Vasopressin antagonist analogs modified at position 7.
Vasopressin antagonist analogs having alanine or glycine at position 7 were essentially equipotent with analogs with proline, N-methylalanine or sarcosine at position 7. This demonstrates that the conformational constraint imposed by an N-alkyl residue at position 7 is not necessary for binding of antagonist to the receptor, the exact opposite of what is seen in agonists. This suggests that antagonists bind to the receptor in a manner which is very different from that of agonists.
D000818:Animals; D002462:Cell Membrane / Q000378:metabolism; D007679:Kidney Medulla / Q000378:metabolism; D007700:Kinetics; D011487:Protein Conformation; D011945:Receptors, Angiotensin / Q000187:drug effects / Q000378:metabolism; D017483:Receptors, Vasopressin; D013329:Structure-Activity Relationship; D013552:Swine; D014667:Vasopressins / Q000037:antagonists & inhibitors* / Q000494:pharmacology
D011945:Receptors, Angiotensin; D017483:Receptors, Vasopressin; D014667:Vasopressins