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Pharmacological characterization of LY303870: a novel, potent and selective nonpeptide substance P (neurokinin-1) receptor antagonist

Autor: B D, Gitter, R F, Bruns, J J, Howbert, D C, Waters, P G, Threlkeld, L M, Cox, J A, Nixon, K L, Lobb, N R, Mason, P W, Stengel

Publikováno v: The Journal of pharmacology and experimental therapeutics. 275(2)

LY303870 [(R)-1-[N-(2-methoxybenzyl)acetylamino]-3-(1H-indol-3-yl)-2-[N-(2-(4- (piperidin-1-yl)piperidin-1-yl)acetyl)amino]propane] is a new, potent and selective nonpeptide neurokinin-1 (NK-1) receptor antagonist. LY303870 bound selectively and with

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::5c5c0e91e949c65a5596c944f83cb07b
https://pubmed.ncbi.nlm.nih.gov/7473161

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Allosteric enhancer PD 81,723 acts by novel mechanism to potentiate cardiac actions of adenosine

Autor: Jackie Ruble, C Kollias-Baker, R F Bruns, J Linden, Donn M. Dennis, Luiz Belardinelli

Publikováno v: Circulation research. 75(6)

The 2-amino-3-benzoylthiophene derivative PD 81,723 is an allosteric enhancer of agonist binding to brain A1 adenosine receptors. One aim of this study was to characterize and contrast the effects of PD 81,723 on the A1 receptor-mediated negative dro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::abfb020b40d6c925766265d178b08a19
https://pubmed.ncbi.nlm.nih.gov/7955150

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Selective potentiation by an A1 adenosine receptor enhancer of the negative dromotropic action of adenosine in the guinea pig heart

Autor: B, Amoah-Apraku, J, Xu, J Y, Lu, A, Pelleg, R F, Bruns, L, Belardinelli

Publikováno v: The Journal of pharmacology and experimental therapeutics. 266(2)

The drug (2-amino-4,5-dimethyl-3-thienyl)-[3(trifluoromethyl)-phenyl]methanone (PD 81,723) has been shown to enhance allosterically A1 adenosine receptor binding in brain membranes. The objective of this study was to determine the specificity and sel

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::3ad2f425f853a468f37559d2c79afad1
https://pubmed.ncbi.nlm.nih.gov/8355194

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Cardiac functional responses to adenosine by PD 81,723, an allosteric enhancer of the adenosine A1 receptor

Autor: S. C. Montamat, R. V. Mudumbi, Robert E. Vestal, R. F. Bruns

Publikováno v: The American journal of physiology. 264(3 Pt 2)

Adenosine, a locally released and rapidly metabolized nucleoside, protects the heart from damage during ischemia by reducing oxygen demand and increasing oxygen supply. The aminothiophene derivative (2-amino-4,5-dimethylthien-3-yl)[3-(trifluoromethyl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c05285a6480319a8e134cd0c584b7bad
https://pubmed.ncbi.nlm.nih.gov/8456969

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Allosteric enhancement of adenosine A1 receptor binding and function by 2-amino-3-benzoylthiophenes

Autor: R F, Bruns, J H, Fergus

Publikováno v: Molecular pharmacology. 38(6)

Several 2-amino-3-benzoylthiophenes were found to increase the binding of [3H]N6-cyclohexyladenosine to A1 adenosine receptors in rat brain membranes. Concentration-response curves were bell-shaped, with up to 45% stimulation of binding at 10 microM

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::e962d0ca3ca5591c974e8dc7fc71d443
https://pubmed.ncbi.nlm.nih.gov/2174510

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Structure-activity relationships for enhancement of adenosine A1 receptor binding by 2-amino-3-benzoylthiophenes

Autor: R F, Bruns, J H, Fergus, L L, Coughenour, G G, Courtland, T A, Pugsley, J H, Dodd, F J, Tinney

Publikováno v: Molecular pharmacology. 38(6)

The structural requirements for stimulation of adenosine A1 agonist binding by 2-amino-3-benzoylthiophenes and related compounds were investigated. Slowing of the dissociation of [3H]N6cyclohexyladenosine binding was used as a specific measure of the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::fd7395f29ae4363684ced9d8806c98ba
https://pubmed.ncbi.nlm.nih.gov/2250667

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Subclasses of angiotensin II binding sites and their functional significance

Autor: D T, Dudley, R L, Panek, T C, Major, G H, Lu, R F, Bruns, B A, Klinkefus, J C, Hodges, R E, Weishaar

Publikováno v: Molecular pharmacology. 38(3)

Specific binding sites for angiotensin II were identified in the rabbit adrenal gland and uterus and in the rat liver and were divided into two subclasses based on inhibition by nonpeptide ligands. Peptide ligands affected binding equally in all thre

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::c96085dc59f0ee020d9847af15c0e254
https://pubmed.ncbi.nlm.nih.gov/2402226

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Structure Activity Relationships for Adenosine Antagonists

Autor: R. F. Bruns

Publikováno v: Purines in Cellular Signaling ISBN: 9781461279969

An important milestone in adenosine research was the discovery by Sattin and Rall in 1970 that theophylline and other methylxanthines could block responses to adenosine. With the availability of competitive adenosine antagonists, it was possible for

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::364a57ddacc35eb53deefba8d6518145
https://doi.org/10.1007/978-1-4612-3400-5_21

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