- 0.014 nM and a Bmax value of 16.6 +/- 1.2 fmol mg-1 protein were obtained for the high affinity binding site from the Scatchard analysis. The second binding site, obtained by displacement studies, showed a Ki value of 0.57 +/- 0.09 microM. 2. Displacement of [3H]-Ap4A by non-labelled Ap4A and P2-purinoceptor ligands showed a displacement order of Ap4A > adenosine 5'-O-(2-thiodiphosphate) (ADP-beta-S) > 5'-adenylyl-imidodiphosphate (AMP-PNP) > alpha,beta-methylene adenosine 5'-triphosphate (alpha,beta-MeATP) in both sites revealed by the Ki values of 0.017 nM, 0.030 nM, 0.058 nM and 0.147 nM respectively for the high affinity binding site and values of 0.57 microM, 0.87 microM, 2.20 microM and 4.28 microM respectively for the second binding site. 3. Studies of the P2-purinoceptors present in synaptosomes were also performed with [35S]-ADP-beta-S. This radioligand showed two binding sites the first with Kd and Bmax values of 0.11 +/- 0.022 nM and 3.9 +/- 2.1 fmol mg-1 of protein respectively for the high affinity binding site obtained from the Scatchard plot. The second binding site showed a Ki of 0.018 +/- 0.0035 microM obtained from displacement curves. 4. Competition studies with diadenosine polyphosphates of [35S]-ADP-beta-S binding showed a displacement order of Ap4A > Ap5A > Ap6A in the high affinity binding site and Ki values of 0.023 nM, 0.081 nM and 5.72 nM respectively. The second binding site potency order was Ap5A> Ap4A > Ap6A,with Ki values of 0.28 microM, 0.53 microM and 5.32 microM respectively.5. Displacement studies of [35S]-ADP-beta-S with P2-purinoceptor agonists showed the following potency pattern: ADP-beta-S > AMP-PNP >alpha,beta-MeATP with Ki values of 0.021 nM, 0.029 nM 0.215 nM respectively in the high affinity binding site. 2-Methylthio-adenosine 5'-triphosphate (2MeSATP) was unable to displace [35S]-ADP-beta-S in this binding site. The second binding site showed a profile of ADP-beta-S> a,beta-MeATP> AMP-PNP > 2MeSATP and Ki values of 0.0 18 microM, 0.212 microM, 0.481 microM and 18.04 microM respectively.6. These studies suggest the presence of a new P2-purinoceptor in rat brain synaptosomes with high affinity for diadenosine polyphosphates which we tentatively designate as P2d.
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