PMID- 3383999
OWN - NLM
STAT- MEDLINE
DCOM- 19880808
LR  - 20190624
IS  - 0014-2999 (Print)
IS  - 0014-2999 (Linking)
VI  - 148
IP  - 1
DP  - 1988 Mar 22
TI  - Effects of vasopressin on the human non-pregnant uterus: studies with analogues 
      of different vasopressor potencies.
PG  - 93-9
AB  - The uterotonic effects of arginine8-vasopressin (AVP) have been studied on 
      uterine strips from non-pregnant women. Concentration-dependent contractions 
      could be recorded over a 10 min period in the presence of AVP 
      (5.5.10(-10)-3.10(-7) M); the most reproducible recordings were obtained with 
      tissue from the inner part of the myometrium. Analogues of AVP and oxytocin (OT), 
      modified at positions 1 (2-hydroxy-3-mercaptopropionic acid, 
      deamino-3-mercaptopropionic acid), 2 (Phe), 4 (Arg, Val), 7 (Sar) or 8 (Orn) were 
      synthesized and tested for uterotonic activity on human and rat uterine strips, 
      and for vasopressor and antidiuretic activity in the rat in vivo. There was a 
      positive correlation between the activity of these analogues on non-pregnant 
      human myometrial tissue with that in the rat vasopressor assay (r = 0.86, P less 
      than 0.01) but none with their activity in the antidiuretic assay. For example, 
      [Mpa1,D-Arg8]vasopressin had more than twice the antidiuretic activity of AVP but 
      less than 0.2% of its pressor or human uterotonic potency (Mpa = 
      3-mercaptopropionic acid). Correspondingly, the specific pressor analogue 
      [Hmp1,Phe2,Orn8]OT was as potent as AVP on the human uterus, but had less than 3% 
      of its antidiuretic activity (Hmp = 2-hydroxy-3-mercaptopropionic acid). There 
      was no correlation between the uterotonic activities of AVP or its analogues when 
      non-pregnant human and rat tissues were compared, indicating that rat uterine 
      tissue is a poor guide when testing analogues intended for clinical use in 
      non-pregnant women.(ABSTRACT TRUNCATED AT 250 WORDS)
FAU - Melin, P
AU  - Melin P
AD  - Research Department, Ferring Pharmaceuticals, Malmo, Sweden.
FAU - Trojnar, J
AU  - Trojnar J
FAU - Carlsson, A M
AU  - Carlsson AM
FAU - Bengtsson, B
AU  - Bengtsson B
FAU - Akerlund, M
AU  - Akerlund M
FAU - Robinson, I
AU  - Robinson I
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Netherlands
TA  - Eur J Pharmacol
JT  - European journal of pharmacology
JID - 1254354
RN  - 0 (Peptide Fragments)
RN  - 113-79-1 (Arginine Vasopressin)
RN  - 87619-87-2 (argipressin (4-9))
SB  - IM
MH  - Adult
MH  - Animals
MH  - Arginine Vasopressin/*pharmacology
MH  - Blood Pressure/drug effects
MH  - Diuresis/drug effects
MH  - Female
MH  - Humans
MH  - In Vitro Techniques
MH  - Middle Aged
MH  - Peptide Fragments/*pharmacology
MH  - Rats
MH  - Uterine Contraction/*drug effects
EDAT- 1988/03/22 00:00
MHDA- 1988/03/22 00:01
CRDT- 1988/03/22 00:00
PHST- 1988/03/22 00:00 [pubmed]
PHST- 1988/03/22 00:01 [medline]
PHST- 1988/03/22 00:00 [entrez]
AID - 0014-2999(88)90457-8 [pii]
AID - 10.1016/0014-2999(88)90457-8 [doi]
PST - ppublish
SO  - Eur J Pharmacol. 1988 Mar 22;148(1):93-9. doi: 10.1016/0014-2999(88)90457-8.