Rusterholz D B, Long J P, Flynn J R, Glyn J R, Barfknecht C F, Lind R W, Johnson A K
Arch Int Pharmacodyn Ther. 1978 Apr;232(2):246-60.
In order to elucidate the pharmacological properties of a series of 1-phenyl-2-aminopropane and 2-amino-1, 2, 3, 4-tetrahydronaphthalene derivatives, their ability to inhibit a number of apomorphine-induced behaviors was investigated. Several members of the series under study were potent inhibitors of apomorphine-induced pecking behavior in pigeons, emesis in dogs, and gnawing in rats. In addition, these compounds were able to inhibit responding in self-stimulating rats and to a lesser degree counteracted the depression of the linguomandibular reflex induced by 5, 6-dihydroxy-2-dimethylamino-1, 2, 3, 4-tetrahydronaphthalene (M-7) in the cat. The most effective member of the experimental compounds was N-methyl-5, 8-dimethoxy-2-amino-1, 2, 3, 4-tetrahydronaphthalene; however, neither this material nor any of the related structures were able to inhibit apomorphine-induced rotational behavior in substantia nigra lesioned rats. The possibility that the more effective members of the experimental series are able to inhibit certain apomorphine-induced behaviors by stimulation of central alpha adrenergic receptors is discussed.
为阐明一系列1-苯基-2-氨基丙烷和2-氨基-1,2,3,4-四氢萘衍生物的药理特性,研究了它们抑制多种阿扑吗啡诱导行为的能力。所研究系列中的几种化合物是阿扑吗啡诱导的鸽子啄食行为、狗呕吐和大鼠啃咬行为的有效抑制剂。此外,这些化合物能够抑制自我刺激大鼠的反应,并在较小程度上抵消5,6-二羟基-2-二甲氨基-1,2,3,4-四氢萘(M-7)诱导的猫舌下颌反射抑制。实验化合物中最有效的是N-甲基-5,8-二甲氧基-2-氨基-1,2,3,4-四氢萘;然而,该物质及任何相关结构均不能抑制黑质损伤大鼠的阿扑吗啡诱导的旋转行为。讨论了实验系列中更有效的化合物通过刺激中枢α-肾上腺素能受体抑制某些阿扑吗啡诱导行为的可能性。