Download Adenosine Receptors - Theraputic Aspects by G. Hasko, et al., PDF

By G. Hasko, et al.,

ISBN-10: 0849339995

ISBN-13: 9780849339998

Show description

Read or Download Adenosine Receptors - Theraputic Aspects PDF

Best nonfiction_7 books

Integrals and Series [Vol 2 - Spl Functions]

The fourth and 5th volumes of this broad multivolume venture Integrals and sequence are dedicated to tables of Laplace transforms. In those better half volumes the authors have accumulated facts scattered during the literature, and feature augmented this fabric with many unpublished effects acquired of their personal study.

Trace Metals in Sea Water

In recent times, swift clinical advances were shattering classical thoughts of oceanic hint metals concentrations. many of the information accrued earlier than the mid-1970s have needed to be discarded. attainable institutions of natural and inorganic ligands with the metals have been throwing perspectives of steel speciation into nice uncertainty.

The 1755 Lisbon Earthquake: Revisited

The 1755 earthquake and tsunami have been influential not just in Portugal yet in all eu and North African international locations the place the devastating results have been felt. the whole global used to be deeply inspired and the dialogue of its reasons generated a large number of clinical and metaphysical hypothesis. It encouraged philosophers, poets and writers.

Image Analysis: 13th Scandinavian Conference, SCIA 2003 Halmstad, Sweden, June 29 – July 2, 2003 Proceedings

This booklet constitutes the refeered court cases of the thirteenth Scandinavian convention on snapshot research, SCIA 2003, held in Halmstad, Sweden in June/July 2003. The 148 revised complete papers offered including 6 invited contributions have been conscientiously reviewed and chosen for presentation. The papers are prepared in topical sections on characteristic extraction, intensity and floor, form research, coding and illustration, movement research, scientific photograph processing, colour research, texture research, indexing and categorization, and segmentation and spatial grouping.

Additional info for Adenosine Receptors - Theraputic Aspects

Example text

The phenyl carbamoyl pharmacophores used previously in pyrazolotriazolopyrimidienes were incorporated into the N6-position of an 8-azaadenine template, of which derivatives have demonstrated selective A1AR antagonistic behavior. 63 An alternate approach to designing A3 antagonists is to start with high-affinity adenosine derivatives and simply truncate the molecule in stages to remove its ability to activate the receptor without losing its high affinity of binding. , substituted benzyl groups or large cycloalkyl rings) reduced the maximal efficacy, leading to reduced efficacy at the A3AR.

Generally, these 2-substituted adenosine derivatives were less potent at the A1AR in comparison to the A3AR, but fully efficacious at that subtype, with binding Ki values over 100 nM. The 2-phenylethyl moiety resulted in higher A3AR affinity (Ki in nM) when linked to the 2-position of adenosine through an ether group (54) than when linked through an amine (310) or thioether (>10,000). Typically, 2-ethers of adenosine are A2A-selective agonists; thus, the compounds mentioned earlier are somewhat exceptional.

G. , Pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A3 adenosine receptor antagonists: influence of the chain at the N8 pyrazole nitrogen, J. Med. , 43, 4768, 2000. 45. G. , Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A3 adenosine receptor antagonists, J. Med. , 42, 4473, 1999. 46. G. , Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors, Bioorg.

Download PDF sample

Rated 4.91 of 5 – based on 18 votes