WOOL AS AN INDICATOR OF NEUROPHARMACOLOGICAL ACTIVITY 77 



We mentioned earlier that different levels of affinity for (wool) protein 

 might correspond to apparently different biological activities. Therefore, we 

 studied the affinity for wool of a series of compounds: antihistaminics, 

 cholinesterase inhibitors, adrenergic blocking agents and quaternary ammon- 

 ium compounds with sympathetic ganglionic blocking activity. Without going 

 into too much detail, it can be stated that there is a gradually increasing 

 affinity for wool of all these compounds displayed in the above-mentioned order. 

 The lowest values are shown by Antistin, an antihistaminic of weak potency, 

 and Panparnit, an agent used to relieve symptoms of Parkinson's disease. Then 

 there is a slight increase when arriving at Pyribenzamine, as well as Prostigmine 

 and Janus green (both cholinesterase inhibitors). 



Benadryl (3.5 mMoles X 10- 2 /gm. wool) and Dibenamine show again an in- 

 crease in their affinity for wool, followed by Priscol (2-benzylimidazolin) as well 

 as by Regitin, 2-(N-p-tolyl-N-m-oxyphenyl-aminomethyl)-imidazolin, both 

 adrenergic blocking agents. The latter is the more potent one and also has a 

 higher affinity for wool than Priscol; the values are 1.7 and 4.3 mMoles X 10 -2 / 

 gm. wool respectively. Chlorpromazin (Largactil), Diparcol and Parsitan show 

 affinity values around 5.3 mMoles X 10 _2 /gm. wool and the two quaternaries, 

 Desogen and Bradosol, phenoxy-ethyl-dimethyl-dodecyl-ammonium bromide, 

 have the highest values recorded, namely 7 mMoles X 10 -2 /gm. wool. 



CH 3 



H,C\(CH,)n 



... s^. 



\ N— CH a 



Br ! CH 2 i 



I I i 

 jCH 2 J 



i I i 



Bradosol 



Thus wool is not only a model for a single enzyme but may also be regarded 

 as a model in a wider sense for all enzymes. 



The different levels of affinity for wool of certain compounds might imply 

 that many compounds with high affinity display biological properties generally 

 including also those associated with compounds of low affinity for wool. The 

 implication may be drawn that there is a hierarchy in terms of biological activity 

 which is associated with the degree of affinity for wool. In general, those com- 

 pounds of a homologous series which show high affinity have also a wider range 



