对自由活动的自发性高血压大鼠进行脊髓上给药[D-蛋氨酸2]FMRF酰胺，可使心率出现纳洛酮敏感的增加。

Supraspinal administration of [D-Met2]FMRFamide produces a naloxone-sensitive increase in heart rate in unrestrained spontaneously hypertensive rats.

作者信息

Raffa R B, Addo M F, Gill A

机构信息

Drug Discovery Research, R. W. Johnson Pharmaceutical Research Institute, Spring House, PA 19477-0776.

出版信息

Neuropeptides. 1992 Apr;21(4):201-5. doi: 10.1016/0143-4179(92)90023-p.

DOI:10.1016/0143-4179(92)90023-p

PMID:1355596

Abstract

Intracerebroventricular (i.c.v.) administration of either Phe-Met-Arg-Phe-NH2 (FMRFamide; molluscan cardioexcitatory neuropeptide; 3-30 micrograms) or the FMRFamide analog Phe-D-Met-Arg-Phe-NH2 ([D-Met2]FMRFamide; 15 micrograms) to conscious unrestrained spontaneously hypertensive rats (SHR) produced a relatively long lasting (greater than 1 h) increase in heart rate. The increase in heart rate produced by [D-Met2]FMRFamide was attenuated by i.c.v. injection of the opiate antagonist naloxone (2 micrograms). These results extend to a second endpoint an apparent opioid agonist-like (naloxone-reversible) action of [D-Met2]FMRFamide.

摘要

向清醒、不受束缚的自发性高血压大鼠（SHR）脑室内（i.c.v.）注射苯丙氨酸 - 蛋氨酸 - 精氨酸 - 苯丙氨酸 - 酰胺（FMRF酰胺；软体动物心脏兴奋神经肽；3 - 30微克）或FMRF酰胺类似物苯丙氨酸 - D - 蛋氨酸 - 精氨酸 - 苯丙氨酸 - 酰胺（[D - Met2]FMRF酰胺；15微克），可使心率产生相对持久（大于1小时）的增加。[D - Met2]FMRF酰胺引起的心率增加可被脑室内注射阿片拮抗剂纳洛酮（2微克）减弱。这些结果将[D - Met2]FMRF酰胺的一种明显的阿片样激动剂样（纳洛酮可逆）作用扩展到了第二个终点。