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Zelinski-Wooten MB; Slayden OD; Chwalisz K; Hess DL; Brenner RM; Stouffer RL 《Human reproduction (Oxford, England)》1998,13(2):259-267
Large doses of antiprogestin typically disrupt menstrual cyclicity. A
chronic low-dose regimen of the potent new antiprogestin ZK 137 316, which
permits continued menstrual cyclicity but alters gonadal- reproductive
tract activity, was established. Rhesus monkeys received vehicle (n = 6) or
0.01 (n = 8), 0.03 (n = 8) or 0.1 (n = 5) mg ZK 137 316/kg body weight
daily for five menstrual cycles (C-1 to C-5). Oestradiol, progesterone and
gonadotrophin profiles were normal during cycles involving vehicle and 0.01
and 0.03 mg ZK 137 316/kg body weight. In the 0.1 mg/kg group, mid-cycle
oestradiol and gonadotrophin surges, and subsequent progesterone
production, were absent in C-3 and C-5. Ovarian cyclicity was accompanied
by timely menstruation in the vehicle and 0.01 mg/kg groups. By C-3, half
the animals in the 0.03 mg/kg group and all animals in the 0.1 mg/kg group
were amenorrhoeic. A corpus luteum was noted during the mid-luteal phase of
C-5 in the vehicle, 0.01 mg/kg and 0.03 mg/kg groups. Large antral and
cystic follicles were evident in the 0.1 mg/kg group. Thus, a daily
treatment with 0.01 mg/kg ZK 136317 permitted normal menstrual cyclicity in
macaques. While the daily administration of 0.03 mg/kg ZK 136 317 allowed
ovarian cyclicity, menstruation was disrupted in some animals. Increasing
the dose to 0.1 mg/kg antagonized pituitary function and resulted in
anovulation and amenorrhoea. A chronic low-dose regimen of the
antiprogestin ZK 137 316, which permits normal ovarian/menstrual cyclicity,
has potential as a contraceptive in women.
相似文献
26.
Benzodiazepine receptors in the human spinal cord: a detailed anatomical and pharmacological study 总被引:7,自引:0,他引:7
The anatomical distribution and pharmacological characteristics of benzodiazepine receptors in the human spinal cord were examined in four cases aged 20-41 years using in vitro autoradiography and biochemical assays of [3H]flunitrazepam binding. In all cases, the autoradiograms demonstrated that benzodiazepine receptors were distributed in a consistently similar fashion in the gray matter of the cervical, thoracic, lumbar and sacral regions of the human spinal cord. At all levels, the highest densities of benzodiazepine receptors were found to be localized within lamina II of the dorsal horn as defined on cytoarchitectonic, myeloarchitectonic and substance P immunocytochemical criteria. Within this lamina the receptors were concentrated mainly in its deeper, inner portion which lies immediately adjacent to lamina III, with some overlap dorsally into the outer segment of lamina II and ventrally into the adjacent region of lamina III. The lowest density of receptors was found in regions of laminae I, IV, VII and X; in particular, in lamina VII the lowest concentration of receptors was found in the dorsal nucleus of Clarke and the sacral parasympathetic nucleus. The remaining laminae of the spinal gray (laminae, V, VI, VIII and IX) showed a moderate density of receptors. Biochemical assays of membranes prepared from the lumbosacral cord indicated that these [3H]flunitrazepam binding sites have high affinity and have the pharmacological characteristics of the "central" Type II benzodiazepine receptor. These results show a high concentration of Type II benzodiazepine receptors in the substantia gelatinosa of the human spinal cord and suggest a possible role for these receptors in spinal sensory functions. 相似文献
27.
The phencyclidine (PCP) binding site of the N-methyl-D-aspartate receptor, the kainic acid (KA) receptor and the quisqualate (QA) receptor were visualised, using autoradiography in the human spinal cord and the distributions compared with that of benzodiazepine (BDZ) receptors and substance P (SP). All of the receptor types, and SP, were concentrated in lamina II of the dorsal horn, consistent with physiological data indicating that glutamate is a neurotransmitter of primary afferent terminals in the spinal cord. 相似文献
28.
We performed a randomized doubled-blind study to evaluate whether there was a benefit in delay in tourniquet deflation with intra-articular administration of morphine and bupivacaine following operative arthroscopic surgery. In 34 patients the tourniquet was deflated immediately and in 38 patients the tourniquet remained inflated for 10 min following injection. The analgesic efficacy was assessed using pain scores and the amount of supplementary analgesia required. The results demonstrate no benefit in delay in tourniquet deflation. 相似文献
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The use of specialized coils to improve signal-to-noise ratios in magnetic resonance (MR) imaging is an important innovation. The role of surface coils has not yet been well defined, but it seems likely that they will be routinely used for clinical imaging of the orbit, neck, and spine. Surface coils have important limitations that make other designs, such as "closely coupled" volume coils, attractive for some applications, especially for limb imaging. With improvement in our ability to visualize anatomy with MR imaging, specialized radio frequency coils may provide new imaging capabilities for clinical problems that were not previously considered to be indications for diagnostic imaging. 相似文献