PMID

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Article Title

Organization

C4-substituted 1-beta-D-ribofuranosylpyrazolo[3,4-d]pyrimidines as adenosine agonist analogues.

TBA

Similarities and differences in affinity and binding modes of tricyclic pyrimido- and pyrazinoxanthines at human and rat adenosine receptors.

Jagiellonian University Medical College

alpha-adrenoreceptor reagents. 1. Synthesis of some 1,4-benzodioxans as selective presynaptic alpha 2-adrenoreceptor antagonists and potential antidepressants.

TBA

2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.

University Of Bonn

1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.

Institute

Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists.

Universit£

Nucleosides and nucleotides. 177. 9-(6,7-dideoxy-beta-D-allo-hept-5- ynofuranosyl)adenine: a selective and potent ligand for P3 purinoceptor-like protein.

Hokkaido University

(5aR,11bS)-4,5,5a,6,7,11b-hexahydro-2-propyl-3-thia-5-azacyclopent-1- ena[c]-phenanthrene-9,10-diol (A-86929): a potent and selective dopamine D1 agonist that maintains behavioral efficacy following repeated administration and characterization of its diacetyl prodrug (ABT-431).

Abbott Laboratories

Photoisomerization of a potent and selective adenosine A2 antagonist, (E)-1,3-Dipropyl-8-(3,4-dimethoxystyryl)-7-methylxanthine.

Kyowa Hakko Kogyo

Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.

Kyowa Hakko Kogyo

8-Polycycloalkyl-1,3-dipropylxanthines as potent and selective antagonists for A1-adenosine receptors.

Kyowa Hakko Kogyo

Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.

Niddk

Synthesis and biological activity of N6-(p-sulfophenyl)alkyl and N6-sulfoalkyl derivatives of adenosine: water-soluble and peripherally selective adenosine agonists.

National Institute Of Diabetes

Nucleosides and nucleotides. 103. 2-Alkynyladenosines: a novel class of selective adenosine A2 receptor agonists with potent antihypertensive effects.

Hokkaido University

Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.

Kyowa Hakko Kogyo

Nucleosides and nucleotides. 112. 2-(1-Hexyn-1-yl)adenosine-5'-uronamides: a new entry of selective A2 adenosine receptor agonists with potent antihypertensive activity.

Hokkaido University

2-Alkynyl derivatives of adenosine and adenosine-5'-N-ethyluronamide as selective agonists at A2 adenosine receptors.

Universit£

Nucleosides and nucleotides. 107. 2-(cycloalkylalkynyl)adenosines: adenosine A2 receptor agonists with potent antihypertensive effects.

Yamasa Shoyu

N6,9-disubstituted adenines: potent, selective antagonists at the A1 adenosine receptor.

University Of South Florida

Highly selective adenosine A2 receptor agonists in a series of N-alkylated 2-aminoadenosines.

Ciba-Geigy

1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists.

Center For Bio-Pharmaceutical Sciences

N6-substituted adenosine receptor agonists: potential antihypertensive agents.

Warner-Lambert

Activity of N6-substituted 2-chloroadenosines at A1 and A2 adenosine receptors.

University Of South Florida

4-Amino[1,2,4]triazolo[4,3-a]quinoxalines. A novel class of potent adenosine receptor antagonists and potential rapid-onset antidepressants.

Pfizer

2-(Arylalkylamino)adenosin-5'-uronamides: a new class of highly selective adenosine A2 receptor ligands.

Ciba-Geigy

A novel synthesis of xanthines: support for a new binding mode for xanthines with respect to adenosine at adenosine receptors.

Merrell Dow Research Institute

Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.

Pfizer

Sulfur-containing 1,3-dialkylxanthine derivatives as selective antagonists at A1-adenosine receptors.

Niddk

Electrophilic derivatives of purines as irreversible inhibitors of A1 adenosine receptors.

Niddk

N6-bicycloalkyladenosines with unusually high potency and selectivity for the adenosine A1 receptor.

Warner-Lambert

N6-[2-(3,5-dimethoxyphenyl)-2-(2-methylphenyl)ethyl]adenosine and its uronamide derivatives. Novel adenosine agonists with both high affinity and high selectivity for the adenosine A2 receptor.

Warner-Lambert

Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives.

Universit£

N6-(arylalkyl)adenosines. Identification of N6-(9-fluorenylmethyl)adenosine as a highly potent agonist for the adenosine A2 receptor.

Warner-Lambert

Binary drugs: conjugates of purines and a peptide that bind to both adenosine and substance P receptors.

TBA

N6-phenyladenosines: pronounced effect of phenyl substituents on affinity for A2 adenosine receptors.

TBA

N6-(2,2-diphenylethyl)adenosine, a novel adenosine receptor agonist with antipsychotic-like activity.

Parke-Davis Pharmaceutical Research Division

N6-substituted N-alkyladenosine-5'-uronamides: bifunctional ligands having recognition groups for A1 and A2 adenosine receptors.

TBA

Ribose-modified adenosine analogues as adenosine receptor agonists.

TBA

N6-cycloalkyladenosines. Potent, A1-selective adenosine agonists.

TBA

Adenosine receptors: targets for future drugs.

TBA

Fluorescent probes for adenosine receptors: synthesis and biology of N6-dansylaminoalkyl-substituted NECA derivatives.

Glaxowellcome Medicines Research Center

 

High selectivity of novel isoguanosine analogues for the adenosine A1 receptor

TBA

 

Discovery of FK453, a novel non-xanthine adenosine A₁ receptor antagonist

TBA

 

5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT_1D receptor agonists

TBA

 

The synthesis and biochemical evaluation of new A₁ selective adenosine receptor agonists containing 6-hydrazinopurine moieties

TBA

 

An explanation of the substituent effect of 1,3,8-trisubstituted xanthines on adenosine A₁/A₂ affinity.

TBA

Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.

National Institute Of Diabetes & Digestive & Kidney Diseases

Novel non-xanthine antagonist of the A

Bayer Pharmaceuticals

Design, synthesis, and evaluation of chromen-2-ones as potent and selective human dopamine D4 antagonists.

Warner-Lambert

Isoindolinone enantiomers having affinity for the dopamine D4 receptor.

Parke-Davis Pharmaceutical Research

A

Rheinische Friedrich-Wilhelms-Universitat Bonn

Substituted [(4-phenylpiperazinyl)-methyl]benzamides: selective dopamine D4 agonists.

Warner-Lambert

Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists.

National Institute Of Diabetes

Synthesis of paraxanthine analogs (1,7-disubstituted xanthines) and other xanthines unsubstituted at the 3-position: structure-activity relationships at adenosine receptors.

Pharmazeutische Chemie

Discovery of 6-oxo-3-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-1(6H)- pyridazinebutanoic acid (FK 838): a novel non-xanthine adenosine A1 receptor antagonist with potent diuretic activity.

Fujisawa Pharmaceutical

Structure-activity profile of a series of novel triazoloquinazoline adenosine antagonists.

Ciba-Geigy

[1,2,4]Triazolo[4,3-a]quinoxalin-4-amines: a new class of A1 receptor selective adenosine antagonists.

Warner-Lambert

Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists.

Merrell Dow Research Institute

Analogues of 1,3-dipropyl-8-phenylxanthine: enhancement of selectivity at A1-adenosine receptors by aryl substituents.

TBA

Fluorescent-Labeled Selective Adenosine A

University Of Bonn

Linear and proximal benzo-separated alkylated xanthines as adenosine-receptor antagonists.

University Of South Florida

Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.

National Institutes Of Health

7-Deaza-2-phenyladenines: structure-activity relationships of potent A1 selective adenosine receptor antagonists.

National Institute Of Diabetes

Imidazodiazepinediones: a new class of adenosine receptor antagonists.

National Institute Of Diabetes

1,3,8-trisubstituted xanthines. Effects of substitution pattern upon adenosine receptor A1/A2 affinity.

Nova Pharmaceutical

8-(Dicyclopropylmethyl)-1,3-dipropylxanthine: a potent and selective adenosine A1 antagonist with renal protective and diuretic activities.

Kyowa Hakko Kogyo

Synthesis and adenosine receptor affinity of a series of pyrazolo[3,4-d]pyrimidine analogues of 1-methylisoguanosine.

Griffith University

Structure-activity relationships of 8-cycloalkyl-1,3-dipropylxanthines as antagonists of adenosine receptors.

Vanderbilt University

(E)-1,3-dialkyl-7-methyl-8-(3,4,5-trimethoxystyryl)xanthines: potent and selective adenosine A2 antagonists.

Kyowa Hakko Kogyo

Conformationally restrained, chiral (phenylisopropyl)amino-substituted pyrazolo[3,4-d]pyrimidines and purines with selectivity for adenosine A1 and A2 receptors.

Marion Merrell Dow Research Institute