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46 Cards in this Set
- Front
- Back
Striated muscle nicotinic receptor |
(a1)2 B1 d E |
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Fetal muscle nicotinic receptor |
(a1)2 B1 d y |
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Autonomic ganglia nicotinic receptors |
(a3)2 (B4)3 |
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Brain nicotinic receptors |
(a4)2 (B4)3; (a7)5; (a3)2 (B4)3 (a7)5 is highly Ca2+ permeable- others are permeable to Na/K |
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M1 and M3 receptor |
Gq/11- activates PLCB- PIP2 hydrolysis- IP3 and DAG and cause SM contractions in viscera through Ca2+-CaM dependent activation of MLCK which prosphorylates MLC and htis initiates contraction |
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Endothelial M3 |
Increase in Ca2+-calmodulin, activates eNOS which converts arginine to No and citrulline. NO activates cGMP- relaxation of smooth muscle |
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M1 in neurones |
activation inhibits a K+ conductance known as the M current. This produces a slow EPSP. The M current is mediated by Ku7 family and they are activated by PIP2 binding to their C terminus. M1 activation induced depletion of PIP2 causes inhibition |
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M2 (and M4) |
Gi- found in the heart a subunit inhibits AC- decrease cAMP and PKA, decrease phosphorylation of VGCa2+C, decrease excitability of heart m By subunit- opens GIRK of heart and this decreases HR Expressed presynaptically and decreases CaV activity (decrease Cav phosphorylation) at nerve endings and decrease trasmitter release |
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a1 |
Gq/11 coupled- PLC activation- increase in IP3, DAG and Ca2+ Dilation of pupils; vasoconstriction to vessels to viscera, brain and skin; salivary secretion; decreased GI motility and tone (relax SM), localized sweat secretion- hands; piloerection; contraction of trigone and sphincter of bladder; ejaculation of sperm; increased gluconeogenesis and glycogenolysis |
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a2 |
Gi Inhibition of neurotransmitter release, platelet aggregation, vasoconstriction, inhibition of insulin release from B cells |
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B1 |
Gs coupled- in the heart Increased force of myocardial contraction, increased heart rate B1 in the kidney stimulates renin secretion |
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B2 |
Gs coupled Relaxation of tracheal and bronchial SM; relaxation of SM of bvs supplying the heart and SKM; relaxation of uterine SM (non pregnant); hepatic glycogenolysis |
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B3 |
G2 coupled Lipolysis, thermogenesis |
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P2X1-7 |
Stimulated by ATP, signal and homo/heterodimers, ligand gated ion channels |
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P2X 2,4,6 |
Main subtypes in postsynaptic neurones- critical for initation of AP P2X2/3 receptors on subepithelial sensory nn are responsible for visceral pain |
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P2X1 |
In smooth muscle, stimulation causes contraction of the vas deferens to propel sperm into the ejaculate. Mice lacking these receptors are infertile |
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P2Y |
GPCRs, some are activated by ATP but can be activated by ADP, UTP etc |
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Adensine receptors- A1, A2a and A3 (P1) |
GPCRs A1- decreases rate and force of contraction of heart- adenosine is given IV to stop supraventricular tachycardia A1 and A2- inhibitory effects on many CNS neurons |
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AT2 |
Angiotensin II receptor, activation causes vasodilation by generation of NO- increase cGMP Binding of AII in some cells can inhibit prolieration, mediate differentiation in neural tissue and can induce apoptosis |
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AT4 |
Angiotensin receptor, may be activated by AIV, located not just in brain, activation has been proposed as a strategy for memory enhancement esp Alzheimer's disease |
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H1 |
Gq/11, histamine receptor imp in inflammation. Causes SM contraction in the ileum, bronchioles and uterus, blood vessel dilation- mediated by NO, itching via activation of pruritoceptors, triple response |
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H2 |
G2- histamine receptor imp in gastric acid secretion |
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H3 |
Gi- histamine receptor that is an imp inhibitory autoreceptor in the CNS |
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H4 |
Gi- decrease chemotaxis and cytokine release |
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B1 and B2 |
Gq coupled, B1 are upregulated in inflammation and the primary agonist is des-Arg bradykinin. B2 are constitutively expressed and are activated by bradykinin and kallidin Activation on endothelium mediates vasodilation via PGI2 and NO Activation also activates nociceptors |
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NK1 receptor |
Neurokinin receptor- Gq coupled activated by substance P. Mast cell degranulation, SM contraction, vasodilation and neuronal sensitisation |
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NK2 |
Neurokinin receptor- Gq coupled activated by neurokinin A, Mast cell degranulation, SM contraction, vasodilation and neuronal sensitisation |
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FMR2 |
Formyl peptide receptor 2- Gi coupled. Activated by Annexin-A1 and LXA4, anti-inflammatory- decrease neutrophil chemotaxis and degranulation of mast cells |
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BLT1 and BLT2 |
GPCR receptor for LTB4- chemoattraction, activate neutrophils |
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CysLt1 |
Activated by LTD4, bronchoconstricion, increase vascular permeability and mucus secretion |
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CysLT2 |
activated by LTC4, bronchoconstricion,increase vascular permeability and mucus secretion |
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DP1 |
Gs coupled- when PGD2 binds- vasodilation, inhibit platelet aggregation, relaxes GI/uterine muscle |
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EP2 |
Gs coupled- when PGE2 binds= bronchodilation, vasodilation and relaxation of GI muscle |
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EP4 |
Gs coupled, activated by PGE2- cause sensitisation of nociceptors |
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IP receptor |
Gs coupled, activated by PGI2- vasodilation and inhibition of platelet aggregation |
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EP1 |
Gq coupled, activated by PGE2 to cause bronchial/GI muscle contraction |
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FP |
Gq coupled, activated by PGF2a- uterine contraction and bronchoconstriction (cats and dogs) |
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TP |
Gq coupled, activated by PGD2 and TXA2- bronchoconstriction, vasoconstriction and platelet aggregation |
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DP2 |
Gi coupled |
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EP3 |
Gi coupled- GI muscle contraction, fever, inhibition of GA secretion and increase gastric mucous secretion |
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5HT1A,B,D,F |
Gi GPCRs |
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5HT2A-C |
Gq coupled |
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5HT3 |
ionotropic receptor |
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A1 |
Gi coupled, decrease rate and force of contraction in heart, bronchoconstriction, presynaptic inhibition, decrease glutamate release, induces sleep, endogenous antiepileptic |
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A2 |
2 types- A and B, both G2 coupled, vasodilation (including in the coronary aa) decrease activation neutrophils |
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A3 |
Gq/11 coupled, decrease eosinophil activation, esp in lungs |