2000
DOI: 10.1016/s0165-1838(00)00128-4
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In search of selective P2 receptor ligands: interaction of dihydropyridine derivatives at recombinant rat P2X2 receptors

Abstract: Abstract1,4-Dihydropyridines are regarded as privileged structures for drug design, i.e. they tend to bind to a wide variety of receptor sites. We have shown that upon appropriate manipulation of the substituent groups on a 1,4-dihydropyridine template, high affinity and selectivity for the A 3 subtype of adenosine receptors ('P1 receptors') may be attained. In the present study we have begun to extend this approach to P2 receptors which are activated by ATP and other nucleotides. Nicardipine, a representative… Show more

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Cited by 19 publications
(17 citation statements)
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“…Nifedipine [76,90,91] Nicardipine [92] Nilvadipine [83,93] Felodipine [94] ( sulfonamide [67,75], spiroindanyl piperidine [75], 1,4-dihydropyridine [76], 2,6-dichloro-9-thiabicyclo[3.3.1]nonane [77], benzopyran [78,79], pyridazines [80], indoles and quinolines [81,82].…”
Section: The Concept Of Privileged Structuresmentioning
confidence: 99%
“…Nifedipine [76,90,91] Nicardipine [92] Nilvadipine [83,93] Felodipine [94] ( sulfonamide [67,75], spiroindanyl piperidine [75], 1,4-dihydropyridine [76], 2,6-dichloro-9-thiabicyclo[3.3.1]nonane [77], benzopyran [78,79], pyridazines [80], indoles and quinolines [81,82].…”
Section: The Concept Of Privileged Structuresmentioning
confidence: 99%
“…Specific blockers of P2X5 receptors are unknown to date [ 1 ]. However, it was reported recently that α,β-methylene ATP-induced contractions were inhibited by nifedipine in rat vascular smooth muscle cells [ 40 ] and that nicardipine reduced the current induced at recombinant rat P2X2 and P2X4 receptors expressed in Xenopus oocytes [ 28 ]. Therefore, we investigated the effect of several dihydropyridines on hP2X5 FL .…”
Section: Discussionmentioning
confidence: 99%
“…Thus, it is conceivable to repurpose this scaffold for diverse targets. In the case of purinergic signaling pathways, various DHPs have been found to inhibit P2X2 receptors, adenosine receptors, and the equilibrative nucleoside transporter (ENT1) [ 28 , 29 , 30 ].…”
Section: Introductionmentioning
confidence: 99%
“…The macrophages and lymphocytes from the lymph nodes are more susceptible to ATPe compared with the macrophages and lymphocytes from other sources. The literature reports that the EC 50 for the agonist (ATP) of the P2X7 receptor is approximately 780 µ M in macrophages [28]. Several hypotheses could explain this increase in the sensitivity to ATPe.…”
Section: Discussionmentioning
confidence: 99%