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- Title
Tachykinin Receptors Mediating Contractions Of Oestrogen-Primed Rat Uterus: Classification Using Non-Peptide Antagonists.
- Authors
Fisher, L; Pennefather, Jn; Pennefather, Jocelyn
- Abstract
SUMMARY1. The aim of the present study was to characterize the tachykinin receptors mediating contractions of the uterus from the oestrogen-primed rat. Apparent pKB values versus mammalian tachykinins and some subtype-selective agonists were determined for the non-peptide NK1, NK2 and NK3 receptor antagonists SR 140333, SR 48968 and SR 142801, respectively. 2. Apparent pKB values for SR 48968 tested at concen- trations of 3, 10 and 30 nmol/L versus neurokinin (NKA, [Lys5MeLeu9Nle10] NKA(4–10) and [Nle10] NKA(4–10) were 8.79, 9.44 and 9.33, respectively, indicating activation of an NK2 receptor and, in the case of NKA, the possible activation of an additional receptor subtype. SR 48968 (30 nmol/L) did not affect responses to NKB (1 μmol/L), senktide (30 nmol/L), substance P (SP; 100 nmol/L) or [Sar9Met(O2)11] SP (100 nmol/L), indicating its selectivity at this concentration. 3. SR 140333 (1–100 nmol/L) reduced the effects of the NK1-preferring agonists SP and [Sar9Met(O2)11] SP, indicating the presence of NK1 receptors. The pKB estimate versus [Sar9Met(O2)11] was 9.01. SR 140333 (100 nmol/L) did not affect responses to NK2 and NK3 receptor-preferring agonists. 4. SR 142801 (100 nmol/L to 1 μmol/L) produced small rightward shifts in the log concentration–response curves to NKB, yielding an apparent pKB value of 7.0. At 1 μmol/L, SR 142801 reduced responses to the NK2 agonists, suggesting some non-selectivity at this concentration. 5. Taken together, these data provide strong evidence that tachykinin-induced contractions of the uterus of the oestrogen-primed rat are mediated by NK2 receptors, with some contribution from...
- Subjects
TACHYKININS; UTERINE contraction; TACHYKININ antagonists
- Publication
Clinical & Experimental Pharmacology & Physiology, 1999, Vol 26, Issue 9, p729
- ISSN
0305-1870
- Publication type
Article
- DOI
10.1046/j.1440-1681.1999.03119.x