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一氧化氮和对Septide不敏感的NK(1)受体在豚鼠雾化神经激肽A诱导的支气管收缩中的作用

Role of nitric oxide and septide-insensitive NK(1) receptors in bronchoconstriction induced by aerosolised neurokinin A in guinea-pigs.

作者信息

Ricciardolo F L, Trevisani M, Geppetti P, Nadel J A, Amadesi S, Bertrand C

机构信息

Cardiovascular Research Institute, University of California San Francisco, San Francisco, California, USA.

出版信息

Br J Pharmacol. 2000 Mar;129(5):915-20. doi: 10.1038/sj.bjp.0703135.

Abstract

The tachykinin, neurokinin A (NKA), contracts guinea-pig airways both in vitro and in vivo, preferentially activating smooth muscle NK(2) receptors, although smooth muscle NK(1) receptors may also contribute. In vitro evidence suggests that NKA activates epithelial NK(1) receptors, inducing the release of nitric oxide (NO) and subsequent smooth muscle relaxation. A number of selective NK(1) receptor agonists have been reported to activate both smooth muscle and epithelial NK(1) receptors, however septide appears only to activate smooth muscle NK(1) receptors. The aim of the present study was to investigate whether NKA-induced bronchoconstriction in guinea-pigs in vivo may be limited by NO release via NK(1) receptor activation, and whether selective NK(1) receptor agonists may activate this mechanism differently. Aerosolized NKA caused an increase in total pulmonary resistance (RL) that was markedly reduced by the NK(2) receptor antagonist, SR 48968, and abolished by the combination of SR 48968 and the NK(1) receptor antagonist, CP-99, 994. The increase in RL evoked by NKA was potentiated by pretreatment with the NO synthase (NOs) inhibitor, L-NAME, but not by the inactive enantiomer D-NAME. Potentiation by L-NAME of NKA-induced increase in RL was reversed by L-Arginine, but not by D-Arginine. Pretreatment with L-NAME did not affect the increase in RL induced by the selective NK(2) receptor agonist, [beta-Ala(8)]NKA(4-10), and by the selective NK(1) receptor agonist, septide, whereas it markedly potentiated the increase in RL caused by a different NK(1) selective agonist, [Sar(9),Met(O(2))(11)]SP. Dose-response curves showed that septide was a more potent bronchoconstrictor than [Sar(9),Met(O(2))(11)]SP to cause bronchoconstriction. Pretreatment with the NK(1) receptor antagonist, CP-96,994, abolished the ability of L-NAME to increase bronchoconstriction to aerosolized NKA. Bronchoconstriction to aerosolized NKA was increased by L-NAME, after pretreatment with the NK(3) receptor antagonist, SR 142801. The present study shows that in vivo bronchoconstriction in response to the aerosolized naturally occurring tachykinin, NKA, is limited by its own ability to release relaxant NO via NK(1) receptor activation. This receptor is apparently insensitive to septide, thus justifying, at least in part, the high potency of septide to cause bronchoconstriction in guinea-pigs.

摘要

速激肽神经激肽A(NKA)在体外和体内均可使豚鼠气道收缩,优先激活平滑肌NK(2)受体,不过平滑肌NK(1)受体也可能起作用。体外证据表明,NKA激活上皮NK(1)受体,诱导一氧化氮(NO)释放并随后使平滑肌舒张。据报道,多种选择性NK(1)受体激动剂可激活平滑肌和上皮NK(1)受体,然而,七肽似乎仅激活平滑肌NK(1)受体。本研究的目的是调查在豚鼠体内,NKA诱导的支气管收缩是否可能受经由NK(1)受体激活释放的NO的限制,以及选择性NK(1)受体激动剂是否可能以不同方式激活这一机制。雾化吸入NKA导致总肺阻力(RL)增加,NK(2)受体拮抗剂SR 48968可使其显著降低,而SR 48968与NK(1)受体拮抗剂CP-99,994联合使用则可消除该作用。NKA引起的RL增加可被一氧化氮合酶(NOs)抑制剂L-NAME预处理增强,但无活性的对映体D-NAME则无此作用。L-NAME对NKA诱导的RL增加的增强作用可被L-精氨酸逆转,但不能被D-精氨酸逆转。L-NAME预处理不影响选择性NK(2)受体激动剂[β-丙氨酸(8)]NKA(4-10)和选择性NK(1)受体激动剂七肽诱导的RL增加,而它可显著增强另一种NK(1)选择性激动剂[Sar(9),Met(O(2))(11)]SP引起的RL增加。剂量反应曲线表明,七肽作为支气管收缩剂比[Sar(9),Met(O(2))(11)]SP更有效。NK(1)受体拮抗剂CP-96,994预处理可消除L-NAME增强雾化吸入NKA引起的支气管收缩的能力。在用NK(3)受体拮抗剂SR 142801预处理后,L-NAME可增加雾化吸入NKA引起的支气管收缩。本研究表明,在体内,对雾化吸入的天然存在的速激肽NKA的支气管收缩反应受其自身经由NK(1)受体激活释放舒张性NO的能力的限制。该受体显然对七肽不敏感,因此至少部分地解释了七肽在豚鼠中引起支气管收缩的高效性。

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