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| PGI2 and TxA2 |
PGI2 and TXA2 work as antagonists |
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mcs5109 Tue, 23 Sep 2008 14:36:46 GMT |
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| thromboxanes |
promote clotting |
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mcs5109 Tue, 23 Sep 2008 04:38:18 GMT |
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| prostaglandins |
most of which are pro-inflammatory |
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mcs5109 Tue, 23 Sep 2008 04:38:18 GMT |
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| calmodulin |
-4 binding areas for Ca+2
changes shapes of proteins
-activates/inhibits
-calmodulin-dependent kinases |
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mcs5109 Tue, 23 Sep 2008 04:30:13 GMT |
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| Ca as 2nd messenger |
-increased by:
-G protein activating ion gates
-IP3 releasing Ca+2 from ER
-active transport of Ca+2 out of cell blocked
-opening voltage-gated channels |
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mcs5109 Tue, 23 Sep 2008 04:30:13 GMT |
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| IP3, DAG |
-effector= phospholipase C
-causes IPI2 to be converted to IP3, DAG
-DAG activates protein kinases
-IP3 makes ER leaky to Ca+2, increase cytosol Ca+2
-mediates cell responses
-Ca+2= 3rd messenger? |
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mcs5109 Tue, 23 Sep 2008 04:30:13 GMT |
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| cAMP |
-elicits glycogenlysis in liver
-2nd messenger
-adenylyl cyclase is effector protein
-cAMP activates cAMP-dependednt protein kinases
-phosphorylates proteins (inhibits or activates)
to stop:
-phosphodiesterasedegrades cAMP
if blocked, cAMP runs wild
-cGMP analog |
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mcs5109 Tue, 23 Sep 2008 04:18:31 GMT |
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| 2nd messenger system |
-activate G proteins in PM
-can be cAMP, IP3, DAG, Ca+2
-1st messenger binds
-receptor activates G protein
-activates effector proteins in PM
-effector protein generates 2nd messenger
-G protein "couples" receptor and effector |
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mcs5109 Tue, 23 Sep 2008 04:18:31 GMT |
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| receptor couples w/ protein kinase |
-messenger binds to receptor
-receptor activates tyrosin kinase
-P's protein (ATP)
-mediates cell response (esp. growth and devel)
-insulin |
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mcs5109 Tue, 23 Sep 2008 04:18:31 GMT |
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| receptor w/ ion channel |
-messenger binds to receptor
-receptor activates channel
-ex: neurotransmitter action postsynaptically |
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mcs5109 Tue, 23 Sep 2008 04:18:31 GMT |
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| lipid insoluble messages |
-use PM receptors
-receptor w/ ion channel
-receptor w/ protein kinase |
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mcs5109 Tue, 23 Sep 2008 04:09:47 GMT |
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| lipid soluble message |
-steroid hormones pass right through PM and nucleus
-intracellular receptors
-regulate gene transcription |
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mcs5109 Tue, 23 Sep 2008 04:09:47 GMT |
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| anti-asthmatic/allergy |
-singulair
-block leukotriene pathways |
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mcs5109 Tue, 23 Sep 2008 04:09:47 GMT |
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| acetaminophens |
-tylenol
-good analgesix and antipyretic
-poorly understood
-nont really anti-inflammatory
-Cox3? |
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mcs5109 Tue, 23 Sep 2008 04:09:47 GMT |
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| indomethacin |
-more powerful, esp. for arthritus |
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mcs5109 Tue, 23 Sep 2008 03:12:52 GMT |
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| naproxens |
-aleve
-similar to ibuprofens |
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mcs5109 Tue, 23 Sep 2008 03:12:52 GMT |
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| ibuprofens |
-motrin, advil
-inhibit inflammatory rxns in pathway, esp. PGI2 |
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mcs5109 Tue, 23 Sep 2008 03:12:52 GMT |
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| aspirins |
-esp. anti-clotting pathways, can lead to ulcers |
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mcs5109 Tue, 23 Sep 2008 03:12:52 GMT |
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| aspirins/NSAIDs |
-inhibit cyclooxygenase, which converts AA to endoperoxides
-several classes: aspirins, IBprofen, napoxens, indomethacin
-all inhibit COX1 or 2 to some degree |
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mcs5109 Tue, 23 Sep 2008 03:12:52 GMT |
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| COX |
-enzyme that is responsible for formation of endoperoxides
-inhibition of COX can provide relief from the symptoms of inflammation and pain
-method of action of non-steroidal anti-inflammatory drugs (aspirin and ibuprofen) |
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mcs5109 Tue, 23 Sep 2008 02:53:24 GMT |
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| SRA-A |
-slow reacting substance anaphylaxis
-mixture of the leukotrienes
-secreted by mast cells during allergic reaction
-stimulates T cells, interleuken, interferon production
-bronchoconstriction
-increase vascular permeability |
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mcs5109 Tue, 23 Sep 2008 02:53:24 GMT |
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| leukotrienes |
-produced by lipoxygenase on AA
-secreted by certain wbc's |
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mcs5109 Tue, 23 Sep 2008 02:53:24 GMT |
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| TxA2 |
-is a thromboxane
-generated from prostaglandin H2 by thromboxane-A synthase
-major component of blood clots
-very short half life
-vasoconstrictor, bronchoconstrictor
-increases blood aggregation |
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mcs5109 Tue, 23 Sep 2008 02:53:24 GMT |
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| PGI2 |
-prostocyclin
-vasodilator, bronchodilator
-decreases platelet aggregation |
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mcs5109 Tue, 23 Sep 2008 02:53:24 GMT |
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| COX 2 |
-pain and inflammatory pathway
-COX2 inhibitors |
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mcs5109 Tue, 23 Sep 2008 02:53:24 GMT |
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| COX1 |
-platelet aggregation, protects stomach |
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mcs5109 Tue, 23 Sep 2008 02:24:53 GMT |
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| NSAID |
non steroidal anti infammatory drugs |
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mcs5109 Tue, 23 Sep 2008 02:24:53 GMT |
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| cyclooxygenase |
-converts AA to entoperoxides
-inhibited by aspirin, NSAIDS
-COX 1 and 2 |
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mcs5109 Tue, 23 Sep 2008 02:24:53 GMT |
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| phospholipase A |
-converts phospholipid to Arachindonic acid
-inhibited by glucorticoids (steroids) |
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mcs5109 Tue, 23 Sep 2008 02:24:53 GMT |
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| 3 classes of eicosinoids |
-protoglandins
-thromboxanes
-leukotrienes |
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mcs5109 Tue, 23 Sep 2008 02:21:52 GMT |
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| eicosanoids |
-lipid-derived paracrine signals
-derived from arachidonic acid
-present in PM phosopholipids |
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mcs5109 Tue, 23 Sep 2008 02:21:52 GMT |
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| autocrine agents |
-action on same cell that secreted them
-responses mediated by receptors in membrane, cytoplasm, nucleus |
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mcs5109 Tue, 23 Sep 2008 02:21:52 GMT |
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| paracrine agents |
-rapidly degraded
-only affect local tissue
-does not enter blood stream |
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mcs5109 Tue, 23 Sep 2008 02:21:52 GMT |
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