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41.
The pharmacological variety of conotoxins, diverse peptides found in the venoms of marine cone snails, is well recognized. Venoms from each of the estimated 500 species of cone snails contain 50 to 200 distinct biologically active peptides. Most conotoxins characterized to date target receptors and ion channels of excitable tissues, such as ligand-gated nicotinic acetylcholine, N-methyl-D-aspartate, and type 3 serotonin receptors, as well as voltage-gated calcium, sodium, and potassium channels, and G-protein-coupled receptors including α-adrenergic, neurotensin, and vasopressin receptors, and the norepinephrine transporter. Several conotoxins have shown promise in preclinical models of pain, convulsive disorders, stroke, neuromuscular block, and cardioprotection. The pharmacological selectivity of the conotoxins, coupled with the safety and efficacy demonstrated in preclinical models, has led to their investigation as human therapeutic agents. In the following review, we will survey the pharmacology and therapeutic rationale of those conotoxins with potential clinical application, and discuss the unique challenges that each will face in the course of their transition from venom component to human therapeutic. 相似文献
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Blood cell indices and parameters of haemostasis were studied in the common marmoset. The majority of the results were similar to those found in man. Differences from man were that the prothrombin time was shorter in the marmoset, higher concentrations of aggregating stimuli were required to cause platelet aggregation, and marmoset platelets did not aggregate under the influence of adrenalin. There was sexual dimorphism evident in the data for fibrinogen concentration and for platelet count, both of which were higher in females than in males. Marmoset platelets were very similar in ultrastructure to those of man. 相似文献
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