神经系统药理2胆碱能神经系统.ppt

* Btx, taken up into vesicles, cleaves the SNARE proteins, preventing assembly of the fusion complex and thus blocking the release of ACh. * * If norepinephrine or epinephrine is the transmitter, the fiber is called adrenergic (adrenaline is the other name for epinephrine). In the sympathetic system, norepinephrine mediates the transmission of nerve impulse from postganglionic nerve to effector organs. * Norepinephrine (NE) or noradrenaline (NA) Adrenergic nerves most of post-ganglionic fibers of sympathetic nerves * * sympathomimetic amine that contain the 3,4-dihydroxybenzene group, this group is named catechol, such as norepinephrine, epinephrine,isoproterenol and dopamine . * 儿茶酚胺类，易被COMT讲解 1.Increaseing the size of alkyl substitutions on the amino group tends to increase b-receptor activity. 2.Without any substitution (e.g. –OH group) on the benzene ring may reduce the potency of the drug, may increase the bioavailability after oral administration and prolongs the duration of action. Furthermore, absence of –OH group tends to increase the distribution to the CNS. 3.Substitution at the alpha carbon block oxidation by monoamine oxidase (MAO). 4.Substitution on the beta Carbon the drug can activate the receptor directly. Furthermore, the hydroxyl group may be important for storage of sympathomimetic amines in neural vesicles. * The dopamine receptors are distinct from a and b receptors and are particularly important in the brain. And they also distribute in the vascular beds of kidney and ileus. * adrenomimetic; sympathomimetic; adrenergic agonist The mode of action: DIRECT; INDIRECT; MIXED DIRECT: direct interaction with adrenergic receptors. INDIRECT: causes response indirectly by provoking release of intraneuronal NE into synaptic cleft or interfering with NE reuptake. MIXED: combination of DIRECT and INDIRECT mechanisms. * * fully adequate replacement of intravascular fluid Furosemide is a drug used for * In isolated cardiac tissue NE stim