Stereoselective synthesis, in vitro , and initial in vivo evaluation of 1-methylpiperidin-4-yl α-hydroxy-α-(1-iodo-1-propen-3-yl)-α-phenylacetate (IPIP): a novel radioiodinated molecular probe with high affinity for the muscarinic receptor

The development of a β-CCT-lanthanide conjugate that binds the dopamine transporter (DAT) with high affinity (Kd = 303 nM) is described. This molecular probe could be used for in vivo or in vitro studies of the DAT via MRI, PET or SPECT.

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Design, Synthesis, and in Vitro and in Vivo Evaluation of High Affinity and Specificity Near-Infrared Fluorescent Bombesin Antagonists for Tumor Imaging

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.8b00614 ◽

2018 ◽

Vol 61 (17) ◽

pp. 7657-7670 ◽

Cited By ~ 7

Author(s):

Hang Xu ◽

Rajendra P. Bandari ◽

Li Lee ◽

Ran Li ◽

Ping Yu ◽

...

Keyword(s):

Near Infrared ◽

Tumor Imaging ◽

In Vivo Evaluation ◽

Design Synthesis ◽

High Affinity

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In Vitro and In Vivo Evaluation of Alexa Fluor 680-Bombesin[7–14]NH2Peptide Conjugate, a High-Affinity Fluorescent Probe with High Selectivity for the Gastrin-Releasing Peptide Receptor

Molecular Imaging ◽

10.2310/7290.2007.00013 ◽

2007 ◽

Vol 6 (3) ◽

pp. 7290.2007.00013 ◽

Cited By ~ 23

Author(s):

Lixin Ma ◽

Ping Yu ◽

Bhadrasetty Veerendra ◽

Tammy L. Rold ◽

Lauren Retzloff ◽

...

Keyword(s):

Fluorescent Probe ◽

High Selectivity ◽

In Vivo Evaluation ◽

Peptide Receptor ◽

Alexa Fluor ◽

Gastrin Releasing Peptide ◽

High Affinity

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In vitro and in vivo evaluation of the anti-inflammatory effects of Arzanol from Helichrysum italicum

Planta Medica ◽

10.1055/s-0030-1264369 ◽

2010 ◽

Vol 76 (12) ◽

Author(s):

J Bauer ◽

F Dehm ◽

A Koeberle ◽

F Pollastro ◽

G Appendino ◽

...

Keyword(s):

In Vivo Evaluation ◽

Anti Inflammatory

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Effects of Heparin Oligosaccharides with High Affinity for Antithrombin III in Experimental Venous Thrombosis

Thrombosis and Haemostasis ◽

10.1055/s-0038-1657178 ◽

1982 ◽

Vol 47 (03) ◽

pp. 244-248 ◽

Cited By ~ 47

Author(s):

D P Thomas ◽

Rosemary E Merton ◽

T W Barrowcliffe ◽

L Thunberg ◽

U Lindahl

Keyword(s):

Antithrombin Iii ◽

Specific Activity ◽

High Specific Activity ◽

Factor Xa ◽

Blood Levels ◽

Thrombin Time ◽

High Affinity ◽

Very High

SummaryThe in vitro and in vivo characteristics of two oligosaccharide heparin fragments have been compared to those of unfractionated mucosal heparin. A decasaccharide fragment had essentially no activity by APTT or calcium thrombin time assays in vitro, but possessed very high specific activity by anti-Factor Xa assays. When injected into rabbits at doses of up to 80 ¼g/kg, this fragment was relatively ineffective in impairing stasis thrombosis despite producing high blood levels by anti-Xa assays. A 16-18 monosaccharide fragment had even higher specific activity (almost 2000 iu/mg) by chromogenic substrate anti-Xa assay, with minimal activity by APTT. When injected in vivo, this fragment gave low blood levels by APTT, very high anti-Xa levels, and was more effective in preventing thrombosis than the decasaccharide fragment. However, in comparison with unfractionated heparin, the 16-18 monosaccharide fragment was only partially effective in preventing thrombosis, despite producing much higher blood levels by anti-Xa assays.It is concluded that the high-affinity binding of a heparin fragment to antithrombin III does not by itself impair venous thrombogenesis, and that the anti-Factor Xa activity of heparin is only a partial expression of its therapeutic potential.

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