Probes for vasopressin receptors Attachment of affinity and fluorescent groups in vasopressin

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Abstract
Fluorescent, photoreactive, and biotinylated analogs of vasopressin have been prepared in which one of these three groups has been attached to a reactive amino group in either position 4 or position 7. Using solid phase methodology, we have synthesized two active parent compounds, [l‐desamino,4‐lysine,7‐hydroxy‐prolinelarginine vasopressin and [l‐desamino,7‐aminoproline]arginine vasopressin, and acylated them to obtain biotinyl, azidobenzoyl, and fluoresceinyl derivatives. We have also prepared analogs in which a “spacer arm” was inserted between lysine in position 4 and the marker group. Some of these derivatives have good antidiuretic activity and could be valuable probes in studying hormone‐receptor interaction and in receptor visualization and purification.