Nieber K, Milenov K, Rakovska A, Henklein P, Oehme P
Institute of Drug Research, Academy of Sciences, Berlin-GDR.
Methods Find Exp Clin Pharmacol. 1988 Aug;10(8):513-20.
Cholecystokinin 7 (CCK 7), a synthetic analogue of cholecystokinin/pancreozymin (CCK 33), increased in a dose-dependent manner the tone of the guinea-pig ileal, gastric and gall bladder smooth muscle preparations. In all these preparations CCK 7 was more potent than CCK 8 and CCK 33 and all three cholecystokinins were more potent than acetylcholine (ACH). Atropine and tetrodotoxin (TTX) did not influence the CCK 7 action in fundus and gall bladder muscle strips but reduced non-competitively its effect in ileal muscle strips. Neither GE 410 nor dbcGMP affected the ACH and histamine (His) response of the muscle strips but both antagonists shifted the dose-response curve of CCK 7 to the right, GE 410 (cholecystokinin antagonist) being a much more potent antagonist of CCK 7 as compared to dbcGMP. In all muscle strips a competitive action on the CCK 7 responses was found for GE 410. In gastric muscle strips a competitive influence on the CCK 7 responses was found for dbcGMP at low concentration (1 x 10(-5)M) and a non-competitive influence at high concentration (5 x 10(-4)M). The results suggest that the contractile effects of CCK 7 in the isolated ileal smooth muscle are realized by cholinergic and direct myogenic mechanisms, whereas in the isolated gall bladder and gastric smooth muscles, by a direct myogenic mechanism only.
胆囊收缩素7(CCK 7),一种胆囊收缩素/促胰酶素(CCK 33)的合成类似物,能以剂量依赖的方式增加豚鼠回肠、胃和胆囊平滑肌标本的张力。在所有这些标本中,CCK 7比CCK 8和CCK 33更有效,并且这三种胆囊收缩素都比乙酰胆碱(ACH)更有效。阿托品和河豚毒素(TTX)不影响CCK 7对胃底和胆囊肌条的作用,但能非竞争性地降低其对回肠肌条的作用。GE 410和二丁酰环磷鸟苷(dbcGMP)都不影响肌条对ACH和组胺(His)的反应,但这两种拮抗剂都使CCK 7的剂量反应曲线右移,与dbcGMP相比,GE 410(胆囊收缩素拮抗剂)是一种对CCK 7更有效的拮抗剂。在所有肌条中,发现GE 410对CCK 7的反应具有竞争性作用。在胃肌条中,低浓度(1×10⁻⁵M)的dbcGMP对CCK 7的反应具有竞争性影响,高浓度(5×10⁻⁴M)时具有非竞争性影响。结果表明,CCK 7在离体回肠平滑肌中的收缩作用是通过胆碱能和直接肌源性机制实现的,而在离体胆囊和胃平滑肌中,仅通过直接肌源性机制实现。