ENHANCEMENT OF INVITRO BINDING AND SOME OF THE PHARMACOLOGICAL PROPERTIES OF DIAZEPAM BY A NOVEL ANTHELMINTIC AGENT, AVERMECTIN-B1A

被引:56
作者
WILLIAMS, M
YARBROUGH, GG
机构
[1] Merck Institute for Therapeutic Research, West Point
关键词
!sup]3[!/sup]H-Diazepam binding; Anthelmintic; Diazepam;
D O I
10.1016/0014-2999(79)90183-3
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
A novel macrocyclic lactone disaccharide anthelmintic agent, Avermectin B1a (AVM) has been found to cause a concentration-dependent increase in the in vitro binding of 3H-diazepam to rat and mouse brain membranes. The increase in binding is manifested as both an increase in the affinity and number of binding sites for 3H-diazepam. Preliminary in vivo studies demonstrate that AVM can also enhance some of the pharmacological actions of diazepam. © 1979.
引用
收藏
页码:273 / 276
页数:4
相关论文
共 10 条
  • [1] CYCLIC ADENOSINE MONOPHOSPHATE PHOSPHODIESTERASE IN BRAIN - EFFECT ON ANXIETY
    BEER, B
    CHASIN, M
    VOGEL, JR
    CLODY, DE
    HOROVITZ, ZP
    [J]. SCIENCE, 1972, 176 (4033) : 428 - +
  • [2] IS THE BENZODIAZEPINE RECEPTOR COUPLED TO A CHLORIDE ANION CHANNEL
    COSTA, T
    RODBARD, D
    PERT, CB
    [J]. NATURE, 1979, 277 (5694) : 315 - 317
  • [3] FRITZ LC, P NAT ACAD SCI US
  • [4] Haefely W, 1975, Adv Biochem Psychopharmacol, P131
  • [5] MACKERER CR, 1978, P SOC EXP BIOL MED, V158, P393
  • [6] MOHLER H, 1977, LIFE SCI, V20, P2102
  • [7] NEILSEN M, 1978, BRAIN RES, V141, P342
  • [8] BENZODIAZEPINE RECEPTORS IN RAT-BRAIN
    SQUIRES, RF
    BRAESTRUP, C
    [J]. NATURE, 1977, 266 (5604) : 732 - 734
  • [9] GABAERGIC MODULATION OF BENZODIAZEPINE BINDING-SITE SENSITIVITY
    TALLMAN, JF
    THOMAS, JW
    GALLAGER, DW
    [J]. NATURE, 1978, 274 (5669) : 383 - 385
  • [10] WILLIAMS M, 1979, LIFE SCI, V24