Costall B, Kelly M E, Naylor R J
Br J Pharmacol. 1984 Nov;83(3):733-40. doi: 10.1111/j.1476-5381.1984.tb16227.x.
The antidyskinetic action of dihomo-gamma-linolenic acid (DHLA) was assessed against dyskinesias induced in the guinea-pig by dopamine injected into the striatum (200 micrograms bilateral 2 h after nialamide, 75 mg kg-1, i.p.) and in the guinea-pig and rat by 2-di-n-propylamino-5, 6-dihydroxytetralin (tetralin), 0.025 mg kg-1, s.c. Dopamine and tetralin-induced dyskinesias in the guinea-pig were reduced or abolished by DHLA given i.p., 30-100 mg kg-1, given once daily for 5-10 days. Tetralin-induced dyskinesias were antagonized by DHLA given orally to the guinea-pig (50-200 mg kg-1, 5 days) or in the diet to the rat (approximately 200 mg kg-1 daily for 10-14 days). DHLA injected into the striatum (2.5-20 micrograms bilateral, 2-4 days) also antagonized tetralin-induced dyskinesias in the rat. The antidyskinetic action of DHLA given i.p. to the guinea-pig could be antagonized by aspirin or eicosa-5,8,11,14-tetraynoic acid (100 mg kg-1 i.p. daily, starting 2 days before a 5 day treatment with DHLA). Aspirin (25-100 mg kg-1, i.p.) dose-dependently antagonized the antidyskinetic activity of 5 and 20 micrograms DHLA given bilaterally into the striatum (2 days). DHLA (100 mg kg-1 i.p.) given daily for 10 days or approximately 200 mg kg-1 DHLA (daily for 10-14 days given in the diet) administration to the rat failed to modify the stereotyped behaviour induced by apomorphine, 0.5 or 2 mg kg-1 s.c., to induce catalepsy, or to modify the cataleptic effects of haloperidol 0.25 or 1 mg kg-1 i.p. 7 It is suggested that the selective inhibition of dyskinesias in the rodent by DHLA may reflect a striatal effect with a dependency on conversion to prostaglandins.
评估了二高 -γ-亚麻酸(DHLA)对豚鼠纹状体注射多巴胺(烟酰胺75mg kg⁻¹腹腔注射2小时后双侧注射200μg)以及豚鼠和大鼠皮下注射2 - 二正丙基氨基 - 5,6 - 二羟基四氢化萘(四氢化萘)0.025mg kg⁻¹诱导的运动障碍的抗运动障碍作用。腹腔注射30 - 100mg kg⁻¹的DHLA,每日一次,持续5 - 10天,可减轻或消除豚鼠中多巴胺和四氢化萘诱导的运动障碍。给豚鼠口服(50 - 200mg kg⁻¹,5天)或在大鼠饮食中添加(每日约200mg kg⁻¹,持续10 - 14天)DHLA可拮抗四氢化萘诱导的运动障碍。向大鼠纹状体注射DHLA(双侧2.5 - 20μg,2 - 4天)也可拮抗四氢化萘诱导的运动障碍。给豚鼠腹腔注射DHLA的抗运动障碍作用可被阿司匹林或5,8,11,14 - 二十碳四炔酸(100mg kg⁻¹腹腔注射,在开始用DHLA进行5天治疗前2天开始)拮抗。阿司匹林(25 - 100mg kg⁻¹腹腔注射)剂量依赖性地拮抗双侧纹状体注射5μg和20μg DHLA(2天)的抗运动障碍活性。给大鼠每日腹腔注射100mg kg⁻¹的DHLA,持续10天,或在饮食中给予约200mg kg⁻¹的DHLA(每日,持续10 - 14天),未能改变皮下注射0.