Tattersall F D, Rycroft W, Hill R G, Hargreaves R J
Merck, Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, U.K.
Neuropharmacology. 1994 Feb;33(2):259-60. doi: 10.1016/0028-3908(94)90018-3.
These studies have examined the effects of the selective neurokinin1 (NK1) receptor antagonist CP-99,994 on the retching and vomiting response to apomorphine. CP-99,994 (1-3 mg/kg i.p.) attenuated retching and vomiting induced by apomorphine (0.25 mg/kg s.c.) with complete inhibition of retching and vomiting at the 3 mg/kg dose. In contrast CP-100,263 (3 mg/kg i.p.), the enantiomer of CP-99,994 with 1000-fold lower affinity for the NK1 receptor, was without effect.
这些研究检测了选择性神经激肽1（NK1）受体拮抗剂CP-99,994对阿扑吗啡引起的干呕和呕吐反应的影响。CP-99,994（腹腔注射1-3毫克/千克）减轻了阿扑吗啡（皮下注射0.25毫克/千克）引起的干呕和呕吐，在3毫克/千克剂量时完全抑制了干呕和呕吐。相比之下，CP-100,263（腹腔注射3毫克/千克），即CP-99,994的对映体，对NK1受体的亲和力低1000倍，没有效果。
