W. KehrH.H. SchneiderR. SchmiechenElsevier B.V.Behavioural Brain ResearchStephens DN, Kehr W, Schneider HH, Schmiechen R (1984) Characterisation of agonist, inverse agonist and partial agonist activities of β-carbolines in a drug-discrimination paradigm (Abstract). Behav Brain Res (in press)
部份作用剂(partial agonists):不能像完全作用剂一样产生最大的效应, 但它能对抗完全作用剂的效应。 其它一些相关的名 … www.docin.com|基于2个网页 3. 部分协同剂 5 5 受体协同剂(Agonist)分为经典协同剂(Conventional agonists)、反向协同剂 (Inverse agonists)和部分协同剂(Partial agonists)。
Salmeterol is a partial agonist for the β2 adrenergic receptor (β2AR) and the first long-acting β2AR agonist to be widely used clinically for the treatment of asthma and chronic obstructive pulmonary disease. Salmeterol’s safety and mechanism of action have both been controversial. To unders...
In drug design, G protein-coupled receptor (GPCR) partial agonists enable one to fine-tune receptor output between basal and maximal signaling levels. Here, we add to the structural basis for rationalizing and monitoring partial agonism. NMR spectroscopy of partial agonist complexes of the A2A aden...
[J] . Faga LA, Sorensen BR, VanScyoc WS, Proteins: Structure, Function, and Genetics . 2003,第3期 机译:钙调蛋白中的基本域间边界残基通过稳定螺旋-螺旋相互作用降低了位点I和II的钙亲和力。 3. Systemic administration of the benzodiazepine receptor partial inverse agonist FG-7142 disrupts corticoli...
However, the original Loewe model cannot accommodate concentration-response curves with different maximal responses and, by consequence, combinations of an agonist with a partial or inverse agonist. We propose an extension, named Biochemically Intuitive Generalized Loewe (BIGL), that can address ...
Photolabeling of the benzodiazepine receptor, which to date has been done with benzodiazepine agonists such as flunitrazepam, can also be achieved with Ro 15-4513, a partial inverse agonist of the benzodiazepine receptor. [3H]Ro 15-4513 specifically and irreversibly labeled a protein with an ...
1 (5-HT-1 ~). The compounds of the invention are useful in the treatment or prevention of depression, anxiety, obsessive compulsive disorder (DOC) and other disorders for which a 5-HT-1 agonist or antagonist is indicated.MICHAEL AARON BRODNEY...
We have tested the ability of lurasidone, an atypical APD with potent 5-HTpartial agonist properties, tandospirone, a selective 5-HTpartial agonist, haloperidol, a Dantagonist, and pimavanserin, a 5-HTinverse agonist, to prevent the development of the PCP-induced NOR deficit. Rats were ...
Combination of serotonin reuptake inhibitor and 5-HT2C antagonist, inverse agonist or partial agonist本发明涉及具有血清素再摄取抑制活性和5-HT The present invention relates to a serotonin reuptake inhibitory activity and 5-HTT·I·F·H·克雷默斯...