672118
Descrição
Mapa Mental por David Bone, atualizado more than 1 year ago
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Criado por David Bone
mais de 10 anos atrás
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Muscarinic Receptors:Organ Bath
- Cholinergic muscarinic receptors
- Prejunctionally
- Postjunctionally
- Prejunctionally
- ACH muscurinic Receptors
- Plasma membrane receptors
- Mediate signal transduction coupling
- Heterotrimeric guanine nuecleotide binding protiens (G-proteins)
- Heterotrimeric guanine nuecleotide binding protiens (G-proteins)
- Plasma membrane receptors
- Five Subtypes
- M4
- M3
- Mediates all contactile responses in vitro.
- Act via a variety of secondary messagers
- Cause direct smooth muscle contraction
- Cause direct smooth muscle contraction
- Activates phospolipase C (PLC)
- Via Gq protiens
- Via Gq protiens
- Mediates all contactile responses in vitro.
- M2
- 75% Population share.
- Pig detrusor muscle
- Pig detrusor muscle
- 75% Population share.
- M5
- M1
- M4
- Similar 3 dimentional structures
- Single protein seven transmembrane domains
- Linked by 3 intracellular and three extra cellular loops
- Linked by 3 intracellular and three extra cellular loops
- Single protein seven transmembrane domains
- Antagonist
- Drug that block/partilly block a response
- Competative anatagonist binds reversibily to the same receptor as the agonist
- Competative anatagonist binds reversibily to the same receptor as the agonist
- Dose Response Curve
- Fixed concentration of antagonist will be shifted to the right
- Fixed concentration of antagonist will be shifted to the right
- Not completly selective
- Tool for discriminating muscarinic receptor subtypes in a given tissue
- Tool for discriminating muscarinic receptor subtypes in a given tissue
- Obtaining affinity constant (pK) or affinity estimates
(pA2)
- For Currently available antagonist to generate an affinity profile of these drugs at functional muscarinic
receptors
- To find pK2 and pA2 for specific receptor antagonist, concentration-response
curve
- to a muscarinic receptor agonist in absence and presence of specific
receptor
- Postjunctional contractile responses of muscle tissue at each concentration are measured to find
plateau
- between agaonist and magnitude of the effect produced is : concentration-response/dose response
relationship.
- between agaonist and magnitude of the effect produced is : concentration-response/dose response
relationship.
- Postjunctional contractile responses of muscle tissue at each concentration are measured to find
plateau
- pKb = log (CR1)- LOG [B]
- CR= Concentration ratio
- extent of shitf in the concentration -response curve in presence of an antagonist.
- extent of shitf in the concentration -response curve in presence of an antagonist.
- CR= Concentration ratio
- to a muscarinic receptor agonist in absence and presence of specific
receptor
- To find pK2 and pA2 for specific receptor antagonist, concentration-response
curve
- For Currently available antagonist to generate an affinity profile of these drugs at functional muscarinic
receptors
- Drug that block/partilly block a response
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