✦ LIBER ✦

Radioiododestannylation. Convenient synthesis of a high affinity thromboxane A2/prostaglandin H2 receptor antagonist

✍ Scribed by Dale E. Mais; Perry V. Halushka; Masao Naka; Thomas A. Morinelli; John E. Oatis JR.; Nobuyuki Hamanaka

Publisher: John Wiley and Sons
Year: 1991
Tongue: French
Weight: 201 KB
Volume: 29
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.2580290110

No coin nor oath required. For personal study only.

✦ Synopsis

Radioiodination

of methyl-7-[(2R, 2S, 3S, 5 R ) -6 , 6 -d i m e t h y l -3 -( 4trimethylstannylbenzenesulfonylamino) bicyclo[3.1.l]hept-2-yl]-5(Z)-heptenoate with (1251] Na using a modification of the chloramine-T method in organic solvent is simple with high yields and site specific. The product, following hydrolysis of the ester, 7-[(2R. 2S, 3S, 5 R ) -6,6-di met h y 1-3 -(4-[ 2 5 I]iodo be nzenesu If on y la mi no) bic yclo [3.1 .I ] hep t -2-ylI ~ S(Z)-heptenoic acid ([l 251]-ISAP), was purified by HPLC. The high specific activity and specific binding will make the ligand a useful tool for the characterization of thromboxane Aplprostaglandin H2 receptors.

📜 SIMILAR VOLUMES

Synthesis of an [125I]-azido photoaffini

Synthesis of an [125I]-azido photoaffinity probe for the human platelet thromboxane A2/prostaglandin H2 receptor

✍ Dale E. Mais; Perry V. Halushka 📂 Article 📅 1988 🏛 John Wiley and Sons 🌐 French ⚖ 257 KB 👁 1 views

The synthesis o f [1251]-( 1S,2S,3S,5R)-2-(6~-carboxyhex-(2~Z)enyl)-3-(2-hydroxy-3-(4-hydroxy-3-iodophenyl)-l-propyl ami n0)-6,6-dimethyl b i c y c l o[ 3.1.13 heptane( I-PTA-OH), a h i g h a f f i n i t y thromboxane A /prostaglandin H (TXA /PGH ) receptor antag o n i s t has been p r e v i o u s l

ChemInform Abstract: 2-Aryltryptamines:

ChemInform Abstract: 2-Aryltryptamines: Selective High-Affinity Antagonists for the h5-HT2A Receptor.

✍ Graeme I. Stevenson; Adrian L. Smith; Stephen Lewis; Stephen G. Michie; Joseph G 📂 Article 📅 2001 🏛 John Wiley and Sons ⚖ 34 KB 👁 1 views

ChemInform Abstract: Synthesis and Evalu

ChemInform Abstract: Synthesis and Evaluation of Trimetoquinol Derivatives: Novel Thromboxane A2/Prostaglandin H2 Antagonists with Diminished β- Adrenergic Agonist Activity.

✍ J. J. CHRISTOFF; L. BRADLEY; D. D. MILLER; L. LEI; F. RODRIGUEZ; P. FRAUNDORFER; 📂 Article 📅 2010 🏛 John Wiley and Sons ⚖ 36 KB 👁 2 views

The Discovery of a Selective, High Affin

The Discovery of a Selective, High Affinity A2B Adenosine Receptor Antagonist for the Potential Treatment of Asthma.

✍ Jeff Zablocki; et al. et al. 📂 Article 📅 2005 🏛 John Wiley and Sons ⚖ 27 KB 👁 2 views

ChemInform Abstract: Synthesis, Structur

ChemInform Abstract: Synthesis, Structural Characterization and Thromboxane A2 Receptor Antagonistic Activity of 3-Substituted 2-[(Arylsulfonyl)imino]-2,3-dihydrothiazolyl Derivatives.

✍ Fabrice Lacan; Martine Varache-Lembege; Joseph Vercauteren; Jean-Michel Leger; B 📂 Article 📅 2010 🏛 John Wiley and Sons ⚖ 31 KB 👁 1 views

Synthesis, Structural Characterization and Thromboxane A 2 Receptor Antagonistic Activity of 3-Substituted 2-[(Arylsulfonyl)imino]-2,3-dihydrothiazolyl Derivatives. -Seven new title derivatives such as (I) are prepared by the Hantzsch synthesis. Compounds (I) show significant binding affinities in

Potent antagonists for the human adenosi

Potent antagonists for the human adenosine A2B receptor. Derivatives of the triazolotriazine adenosine receptor antagonist ZM241385 with high affinity

✍ Maarten de Zwart; Roel C. Vollinga; Margot W. Beukers; Danielle F. Sleegers; Jac 📂 Article 📅 1999 🏛 John Wiley and Sons 🌐 English ⚖ 147 KB 👁 2 views

A series of novel and known 5-substituted 7-amino-2-(2-furyl) [1,2,4]triazolo [1,5a][1,3,5]triazine derivatives were synthesized and tested for adenosine receptor antagonism in radioligand binding assays at all four adenosine receptor subtypes and for inhibition of the agonist-induced cyclic AMP res