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The I 1 subtype of imidazoline receptors (I 1 R) is a plasma membrane protein that is involved in diverse physiological functions. Available radioligands used so far to characterize the I 1 R were able to bind with similar affinities to ␣ 2 -adrenergic receptors (␣ 2 -ARs) and to I 1 R. This feature was a major drawback for an adequate characterization of this receptor subtype. New imidazoline analogs were therefore synthesized and the present study describes one of these compounds, 2-(2-chloro-4-iodophenylamino)-5-methyl-pyrroline (LNP 911), which was of high affinity and selectivity for the I 1 R. LNP 911 was radioiodinated and its binding properties characterized in different membrane preparations. Saturation experiments with [

Taspoglutide offered good glycaemic control similar to pioglitazone, while achieving beneficial weight loss rather than weight gain, but was associated with more AEs. Due to the higher than expected discontinuation rates, mainly because of gastrointestinal intolerability, the taspoglutide clinical programme was stopped.

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