What is the target for the following compound? O Muscarinic receptor O Acetylcholinesterase enzyme O Choline acetyltransferase O Nicotinic receptor O None of the answers OEt nefa MezN OEt
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- What is the target for the following compound? O Muscarinic receptor O Acetylcholinesterase enzyme O Choline acetyltransferase O Nicotinic receptor O None of the answers MezN OEt fo QEtShown are different derivatives of acetylcholine. A H2N H2N D 1. Which one is expected to lose its ability to bind to the receptor but could elicit CNS side effects? Explain. 2. Which is/are expected to resist metabolism by choline esterase? 3. Which one is not expected to bind and yet prone to metabolism? Explain ZIIn cholinergic neurotransmission, inhibition of the choline transporter will affect the normal synthesis and release acetylcholineTRUE OR FALSE
- Which of the following structures has activity like acetylcholine? Et H3C Me H3C NMeg H.C NMesDepending on the size and complexity of the molecule, small chemical alterations can impart significant activity differences, especially if a certain part of the molecule is critical for binding. Considering this, select structure(s) below that are expected to have high cholinergic agonist activity based on what we leamed about acetylcholine's SAR.The receptors have been found on ganglia of the peripheral nervous system and on the autonomic effector organs are muscarinic receptors O False O True *
- The neurotransmitter acetylcholine is released from presynaptic neurons in response to a nerve impulse and diffuses across the È synaptic cleft, or neuromuscular junction, to a receptor on another neuron or a muscle cell. The nicotinic acetylcholine receptor is a pentamer containing four types of subunits, azßys. Place the events in the correct order, from the release of acetylcholine from a neuron to receptor resensitization: -excited presynaptic neuron releases acetylcholine -acetylcholine diffuses across synaptic cleft or neuromuscular junction -acetylcholine is released from the binding sites -two acetylcholine bind to a receptor; the gate opens -small cations pass through the open pore of the receptor -the plasma membrane of the target cell is depolarized -two acetylcholine are tightly bound to a receptor; the gate is closed -one acetylcholine binds to a receptor; the gate is closed.The a-adrenoceptors are into two subdivided subgroups, a1 and a2, based on their response to the synthetic agonist O True O False *The following compounds exhibit little to no adrenergic receptor function. Consider what components of adrenaline and noradrenaline are necessary for their action as agonists in light of this knowledge. Explain your response. Assume that the pH of the body is 7.
- To maximize the activity of an α4β2 nicotinic Achtylchcholine Receptor (nAChR), how many agonist binding sitea should be occupied?Carbachol have longer durations of action than Ach, because they have both muscarinic and nicotinic activity. they are not hydrolyzed by AChE. They bind to muscarinic receptors. They show little specificity in their actions OWhich of the following would be a side effect of a muscarinic agonist that is used to treat dry mouth? dilate airways decrease heart rate excess saliva production inhibit digestive system excess lipolysis ( please say which option is correct not just explanation)