1996
DOI: 10.1111/j.1476-5381.1996.tb15511.x
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Study of SR 142801, a new potent non‐peptide NK3 receptor antagonist on cardiovascular responses in conscious guinea‐pig

Abstract: The cardiovascular responses to intravenous (i.v.) injection of natural tachykinins, substance P (SP), neurokinin A (NKA), neurokinin B (NKB) and selective tachykinin (NK) receptor agonists, [Sar9, Met(O2)11]SP, [βAla8]NKA(4–10), [MePhe7]NKB and senktide were assessed in conscious, freely moving, guinea‐pigs. SP and [Sar9, Met(O2)11]SP (1–1000 pmol kg−1) induced dose‐dependent decreases in mean arterial blood pressure (MAP) accompanied by increases in heart rate (HR). NKA evoked only weak hypotensive effects a… Show more

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Cited by 31 publications
(16 citation statements)
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“…An effect of SR 142801 on NK 1 receptors can also be excluded, since the selectivity of this compound has clearly been demonstrated by radioligand binding and well characterised in vitro by functional assays for tachykinin receptors [21,29,30] 11 ] substance P in guinea pigs and dogs [22,31]. It has also been shown that SR 142801 failed to inhibit tachykinin and capsaicininduced plasma extravasation in the ear skin of mice, an effect that could be suppressed by SR 140333 [32].…”
Section: Discussionmentioning
confidence: 99%
“…An effect of SR 142801 on NK 1 receptors can also be excluded, since the selectivity of this compound has clearly been demonstrated by radioligand binding and well characterised in vitro by functional assays for tachykinin receptors [21,29,30] 11 ] substance P in guinea pigs and dogs [22,31]. It has also been shown that SR 142801 failed to inhibit tachykinin and capsaicininduced plasma extravasation in the ear skin of mice, an effect that could be suppressed by SR 140333 [32].…”
Section: Discussionmentioning
confidence: 99%
“…The compound selectivity has been demonstrated by radioligand binding and well characterized in vitro functional assays for tachykinin receptors ( Beaujouan et al ., 1997 ; Daoui et al ., 1997 ; Emonds‐Alt et al ., 1995 ; Nguyen‐Le et al ., 1996 ; Oury‐Donat et al ., 1995 ; Patacchini et al ., 1995 ). In vivo , the selectivity of SR 142801 is clearly suggested by two assays: in contrast to SR 48968, SR 142801 (1 mg kg −1 ) did not inhibit bronchoconstriction induced by [Nle 10 ]NKA (4‐10) in anaesthetized guinea‐pigs ( Daoui et al ., 1997 ); and unlike SR 140333, SR 142801 (1 mg kg −1 ) failed to inhibit the hypotension induced by [Sar 9 , Met(O 2 ) 11 ]SP in guinea‐pigs and dogs ( Emonds‐Alt et al ., 1993 , 1995 ; Roccon et al ., 1996 ).…”
Section: Discussionmentioning
confidence: 99%
“…In an experimental pig study, Roccon et al [29] reported that intravenous NK-3 agonist increases BP. Interestingly, D'Anna and colleagues have reported a strong correlation between the SBP and neurokinin B levels in pre-eclampsia patients [18].…”
Section: Discussionmentioning
confidence: 98%