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991.
A study of heterogeneity among muscarinic receptors was carried out with new rigid molecules, comprising structures in the fused quinuclidine-valerolactone, quinuclidine-cyclohexenone, quinuclidine-cyclohexanone and quinuclidine-cyclohexane derivatives. These are structurally related to the potent muscarinic agent, 3-acetoxyquinuclidine but substantially different from in it conformation. All proved to antagonize acetylcholine-like activity, but to a different extent in different systems. The equipotent molar ratio with respect to atropine (as 1) was: isolated guinea pig ileum, 10,000-1,000; salivary gland (mouse), 1,000-100; superior cervical ganglion (cat), 100-10; CNS (mouse), approximately 10. It is suggested that the rigid structure induces a three-point constrained fit in the receptor (onium group, hydrophobic moiety and carbonyl group), but that not all muscarinic receptors are capable of responding equally. In this case, receptor specificity of the drug is a direct consequence of its graded departure from the preferred conformation of acetycholine and, therefore, is necessarily associated with partial loss of potency.  相似文献   
992.
The author studied 28 men convicted and confined for use of explosives in assaults on superior officers during the Viet Nam war. There were several predominant characteristics in this group, including deprivation and/or brutality in family backgrounds, poor self-image, lack of critical self-observation, the use of externalization, and feelings of insecurity or vulnerability. Drug use joined with these and several other factors related to the situation of these men in Viet Nam in a lethal combination that led to the perpetration of an indirect assault with an explosive device on a figure perceived as powerful and threatening.  相似文献   
993.
Report of a newborn with massive ascites who developed a severe coagulopathy due to multiple intrinsic and extrinsic clotting factor deficiencies. All deficient coagulation factors were present in measurable quantities in the infant's ascitic fluid. It is postulated that she sustained loss of coagulant proteins by transudation into her peritoneal cavity. A similarly acquired coagulopathy should be suspected in all patients with a known increase in extravascular fluid compartments.  相似文献   
994.
This paper describes a hybrid electric vehicle drive control system under microcomputer control where the propulsion power is shared between a gasoline engine and a dc motor. The control functions have been developed, analyzed, and implemented with highlevel language in a dual Intel 8086 microcomputer system. The drive system has been integrated and tested, and shows excellent results.  相似文献   
995.
Made behavioral comparisons between Long-Evans rats with complete removal of the neocortex of one hemisphere (hemidecorticate) or of the cortex anterior to bregma in both hemispheres (frontal cortex) in adulthood and rats with similar removals at 7 days of age. Neonatal ablation of the frontal cortex produced partial sparing of performance on the Morris water task and reduced the thickness of the remaining neocortex. Neonatal hemidecortication produced similar sparing of function on the water task but increased the thickness of the contralateral neocortex. Results are consistent with hemispherectomy studies done with children and imply that behavioral sparing following neonatal cortical lesions is independent of the gross morphogenesis of the remaining neocortex. (16 ref) (PsycINFO Database Record (c) 2010 APA, all rights reserved)  相似文献   
996.
Activation of phosphatidylcholine-specific phospholipase D (PLD) has been proposed to play roles in numerous cellular pathways including signal transduction and membrane vesicular trafficking. We previously reported the cloning of two mammalian genes, PLD1 and PLD2, that encode PLD activities. We additionally reported that PLD1 is activated in a synergistic manner by protein kinase c-alpha (PKC-alpha), ADP-ribosylation factor 1 (ARF1), and Rho family members. We describe here molecular analysis of PLD1 using a combination of domain deletion and mutagenesis. We show that the amino-terminal 325 amino acids are required for PKC-alpha activation of PLD1 but not for activation by ARF1 and RhoA. This region does not contain the sole PKC-alpha interaction site and additionally functions to inhibit basal PLD activity in vivo. Second, a region of sequence unique to PLD1 (as compared with other PLDs) known as the "loop" region had been proposed to serve as an effector regulatory region but is shown here only to mediate inhibition of PLD1. Finally, we show that modification of the amino terminus, but not of the carboxyl terminus, is compatible with PLD enzymatic function and propose a simple model for PLD activation.  相似文献   
997.
Floc simulation studies have been extended to include the more realistic cases of aggregates formed by spheres having a range of sizes or formed by non-spherical primary particles. The situation of anisometric particles was treated by using clusters of spheres to approximate the desired shape. Floc parameters were generated and are discussed in relation to the experimental findings with flocculated and close-packed systems.  相似文献   
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