INVESTIGATION INTO SPECIES VARIANTS IN TACHYKININ NK1 RECEPTORS BY USE OF THE NONPEPTIDE ANTAGONIST, CP-96,345

被引:229
|
作者
BERESFORD, IJM
BIRCH, PJ
HAGAN, RM
IRELAND, SJ
机构
[1] Department of Neuropharmacology, Glaxo Group Research Ltd., Ware, Hertfordshire, SG12 0DP, Park Road
关键词
TACHYKININ NK1 RECEPTOR; NK1 RECEPTOR ANTAGONIST; SPECIES VARIANTS; SUBTYPE, CP-96,345;
D O I
10.1111/j.1476-5381.1991.tb12423.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The affinity of the non-peptide antagonist CP-96,345 for tachykinin NK1 receptors has been estimated in a range of species by use of both radioligand binding and functional assays. CP-96,345 was 30-120 fold less active at NK1 receptors in rat and mouse than in the other species examined, including man. These results demonstrate the existence of species variations in NK1 receptors.
引用
收藏
页码:292 / 293
页数:2
相关论文
共 50 条
  • [21] INHIBITION OF NEUROGENIC PLASMA EXUDATION IN GUINEA-PIG AIRWAYS BY CP-96,345, A NEW NONPEPTIDE NK(1) RECEPTOR ANTAGONIST
    LEI, YH
    BARNES, PJ
    ROGERS, DF
    BRITISH JOURNAL OF PHARMACOLOGY, 1992, 105 (02) : 261 - 262
  • [22] EFFECT OF CP-96,345, A NONPEPTIDE SUBSTANCE-P RECEPTOR ANTAGONIST, ON SALIVATION IN RATS
    SNIDER, RM
    LONGO, KP
    DROZDA, SE
    LOWE, JA
    LEEMAN, SE
    PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1991, 88 (22) : 10042 - 10044
  • [23] THE EFFECTS OF MORPHINE, MK-801, AN NMDA ANTAGONIST, AND CP-96,345, AN NK1 ANTAGONIST, ON THE HYPERESTHESIA EVOKED BY CARAGEENAN INJECTION IN THE RAT PAW
    YAMAMOTO, T
    SHIMOYAMA, N
    MIZUGUCHI, T
    ANESTHESIOLOGY, 1993, 78 (01) : 124 - 133
  • [24] INHIBITORY EFFECT OF CP-96,345, A NONPEPTIDE NK-1 RECEPTOR ANTAGONIST, ON AUTONOMIC NEUROTRANSMISSION OF THE GUINEA-PIG AIRWAY INVITRO
    KAMIKAWA, Y
    REGULATORY PEPTIDES, 1992, : S85 - S85
  • [25] PHARMACOLOGY OF CP-99,994 - A NONPEPTIDE ANTAGONIST OF THE TACHYKININ NK1 RECEPTOR
    MCLEAN, S
    GANONG, A
    SEYMOUR, PA
    SNIDER, RM
    DESAI, MC
    ROSEN, T
    BRYCE, DK
    LONGO, KP
    REYNOLDS, LS
    ROBINSON, G
    SCHMIDT, AW
    SIOK, C
    HEYM, J
    REGULATORY PEPTIDES, 1992, : S120 - S120
  • [26] REGIONAL BRAIN DISTRIBUTION AND METABOLISM IN GUINEA-PIGS OF [C-11] CP-96,345, A NONPEPTIDE NK-1 ANTAGONIST
    MICKALA, P
    BARRE, L
    DAUPHIN, F
    DEBRUYNE, D
    YOUNG, AR
    SPECKEL, D
    CAMSONNE, R
    MACKENZIE, ET
    BARON, JC
    JOURNAL OF NUCLEAR MEDICINE, 1993, 34 (05) : P241 - P241
  • [27] VARIATIONS IN AFFINITIES FOR THE NK1 RECEPTOR - DIFFERENCES BETWEEN THE NONPEPTIDE SUBSTANCE-P ANTAGONISTS, RP-67580 AND CP-96,345 AND THE AGONIST PEPTIDE
    FARDIN, V
    FOUCAULT, F
    BOCK, MD
    JOLLY, A
    FLAMAND, O
    CLERC, F
    GARRET, C
    REGULATORY PEPTIDES, 1992, : S53 - S53
  • [28] (+/-)-CP-96,345, AN NK1 RECEPTOR ANTAGONIST, HAS LOCAL ANESTHETIC-LIKE EFFECTS IN A MAMMALIAN SCIATIC-NERVE PREPARATION
    KARLSSON, U
    NASSTROM, J
    BERGE, OG
    REGULATORY PEPTIDES, 1994, 52 (01) : 39 - 46
  • [29] EFFECT OF CP-96,345 A NONPEPTIDE SUBSTANCE-P ANTAGONIST, CAPSAICIN, RESINIFERATOXIN AND RUTHENIUM RED ON NOCICEPTION
    SZOLCSANYI, J
    NAGY, J
    PETHO, G
    REGULATORY PEPTIDES, 1993, 46 (1-2) : 437 - 439
  • [30] DIFFERENCES IN THE POTENCY OF CP-96,345 AND RP-67,580, 2 NEW NONPEPTIDE ANTAGONISTS SELECTIVE FOR NK1 RECEPTORS, IN INHIBITING RESPONSES EVOKED BY STIMULATION OF SENSORY NERVES
    DELAYGOYET, P
    SATOH, H
    LUNDBERG, JM
    REGULATORY PEPTIDES, 1992, : S52 - S52