Skip to main content

Possible Long-Term Health Effects of Short-Term Exposure to Chemical Agents Volume 1 (1982) / Chapter Skim
Currently Skimming:

Appendix L: Structure-Activity Relations of the Centrally Active Anticholinergic Agents-- by Leo G. Abood, Ph.D.
Pages 275-284

The Chapter Skim interface presents what we've algorithmically identified as the most significant single chunk of text within every page in the chapter.
Select key terms on the right to highlight them within pages of the chapter.


From page 275...
... , and they do peneit generalizations concerning the relative ability of the anticholinergics to pratuce behavioral disturbances in animals fit may reflect psychotogenlc potency in man. Structural variations in the heterocyclic amino alcohol result in marked changes in potency; the most potent anricholinergic is 3-quinuclidinyl benzi}ate, with its rigi d conf ormation ~ Figure L-1)
Read the entire page →
From page 276...
... An alkynyl group in R: or Rat decreases duration, whereas increasing chain length or branching of the alkynyl group correspondingly increases duration. STEREOSPECIFICITY The anticholinergic glycolate esters of heterocyclic amino alcohols, including scopolamine and relates natural alkaloids, exist as optical isomers, resulting from the asymmetric C of both the amino alcohol and acid moiety.
Read the entire page →
From page 277...
... COMPETITION BE PREEN BEHAV IORAL POTENCY AND RECEPTOR AFFINITY To determine whe the r the centrally active anticholinergica bind to a physiologic receptor, an attempt was made to correlate inhibition binding constants of the various anticholinergic agents with their psychopharmacologic potency (20~. Such a correlation between behavioral and binding data has been attempted with a series of 14 glycolate esters (Figure 2~.
Read the entire page →
From page 278...
... The reasons for the difference may be that cautate nucleus contains a greater concentration of cholinergic receptors ant that a purifier synaptic membrane preparation was used in the later atuty. The relative bintlug affinities of the two isomers however, still had lesa than the 200:1 potency ratio fount in the cat behavioral teat (22)
Read the entire page →
From page 279...
... : 1963: Effect of anticholinergic psychotomimetic agento on motor activity and body temperature.
Read the entire page →
From page 280...
... 1974 In vivo itentification of muscarinic cholinergic receptor binding in rat brain. Brain Res.
Read the entire page →
From page 281...
... effects. The latter involve confualon, hallucinatlona, aemory loca, and delirtum.
Read the entire page →
From page 282...
... Psychotomimetic potency decreases from ~ to X
Read the entire page →
From page 283...
... quInuclidinyl benzilate bindiDg to breln~embrane preparationa BDI - compoalte lcdex of behavlore1 neasurasents in Bvarlou1 anl~la as a olesaure of paychotroplc potency D t d .1 ·_ 1 y ~' '1~ l ~' — 1 ~ 111 fil ~ .
Read the entire page →

Key Terms

  • caudate nucleus
  • heterocyclic amino
  • anticholinergic psychotomimetic
  • optical isomers
  • cholinergic receptor

  • cholinergic receptors
  • behavioral disturbances
  • anticholinergic agents
  • glycolate esters
  • chemical structure

  • quinuclidinyl benzilate
  • benzilate binding
  • behavioral measurements
  • peripheral antimuacarinic
  • anticholinergic action

  • central nervous
  • centrally active
  • disturbance index
  • peripheral anticholinergic
  • behavioral potencies

  • central action
  • anticholinergic potency
  • various anticholinergic
  • acid moiety
  • receptor binding

  • monkey brain
  • amino alcohol
  • psychopharmacologic potency
  • antimuacarinic potency
  • cautate nucleus


    • This material may be derived from roughly machine-read images, and so is provided only to facilitate research.
    More information on Chapter Skim is available.