ISSN:
1573-3904
Keywords:
Oxytocin
;
Antagonists
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
Notes:
Summary [Aib3,Thr5]OT, [Aib3,Thr(OMe)5]OT, [Aib3,Orn8]OT, [Thr(OMe)5,Orn8]OT and [Phe2,Thr(OMe)5,Orn8]OT were synthesized by solid-phase techniques. From the biological properties of these peptides, it seems that the simultaneous replacement of positions 3 and 5 of oxytocin with Aib and Thr(OMe) results in an analogue devoid of antagonistic activity in comparison with the singly substituted compounds. Simultaneous Orn8 substitution does the same in the case of the Aib3 analogue and even leads to agonistic activity in the case of the Thr(OMe)5 analogue. Replacement of Tyr2 by Phe2, e.g. [Phe2,Thr(OMe)5,Orn8]OT, again favors the appearance of minor antagonistic potency.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF00128110
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