Pharmacology Structure-Activity Relationships

The effect of atropine upon chromosomal abnormalities24 has been studied. A significant dose-dependent reduction of heart rate and blood pressure has been observed.25 A possible effectiveness of atropine on Prinzmetal s variant form of 

Feeney, E. A. Piper, and R. Foster, Adv. Pharmacol. Ther. Proc. Congr. Pharmacol., 1978, 3, 281. 

Quaternary 7V-(xanthinylalkyl)nortropines have been claimed32 to have spasmolytic (particularly bronchospasmolytic) effects without the side-effects of atropine. 

A large number of pharmacological studies have been undertaken with cocaine, in animals and in humans. 

Behavioural antecedents of a cocaine-induced stereotype33 and rate dependency of behavioral effects34 have been studied. Studies of the physiological effects on Man of intravenous administration of cocaine35 and of the discriminative response of humans to cocaine36 have given new results. 

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C. Hansch, Quantitative approaches to pharmacological structure-activity relationships. In Structure-Activity Relationships (C.J. Cavallito, Ed.), Vol. 1. Pergamon, Oxford, 1973, pp. 75-165. 

Jacobson KA, van Galen PJM, Williams M. Adenosine receptors pharmacology, structure-activity relationships, and therapeutic potential. J Med Chem 1992 35 407 122. 

Nakazato, A., Sakagami, K., Yasuhara, A., et al. (2004) Synthesis, in vitro pharmacology, structure-activity relationships and pharmacokinetics of 3-alkoxy-2-amino-6-fluorobicyclo[3.1.0]... 

Hackett, A.M.In Plant Flavonoids in Biology and Medicine. Biochemical, pharmacological, structure-activity relationships, Cody, V., Middleton-E, J., Harbome, J.B., Eds. Alan R. Liss Inc. New York, 1986 pp 177-199. 

Turning to the bio-, eco-, or pharmacological structure-activity relationships, the success of the QSAR methods was further certified when it was accepted as the official algorithm by the EU for validating new... 

Z, ] McClarin, T Klein and R Langridge 1985. A Quantitative Structure-Activity Relationship and ecular Graphics Study of Carbonic Anhydrase Inhibitors. Molecular Pharmacology 27 493-498. 

The structure activity relationships ( SAR) of newly synthesized analogues of nucleosides, xanthine heterocycles, and nonxanthine heterocycles have been explored at the ARs. Potent and selective AR antagonists have been prepared for all four subtypes [3, 4], and selective agonists are known for three subtypes [1]. Thus, numerous pharmacological tools are available for in vitro and in vivo use (Table 2). Potent and selective A2b AR agonists are yet to be repotted, although several research groups have identified lead compounds. 

Schon U, Antel J, Bruckner, Messinger J. Synthesis, pharmacological characterization, and quantitative structure-activity relationship analyses of 3,7,9,9-tetraalkylbispidines derivatives with specific bradycardic activity. J Med Chem 1998 41 318-31. 

Abstract Protoberberine alkaloids and related compounds represent an important class of molecules and have attracted recent attention for their various pharmacological activities. This chapter deals with the physicochemical properties of several isoquinoline alkaloids (berberine, palmatine and coralyne) and many of their derivatives under various environmental conditions. The interaction of these compounds with polymorphic DNA structures (B-form, Z-form, H -form, protonated form, triple helical form and quadruplex form) and polymorphic RNA structures (A-form, protonated form, triple helical form and quadruplex form) reported by several research groups, employing various analytical techniques such as spectrophotometry, spectrofluorimetry, circular dichro-ism, NMR spectroscopy, viscometry as well as molecular modelling and thermodynamic analysis to elucidate their mode and mechanism of action for structure-activity relationships, are also presented. 

Okada, Y. and Kuroda, Y., Inhibitory action of adenosine and adenosine analogs on neurotransmission in the olfactory cortex slice of guinea pig Structure-activity relationships, European Journal of Pharmacology, 61, 137, 1980. 

Cerletti, A., Taeschler, M., and Weidmann, H. (1968) Pharmacologic studies on the structure-activity relationship of hydroxyindole alkylamines. Adv. Pharmacol., 6B.233-246. 

Our goal in this discussion is to present the types of structural variations that have been studied in the various classes of hallucinogens and to explain how these changes affect biologic activity. Where possible, reasonable explanations for these differences are offered. Since we are just beginning to scratch the surface in our search for useful structure-activity relationships, the reader will soon note that most of the correlations are empirical, with no readily apparent biochemical or pharmacologic rationale. 

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