Canchola E, Rodríguez-Medina M, Dueñas-Tentori H, Mercado E, Rosado A
División de Ciencias Biológicas y de la Salud, Universidad Autónoma Metropolitana, Unidad Iztapalapa, Mexico City, Mexico.
Pharmacol Biochem Behav. 1996 Jun;54(2):403-7. doi: 10.1016/0091-3057(95)02086-1.
We studied the effect some drugs that participate in the Ca2+/ calmodulin system have on the progesterone (P) facilitation of lordosis behavior in ovariectomized estradiol (E2) primed rats. We injected rats 44 h after E2 priming with 2 mg P together with various dosages of one of the following compounds: pentobarbital, trifluoperazine (TPZ), promethazine (PMZ), Chlorpromazine (CPZ), haloperidol (HAL), pimozide (PIM), and verapamil (VER). Then 4 h after treatment, animals were tested for sexual behavior, expressed as the lordosis quotient (LQ). All drugs at 4 mg/kg or higher inhibited lordosis, but only HAL, PIM, and VER were active at 1 mg/kg. The maximum level of activity was shown by PIM, although at the dose of 8 mg/kg no statistical differences were found between this compound and TPZ or HAL. Pentobarbital (25 mg/kg) showed no significant difference from saline-treated controls. The activity of the tested drugs on the facilitation of sexual behavior appears to be related to their efficiency as inhibitors of calmodulin (CaM)-dependent phosphodiesterase and as ligands for the Ca(2+)-CaM complex.
我们研究了一些参与Ca2+/钙调蛋白系统的药物对去卵巢并用雌二醇（E2）预处理的大鼠中孕酮（P）促进脊柱前凸行为的影响。在E2预处理44小时后，我们给大鼠注射2毫克P以及下列化合物之一的不同剂量：戊巴比妥、三氟拉嗪（TPZ）、异丙嗪（PMZ）、氯丙嗪（CPZ）、氟哌啶醇（HAL）、匹莫齐特（PIM）和维拉帕米（VER）。然后在处理后4小时，对动物进行性行为测试，以脊柱前凸商（LQ）表示。所有4毫克/千克或更高剂量的药物均抑制脊柱前凸，但只有HAL、PIM和VER在1毫克/千克时具有活性。PIM表现出最大活性水平，尽管在8毫克/千克剂量下，该化合物与TPZ或HAL之间未发现统计学差异。戊巴比妥（25毫克/千克）与生理盐水处理的对照组无显著差异。所测试药物对性行为促进的活性似乎与其作为钙调蛋白（CaM）依赖性磷酸二酯酶抑制剂以及作为Ca(2+)-CaM复合物配体的效率有关。
