據(jù)6月19日的《科學(xué)》雜志報(bào)道說(shuō)，一種轉(zhuǎn)運(yùn)蛋白配體（或稱結(jié)合分子）看來(lái)能夠抵消在小鼠以及人類中的焦慮癥和驚恐發(fā)作,，而且它沒(méi)有與其它的當(dāng)前療法相關(guān)的負(fù)面的副作用,。 這些發(fā)現(xiàn)表明，這種叫做XBD173的配體可能成為一個(gè)安全及快速起效的抗焦慮癥的良好的候選藥物,。 目前的諸如benzodiazepines的療法常常存在有害的副作用：如鎮(zhèn)靜,、耐受或在長(zhǎng)期使用之后會(huì)出現(xiàn)戒斷癥狀等。 抗憂郁癥藥物有時(shí)也被用來(lái)治療焦慮癥,，但它們的療效僅僅是在幾個(gè)星期的治療之后才會(huì)出現(xiàn),。
為了尋找新的治療方法，Rainer Rupprecht及其同僚給實(shí)驗(yàn)室大鼠施用了XBD173,。他們觀察到,，XBD173幾乎能夠立刻防止驚恐行為的發(fā)生,，而這些大鼠不會(huì)出現(xiàn)耐受性或任何有害的副作用,。 他們接著在70位健康男性中進(jìn)行有關(guān)的研究，其中還包括一個(gè)服用安慰劑的小組,。他們發(fā)現(xiàn),，XBD173可快速啟動(dòng)一種抗焦慮反應(yīng)且不會(huì)在長(zhǎng)期使用之后出現(xiàn)任何的戒斷癥狀。 文章的作者說(shuō),，XBD173可通過(guò)調(diào)節(jié)抑制性的神經(jīng)遞質(zhì)GABA來(lái)促進(jìn)其鎮(zhèn)靜效果,。他們表示,，這種配體可被考慮在未來(lái)用于臨床。（生物谷Bioon.com）
生物谷推薦原始出處：
Science June 18, 2009 DOI: 10.1126/science.1175055
Translocator Protein (18 kD) as Target for Anxiolytics Without Benzodiazepine-Like Side Effects
Rainer Rupprecht 1*, Gerhard Rammes 2, Daniela Eser 3, Thomas C. Baghai 3, Cornelius Schüle 3, Caroline Nothdurfter 1, Thomas Troxler 4, Conrad Gentsch 4, Hans O. Kalkman 4, Frederique Chaperon 4, Veska Uzunov 4, Kevin H. McAllister 4, Valerie Bertaina-Anglade 5, Christophe Drieu La Rochelle 5, Dietrich Tuerck 6, Annette Floesser 4, Beate Kiese 7, Michael Schumacher 8, Rainer Landgraf 9, Florian Holsboer 9, Klaus Kucher 4
1 Department of Psychiatry and Psychotherapy, Ludwig Maximilian University, Nussbaumstrasse 7, Munich, 80336 Germany.; Max-Planck-Institute of Psychiatry, Kraepelinstrasse 2, Munich, 80804 Germany.
2 Max-Planck-Institute of Psychiatry, Kraepelinstrasse 2, Munich, 80804 Germany.; Department of Anaesthesiology, Technische Universit?t, Munich, Germany.
3 Department of Psychiatry and Psychotherapy, Ludwig Maximilian University, Nussbaumstrasse 7, Munich, 80336 Germany.
4 Novartis Institute for Biomedical Research (NIBR), Neuroscience, Basel, Switzerland.
5 Biotrial, Rennes, France.
6 DMPK, F. Hoffmann-La Roche AG, Basel, Switzerland.
7 Biostatistics, Novartis Pharma AG, Basel, Switzerland.
8 INSERM UMR 788, Paris, France.
9 Max-Planck-Institute of Psychiatry, Kraepelinstrasse 2, Munich, 80804 Germany.
Most antianxiety drugs (anxiolytics) work by modulating neurotransmitters in the brain. Benzodiazepines are fast and effective anxiolytic drugs; however, their long-term use is limited by development of tolerance and withdrawal symptoms. Ligands of the translocator protein (18 kD) may promote the synthesis of endogenous neurosteroids, which also exert anxiolytic effects in animal models. Here, we found that the translocator protein (18 kD) ligand XBD173 enhanced GABAergic neurotransmission and counteracted induced panic attacks in rodents in the absence of sedation and tolerance development. XBD173 also exerted antipanic activity in humans and, in contrast to benzodiazepines, did not cause sedation and withdrawal symptoms. Thus, translocator protein (18 kD) ligands are promising candidates for fast-acting anxiolytic drugs with less severe side effects than benzodiazepines.
