Fontaine J, Ouedraogo C, Famaey J P
Arch Int Pharmacodyn Ther. 1985 Jun;275(2):217-30.
Primaquine (10(-6) to 4.10(-5) M), an antimalarial drug, has stimulatory effects on the guinea-pig ileum which seem to be related to stimulation of histaminergic H1-receptors. Preincubation of the preparations with compound 48/80 greatly inhibits the primaquine induced contractions, indicating that they should result from histamine release. On the other hand, primaquine (from 10(-6) M) like 2 other 8-aminoquinolines, pamaquine and pentaquine, has inhibitory properties on the intramural cholinergic neurones of the ileum, and at higher concentrations (10(-5) M) exerts a direct inhibition on the smooth muscle.
抗疟药伯氨喹(10⁻⁶至4×10⁻⁵M)对豚鼠回肠有刺激作用,这似乎与组胺能H1受体的刺激有关。将制剂与化合物48/80预孵育可大大抑制伯氨喹诱导的收缩,表明这些收缩应源于组胺释放。另一方面,伯氨喹(从10⁻⁶M起)与另外两种8-氨基喹啉(扑疟喹和戊喹)一样,对回肠壁内胆碱能神经元具有抑制特性,且在较高浓度(10⁻⁵M)时对平滑肌有直接抑制作用。