Burcher E, Alouan L A, Johnson P R, Black J L
Department of Pharmacology, University of Sydney, NSW, Australia.
Neuropeptides. 1991 Oct;20(2):79-82. doi: 10.1016/0143-4179(91)90055-n.
Cumulative contractile response curves to neurokinin A (NKA) and neuropeptide gamma (NP gamma) were obtained in human isolated bronchus, in the presence of phosphoramidon 10 microM. NP gamma was approximately 10-fold more potent than NKA (pD2 values 8.6 +/- 0.4 and 7.3 +/- 0.3 respectively, n = 6; P less than 0.01). The NK1-selective agonist [Sar9, Met(O2)11]-SP and the NK3 selective agonist senktide produced negligible contraction. Response curves to NP gamma and NKA were unaffected by the NK2 subtype-selective antagonist MDL 29913 at 2 microM, but NP gamma-induced contraction was markedly inhibited by 20 microM MDL 29,913. Thus NP gamma is the most potent tachykinin in human isolated bronchus and its effects are mediated at a receptor which is not of the 'classical' NK2 subtype found in hamster urinary bladder.
在存在10微摩尔磷酰胺的情况下，获得了人离体支气管对神经激肽A（NKA）和神经肽γ（NPγ）的累积收缩反应曲线。NPγ的效力比NKA高约10倍（pD2值分别为8.6±0.4和7.3±0.3，n = 6；P<0.01）。NK1选择性激动剂[Sar9，Met（O2）11]-SP和NK3选择性激动剂senktide产生的收缩可忽略不计。对NPγ和NKA的反应曲线不受2微摩尔NK2亚型选择性拮抗剂MDL 29913的影响，但20微摩尔MDL 29,913可显著抑制NPγ诱导的收缩。因此，NPγ是人类离体支气管中最有效的速激肽，其作用是通过一种受体介导的，该受体不是在仓鼠膀胱中发现的“经典”NK2亚型。
