Receptor inhibitors

Application of the CCM to small sets (n < 6) of enzyme inhibitors revealed correlations between the inhibitory activity and the chirality measure of the inhibitors, calculated by Eq. (26) for the entire structure or for the substructure that interacts with the enzyme (pharmacophore) [41], This was done for arylammonium inhibitors of trypsin, Di-dopamine receptor inhibitors, and organophosphate inhibitors of trypsin, acetylcholine esterase, and butyrylcholine esterase. Because the CCM values are equal for opposite enantiomers, the method had to be applied separately to the two families of enantiomers (R- and S-enantiomers). 

Hendrix C (2004) Safety, phamacokinetics and antiviral activity of AMD3100, a selective CXCR4 receptor inhibitor, in HlV-1 infection. J Acquir Immune Defic Syndr 37 1253-1262... 

Veratridine appears to act at a different part of pore channel from DDT or pyrethroids Act as agonists causing desensitization of receptor Inhibitor of GABA receptors... 

Abciximab is a first-line glycoprotein Ilb/IIIa receptor inhibitor for patients undergoing primary PCI3,15,18 who have not received fibrinolytics. It should not be administered for... 

In patients with NSTE ACS scheduled for early PCI, administration of either abciximab or eptifibatide (double bolus) is recommended. The use of tirofiban in these patients is not recommended, because it has been shown to be inferior to abciximab.2 Medical therapy with glycoprotein Ilb/IIIa receptor inhibitors in patients not undergoing PCI is reserved for higher-risk patients, such as those with positive troponin or ST-segment depression, and patients who have continued or recurrent ischemia despite other antithrombotic therapy.2... 

Doses and contraindications to glycoprotein Ilb/IIIa receptor blockers are described in Table 5-2. Major bleeding and rates of transfusion are increased with administration of a glycoprotein Ilb/IIIa receptor inhibitor in combination with aspirin and an anticoagulant,30 but there is no increased risk of intracranial hemorrhage in the absence of concomitant fibrinolytic treatment. The risk of thrombocytopenia with tirofiban and eptifibatide appears lower than that with abciximab. Bleeding risks appear similar between agents. 

Princen K, Schols D. HIV chemokine receptor inhibitors as novel anti-HIV drugs. Cytokine Growth Factor Rev 2005 16(6) 659-677. 

The gold-standard assay used for all chemokine receptor inhibitors that reach clinical-phase trials is the chemotaxis functional assay. This assay relies on the ability of chemokines to recruit cells expressing their respective receptor to areas of inflammation. In vitro, this assay was first described in detail by Taub et al. (16) for 24/48-well plates currently, this can be achieved by using 96-well plates. Cells are incubated in the upper chamber with an antagonist for a particular receptor (at different concentrations or with buffer) and challenged to migrate to the lower chamber, which has the relevant chemokine. After 2 to 4 hours of incubation at 37°C, the upper chamber inlet is removed and the cells in the lower chamber quantified by fluorescence with, for example, Calcein AM (Invitrogen, Carlsbad, CA). 

Anti androgens GnRH analogs Steroid synthesis inhibitors f>a reductase inhibitors Testosterone receptor inhibitors... 

H2 receptor inhibitors are more efficacious than sucralfate A... 

Docetaxel, pemetrexed, and an oral epidermal growth factor receptor inhibitor, erlotinib, are options for unresectable stage III or IV NSCLC patients with good performance status who progress during or after first-line therapy. 

Adenosine receptor inhibitors 2001SL1917 2003S1649 2004BML3307... 

The most potent activities (gastric antisecretory activity in the pylorus-ligated rat or anti-ulcer activity on stress-induced gastric lesion in rat) have been observed with compounds (30), (31) [106], (32) [107], (33) and (34) [108], which were shown neither to be histamine H2 receptor inhibitors nor to act as anticholinergic agents. Thus, the activity of compound (32), for example, has been reported to be superior to that of cimetidine [107],... 

Clopidogrel (Plavix, Hematology Platelet receptor inhibitor... 

Diovan HCT (Valsartan) Angiotensin II receptor inhibitor combination 1.0 0.8 1.0... 

Mechanism of Action A glycoprotein Ilb/IIIa receptor inhibitor that rapidly inhibits platelet aggregation by preventing the binding of fibrinogen to GP Ilb/IIIa receptor sites on platelets. Therapeutic Effect Prevents closure of treated coronary arteries. Prevents acute cardiac ischemic complications. 

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