Peptidyl conjugates of adenosine 5'-carboxylic acid synthesized and evaluated as ligands for P2 purinoceptors.
The role of extracellular ATP in vivo and the various cellular responses mediated by P2 purinoceptors have not yet been fully elucidated, in part depending on the lack of subtype-specific high affinity antagonists. Here we describe the synthesis of a new class of compounds, peptidyl derivatives of adenosine 5'-carboxylic acid, among which some have inhibitory effects in certain P2 purinoceptor-carrying biological systems, e.g., glioma and smooth muscle cell lines and isolated smooth muscle tissue preparations from guinea pig vas deferens and urinary bladder.
Järlebark
L
L
Department of Neurochemistry and Neurotoxicology, Arrhenius Laboratories for Natural Sciences, Stockholm University, Sweden.
Erlandsson
M
M
Uri
A
A
King
B F
BF
Ziganshin
A U
AU
Johansson
C
C
Heilbronn
E
E
D000241:Adenosine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism; D000818:Animals; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D009130:Muscle, Smooth / Q000378:metabolism / Q000502:physiology; D010455:Peptides / Q000737:chemistry*; D058910:Purinergic P2 Receptor Agonists; D058919:Purinergic P2 Receptor Antagonists; D011817:Rabbits; D051381:Rats; D018048:Receptors, Purinergic P2 / Q000378:metabolism*; D011994:Recombinant Proteins / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism; D014407:Tumor Cells, Cultured; D014981:Xenopus
D008024:Ligands; D010455:Peptides; D058910:Purinergic P2 Receptor Agonists; D058919:Purinergic P2 Receptor Antagonists; D018048:Receptors, Purinergic P2; D011994:Recombinant Proteins; C102887:adenosine-5'-carboxylic acid; D000241:Adenosine