Makovec F, Bani M, Chistè R, Revel L, Rovati L C, Setnikar I
Regul Pept. 1986 Dec 30;16(3-4):281-90. doi: 10.1016/0167-0115(86)90027-3.
New glutaramic acid derivatives with cholecystokinin antagonistic activity were evaluated for their capacity to inhibit the satiety effect induced in the rat by intraperitoneal (i.p.) injection of cholecystokinin octapeptide (CCK-8). The most active compound, CR 1409, is about 4000 times more potent than proglumide when injected peripherally (i.p.). This compound competitively inhibits the action of CCK-8 at the receptor responsible for the satiety effect. In contrast, CR 1409, i.p. or intracerebroventricularly (i.c.v.) injected does not exhibit antagonistic effects when CCK-8 is administered i.c.v., confirming the existence of at least two different populations of CCK receptors.
对具有胆囊收缩素拮抗活性的新型谷氨酸衍生物进行了评估，以测定它们抑制腹腔注射八肽胆囊收缩素（CCK-8）诱导的大鼠饱腹感效应的能力。活性最强的化合物CR 1409，经外周（腹腔）注射时，其效力比丙谷胺强约4000倍。该化合物在负责饱腹感效应的受体处竞争性抑制CCK-8的作用。相比之下，当通过脑室内注射CCK-8时，腹腔注射或脑室内注射CR 1409均未表现出拮抗作用，这证实了至少存在两种不同类型的CCK受体。
