Receptor binding ability

Masteron has a receptor binding ability 3-5 times greater than that of testosterone. This means that the drug can hang out longer in androgen receptor-sites and is not easily displaced. The result should be increased AAS activity. 

Recent analyses of a Free-Wilsontype have included the in vitro inhibitory activity of a series of heterocyclic compounds against K. pneumonia (197). Other applications of the Free-Wilson approach have included studies on the antimycobacterial activity of 4-alkyl-thiobenzanilides, the antibacterial activity of fluoronapthyridines, and the benzodiazepine receptor-binding ability of some non-benzodi-apzepine compounds such as 3-X-imidazo-[l,2-6]pyridazines, 2-phenylimidazo[l,2-o ]pyri-dines,2-(alkoxycarbony)imidazo[2,l-p]benzo-thiazoles, and 2-arylquinolones(198-200). 

Branching the linker chain with a methyl group adjacent to the quinazolinone ring (68) resulted in a 350-fold decrease in affinity. However, chain branching with a methyl group in the alternate position on the ethylene chain produced compound (69), whose receptor affinity was of the same order of magnitude as the extremely potent lead compound (66). The exponential difference in receptor-binding ability exhibited by the two isomeric branched-chain linker compounds (68) and... 

Fluoroalkenes have been recognized as one of the possible nonhydrolyzable mimetics of amides on the basis of the similarity of charge distribution of the amide bond with the fluoroalkene moiety (Figure 6.2) [31] and their dipole moments (3.7 and 0.97 D for N-methylacetamide and ( )-2-fluoro-2-butene, respectively) [32]. A comparison of the receptor-binding ability of neuropeptide substance P (SP) with some related isosteres with fluoroalkenyl moiety is shown in Table 6.5, which demonstrates the effectiveness of replacement of the amide bond with fluoroalkenyl moiety [33]. 

The highest specific activity is obtained when 1 mCi of Na I is used. However, as far as receptor-binding ability is concerned, 0.5 mCi appears to be the optimum amount. Specific activity can also be controlled by changing the number of beads. 

More subtle modes of action are also possible since the response to hormone receptor binding is complex and could be affected by chemical interference with receptor-related proteins, DNA methylation or histone acetylation. Dioxin (TCDD), for example, reduces the ability of the oestrogen-receptor complex to bind to the oestrogen response element of DNA, reducing gene transcription. ... 

The ability of PO to interact with the acetyl residues of chitin allows us to compare them with monovalent lectins (i.e. extensins) which when binding with hemicellulose are only affected in a medium with a high ionic strength (Brownleader et al., 2006). As a rule, POs are bound with the plant cell wall and act as its modifiers. Some POs can form complexes with an extensin of cell walls (Brownleader et al., 2006). Consequently, chitin-specific sites that are capable of interacting with polysaccharides exist in the molecules of PO, and these sites can resemble the membrane receptor binding sites or else be similar to the domains of heparinbinding proteins (Kim et al., 2001). 

Antiemetics can be administered either intravenously or orally in this situation, depending on patient characteristics such as ability to take oral medications, dosage form availability, and cost considerations.5,10 The intravenous and oral routes are equally effective. When used at equipotent doses, the 5-HT3 antagonists have similar efficacy in preventing acute CINV, despite pharmacokinetic and receptor binding affinity differences.5,10,36... 

Emedastine H,-receptor antagonist inhibits eosinophil chemotaxis Superior Hrreceptor binding ability... 

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