Partial agonist

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  • Áp dụng điều trị Dùng để giảm đau nhẹ và trung bình. Propoxyphen thường được phối hợp với aspirin hoặc acetaminophen. 2.3.5.

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  • Thuốc kháng progestin Mifepriston Được dùng đầu tiên ở Pháp vào năm 1988 Mifepriston là dẫn xuất của 19 - norprogestin, gắn mạnh vào receptor của progesteron.

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  • Unrecognised sleep-related generalised epileptic seizures disturb sleep achritecture as they cause arousals. Generalized epileptic seizures reduce total sleep time and elongate latency to REM sleep. Amount of NREM1 and NREM2 stages may be extended (Foldvary-Schaefer, 2002). Partial epileptic seizures during sleep do not disrupt night sleep markedly, only in case of their secondary generalization (Dasheiff, 2003). Epileptic seizures during daytime influence night sleep too. They reduce REM sleep, what may be cause of fatigue in postparoxysmal period (Bazil, Castro & Walczak, 2000).

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  • For about four decades now, a course in receptor pharmacology has been given at University College London for undergraduate students in their final year of study for the Bachelor of Science degree in pharmacology. More recently, the course has also been taken by students reading for the Bachelor of Science degree in medicinal chemistry. The students following the course have relied for their reading upon a variety of sources, including original papers, reviews, and various textbooks, but no single text brought together the material included in the course.

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  • Estrogen receptors (ERs) and androgen receptors, members of the steroid hormone family of nuclear receptors, are targets of inhibition by drugs used to treat breast and prostate cancers, respectively. Tamoxifen, a partial agonist and antagonist of ER function, can mediate tumor regression in metastatic breast cancer and can prevent disease recurrence in the adjuvant setting, saving thousands of lives each year. Tamoxifen binds to the ER and modulates its transcriptional activity, inhibiting activity in the breast but promoting activity in bone and uterine epithelium.

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  • Regenerative medicine holds promise not only as a means to compensate for donor shortages, but also as a means to improve the standard of care. In many cases, transplants or medical prosthetics are currently available, but they only offer a partial solution in comparison to the healthy, undamaged physiological state. Therefore it is important for researchers in regenerative medicine to stay mindful of current medical options and continually attempt to improve upon them.

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  • Chemoprevention of Breast Cancer Hormonal manipulation is being tested in the primary prevention of breast cancer. Tamoxifen is an antiestrogen with partial estrogen agonistic activity in some tissues, such as endometrium and bone. One of its actions is to upregulate transforming growth factor β, which decreases breast cell proliferation. In randomized placebo-controlled trials to assess tamoxifen as adjuvant therapy for breast cancer, tamoxifen reduced the number of new breast cancers in the opposite breast by more than a third.

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