p.11
Nuclear Receptors and Gene Regulation
What are the main physiological effects of glucocorticoids?
They regulate homeostasis in organs and cells, affecting immunity, metabolism, reproduction, and the nervous system.
p.21
Enzyme-Catalyzed Secondary Messengers
What are the six main classifications of enzymes?
1. Oxidoreductase 2. Transferase 3. Hydrolase 4. Lyase 5. Isomerase 6. Ligase.
p.17
Ion Channel Receptors and Neurotransmission
What type of receptor is the 5-HT3 receptor?
It is a cation channel receptor.
p.11
Nuclear Receptors and Gene Regulation
What is the function of mineralocorticoid receptors (MR)?
They activate renal sodium reabsorption and potassium secretion.
p.26
Ion Channel Receptors and Neurotransmission
What type of receptor is the Ka inate receptor?
A tetrameric excitatory receptor.
p.21
Enzyme-Catalyzed Secondary Messengers
What is the significance of the catalytic triad in serine proteases?
The catalytic triad consists of Ser195, His57, and Asp102, which are crucial for catalysis.
p.16
Ion Channel Receptors and Neurotransmission
Where is the nicotinic acetylcholine receptor primarily located?
At the neuromuscular junction (NMJ), adrenal medulla, and autonomic ganglia.
p.11
Nuclear Receptors and Gene Regulation
What is the role of GR-α and GR-β?
GR-α regulates physiological effects, while GR-β can act without a ligand and suppress gene expression.
p.13
Nuclear Receptors and Gene Regulation
Where is PPAR-α primarily found?
In brown adipose tissue, liver, heart, kidneys, and small intestine.
p.14
Nuclear Receptors and Gene Regulation
What are the two forms of Vitamin D mentioned?
Vitamin D2 (Ergocalciferol) and Vitamin D3 (Cholecalciferol).
p.13
Nuclear Receptors and Gene Regulation
What metabolic processes does PPAR-α influence?
Lipid metabolism, fatty acid oxidation, gluconeogenesis, and insulin sensitivity.
p.17
Ion Channel Receptors and Neurotransmission
What happens when the ligand binds to the 5-HT3 receptor?
It opens the ion channel, allowing Na+ and Ca2+ to flow in and K+ to flow out, leading to depolarization (EPSP).
p.10
Nuclear Receptors and Gene Regulation
AR拮抗劑的例子有哪些？
Flutamide 和 Bicalutamide。
p.11
Nuclear Receptors and Gene Regulation
What is the clinical use of spironolactone?
It is a potassium-sparing diuretic used to treat hypertension and heart failure.
p.16
Ion Channel Receptors and Neurotransmission
What type of receptor is the nicotinic acetylcholine receptor (nAChR)?
It is a ligand-gated ion channel receptor.
p.16
Ion Channel Receptors and Neurotransmission
What is the structure of the nicotinic acetylcholine receptor?
It consists of 5 subunits, typically 2 alpha and 3 beta/other subunits.
p.20
Ion Channel Receptors and Neurotransmission
What determines the direction of Ca²⁺ transport in Na/Ca²⁺ exchange proteins?
The intracellular to extracellular Na/Ca²⁺ ratio.
p.16
Ion Channel Receptors and Neurotransmission
What happens when acetylcholine (ACh) binds to nAChR?
It causes depolarization, leading to an excitatory postsynaptic potential (EPSP).
p.16
Ion Channel Receptors and Neurotransmission
What are the effects of succinylcholine?
It is a depolarizing neuromuscular blocker that causes muscle twitching followed by paralysis.
p.20
Ion Channel Receptors and Neurotransmission
What is the role of ATP-driven membrane pumps in calcium efflux?
They use ATP to pump Ca²⁺ out of the cell.
p.8
Nuclear Receptors and Gene Regulation
What is the significance of the ligand binding domain (LBD)?
It contains the main hormone binding site and allosteric binding sites for coactivators and corepressors.
p.20
Ion Channel Receptors and Neurotransmission
What regulates calcium storage and release in muscle cells?
The sarcoplasmic reticulum.
p.7
Nuclear Receptors and Gene Regulation
What is the location of nuclear receptors (NR)?
Inside the cell membrane.
p.1
Second Messenger Pathways
二次訊息路徑分為哪兩類？
1. ATP、GTP轉化為cAMP、cGMP；2. 水解細胞膜上的磷脂質生成DAG、IP3。
p.10
Nuclear Receptors and Gene Regulation
雄性激素受體如何傳遞訊息？
在細胞質中結合分子伴侶蛋白，然後進入細胞核結合ARE調節基因轉錄。
p.12
Nuclear Receptors and Gene Regulation
What hormone does the hypothalamus secrete that affects the thyroid receptor?
TRH (thyrotropin-releasing hormone).
p.14
Nuclear Receptors and Gene Regulation
What is the effect of the short isoform of Vitamin D?
It decreases bone density.
p.12
Nuclear Receptors and Gene Regulation
What is the role of TSH (thyroid-stimulating hormone)?
It promotes the synthesis and release of T3 and T4.
p.14
Nuclear Receptors and Gene Regulation
What is the role of Calcipotriol?
It inhibits skin cell proliferation and helps restore normal differentiation in conditions like psoriasis.
p.4
Ion Channel Receptors and Neurotransmission
What type of receptor is 5-HT3?
It is an ion channel receptor.
p.21
G Protein-Coupled Receptors (GPCRs)
What happens when guanylyl cyclase receptors are activated?
They convert GTP to cGMP, leading to muscle relaxation.
p.14
Nuclear Receptors and Gene Regulation
What type of receptor is the Vitamin D Receptor (VDR)?
A lipid-soluble receptor with a steroid-like structure.
p.8
Nuclear Receptors and Gene Regulation
What is the function of the N-terminal domain (NTD)?
It can interact with coactivators and corepressors to regulate receptor activation.
p.20
Ion Channel Receptors and Neurotransmission
What is the function of voltage-dependent channels (PDC)?
They open in response to membrane depolarization, allowing Ca²⁺ to flow into the cell.
p.14
Nuclear Receptors and Gene Regulation
How is Vitamin D3 synthesized in the body?
From 7-dehydrocholesterol in the skin through UV exposure.
p.25
Enzyme-Catalyzed Secondary Messengers
What is a transition-state analogue?
A compound that resembles the transition state of a substrate, which has a high affinity for enzymes and can inhibit them.
p.17
Ion Channel Receptors and Neurotransmission
What effect do 5-HT3 receptor antagonists have?
They can prevent nausea and vomiting, especially during chemotherapy and pregnancy.
p.3
G Protein-Coupled Receptors (GPCRs)
β2-腎上腺性受體的N端有什麼修飾？
有碳水化合物修飾 (高mannose-寡糖連接)。
p.1
G Protein-Coupled Receptors (GPCRs)
G_s的作用是什麼？
G_s激活腺苷酸酰化酶（AC），使cAMP上升，進而促進PKA活化，導致Ca²⁺流入。
p.4
G Protein-Coupled Receptors (GPCRs)
What are the subtypes of serotonin receptors?
7 subtypes: 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HT5, 5-HT6, and 5-HT7.
p.1
G Protein-Coupled Receptors (GPCRs)
G_i的功能是什麼？
G_i抑制腺苷酸酰化酶（AC），使cAMP下降，導致K⁺流出，細胞過極化，活性下降。
p.6
Opioid Receptors and Pain Regulation
Aripiprazole的作用機制是什麼？
作為β-arrestin偏向性D2受體配體，促進訊息傳遞。
p.12
Nuclear Receptors and Gene Regulation
What are T3 and T4 synthesized from?
Thyroglobulin (Tyr + I-).
p.26
Ion Channel Receptors and Neurotransmission
What happens when three ATP molecules bind to P2X receptors?
The channel opens, allowing Na, K, and Ca to flow, leading to depolarization.
p.2
Receptor Desensitization and Downregulation
受體的胞吞作用 (endocytosis) 是如何促進的?
與 β-arrestin 結合的受體會與被膜小凹結合，促進胞吞作用。
p.17
Ion Channel Receptors and Neurotransmission
What can high concentrations of Mg2+ and Ca2+ do to zinc channels?
They can inhibit the opening of zinc channels.
p.4
G Protein-Coupled Receptors (GPCRs)
What is the role of 5-HT2 receptors?
They activate phospholipase C, leading to increased intracellular calcium levels.
p.13
Nuclear Receptors and Gene Regulation
What is the primary function of PPAR (Peroxisome Proliferator-Activated Receptor)?
To increase the number of peroxisomes in cells.
p.13
Nuclear Receptors and Gene Regulation
What are the three subtypes of PPAR?
PPAR-α, PPAR-β, and PPAR-γ.
p.8
Nuclear Receptors and Gene Regulation
What are the five regions of the nuclear receptor structure?
N-terminal domain (NTD), DNA binding domain (DBD), hinge domain, ligand binding domain (LBD), and C-terminal domain (CTD).
p.21
Enzyme-Catalyzed Secondary Messengers
What is the function of cofactors in enzymes?
Cofactors are inorganic substances needed by enzymes, such as ions like Fe²⁺, Cu²⁺, and Mg²⁺.
p.2
G Protein-Coupled Receptors (GPCRs)
什麼是捲曲受體 (Frizzled receptor)?
是一類 G 蛋白偶聯受體 (GPCR)，調控胚胎發育和神經突觸的形成。
p.13
Nuclear Receptors and Gene Regulation
What is a therapeutic use of PPAR-α agonists like Fenofibrate?
To lower triglycerides and prevent atherosclerosis.
p.17
Ion Channel Receptors and Neurotransmission
Where are 5-HT3 receptors located?
In presynaptic neurons, particularly in GABA and glutamatergic neurons.
p.13
Nuclear Receptors and Gene Regulation
What role does PPAR-β play in the body?
It is involved in cell proliferation, differentiation, and tissue repair.
p.11
Nuclear Receptors and Gene Regulation
How do glucocorticoids affect pro-inflammatory transcription factors?
They inhibit pro-inflammatory cytokines by binding to transcription factors like AP-1 and NF-κB.
p.8
Nuclear Receptors and Gene Regulation
How do steroid nuclear receptors typically form dimers?
They usually form homodimers with half-sites separated by three spacers.
p.20
Ion Channel Receptors and Neurotransmission
What is the effect of increased Ca²⁺ influx on muscle contraction?
It promotes the release of stored Ca²⁺, facilitating contraction.
p.11
Nuclear Receptors and Gene Regulation
What is the difference in binding strength between mineralocorticoids and glucocorticoids?
Mineralocorticoids bind more strongly to MR than glucocorticoids bind to CR.
p.8
Nuclear Receptors and Gene Regulation
What happens when an agonist binds to the nuclear receptor?
It causes a shift in the orientation of H12, stabilizing the LBD conformation for coactivator binding.
p.13
Nuclear Receptors and Gene Regulation
What are the side effects of PPAR-γ agonists?
Fluid retention, weight gain, and edema, which can be contraindicated in heart failure patients.
p.7
Nuclear Receptors and Gene Regulation
What happens when an agonist activates a nuclear receptor?
It binds to specific DNA response elements, leading to gene expression.
p.20
Ion Channel Receptors and Neurotransmission
What are the subtypes of voltage-dependent Ca²⁺ channels?
T, L, N, P, Q, R channels.
p.7
Nuclear Receptors and Gene Regulation
What are orphan receptors?
Receptors whose ligands are unknown.
p.26
Ion Channel Receptors and Neurotransmission
How many isoforms of P2X receptors are there?
Seven isoforms (P2X1 to P2X7).
p.2
Receptor Desensitization and Downregulation
超敏化作用 (supersensitivity) 是什麼?
細胞受體與拮抗劑結合後，長期無反應，導致細胞自行合成更多受體。
p.25
Enzyme-Catalyzed Secondary Messengers
What is the mechanism of action for adenosine deaminase?
It involves nucleophilic attack by water, forming a tetrahedral intermediate.
p.4
G Protein-Coupled Receptors (GPCRs)
What is the function of 5-HT1 receptors?
They inhibit adenylyl cyclase, leading to decreased cAMP and hyperpolarization.
p.7
Nuclear Receptors and Gene Regulation
What role does HSP (heat shock protein) play in nuclear receptor activation?
It dissociates from the NR-hormone complex, allowing the complex to translocate to the nucleus.
p.24
G Protein-Coupled Receptors (GPCRs)
What is the role of ligands in GPCR function?
Ligands bind to the receptor, activating it and initiating signal transduction.
p.26
Ion Channel Receptors and Neurotransmission
What is the mechanism of voltage-gated ion channels?
They are regulated by changes in membrane potential, not by ligands.
p.7
Nuclear Receptors and Gene Regulation
What characterizes inactive nonsteroid nuclear receptors?
They exist as dimers in the nucleus and bind to corepressors to inhibit gene transcription.
p.20
Ion Channel Receptors and Neurotransmission
What is the role of receptor-operated channels (ROC) in calcium influx?
They allow Ca²⁺ to flow into the cell.
p.11
Nuclear Receptors and Gene Regulation
How do glucocorticoids influence gene transcription?
They bind to GRE, promoting GR's movement from the cytoplasm to the nucleus to regulate gene transcription.
p.21
Enzyme-Catalyzed Secondary Messengers
What is the role of coenzymes in enzymatic reactions?
Coenzymes are organic molecules required by enzymes, such as FAD⁺ and NAD⁺.
p.8
Nuclear Receptors and Gene Regulation
What is the role of the DNA binding domain (DBD)?
It selectively binds to specific DNA response elements to initiate gene transcription.
p.16
Ion Channel Receptors and Neurotransmission
What is the role of antagonists at the nicotinic acetylcholine receptor?
They inhibit receptor activation, preventing depolarization and muscle contraction.
p.26
Ion Channel Receptors and Neurotransmission
Where is the Ka inate receptor located?
Post-synaptically in ganglia for neuronal excitation.
p.17
Ion Channel Receptors and Neurotransmission
What is the role of 5-HT3 receptors in the brainstem and forebrain?
They are involved in the vomiting center.
p.25
Enzyme-Catalyzed Secondary Messengers
How do enzymes affect activation energy?
Enzymes lower the activation energy of reactions, thereby accelerating them.
p.14
Nuclear Receptors and Gene Regulation
How does Calcitriol affect calcium absorption?
It promotes gastrointestinal absorption of calcium and regulates blood calcium levels.
p.20
Ion Channel Receptors and Neurotransmission
What happens when Ca²⁺ efflux decreases?
It terminates contraction and protects the cell from excessive excitation.
p.21
Enzyme-Catalyzed Secondary Messengers
How do competitive inhibitors affect enzyme kinetics?
They change the Km value but do not affect Vmax.
p.19
Ion Channel Receptors and Neurotransmission
What are the two main types of excitatory amino acid receptors (EAA)?
Ionotropic and Metabotropic.
p.15
Ion Channel Receptors and Neurotransmission
What is the function of ligand-gated ion channels?
They open or close in response to the binding of a ligand.
p.21
G Protein-Coupled Receptors (GPCRs)
What is the role of tyrosine kinase receptors?
They are involved in phosphorylation and are activated by ligands like insulin and EGF.
p.19
Ion Channel Receptors and Neurotransmission
What are the three types of ionotropic receptors mentioned?
NMDA, AMPA, and Kainate receptors.
p.15
Ion Channel Receptors and Neurotransmission
What is the structure of ligand-gated ion channels?
They are pentameric receptors composed of five subunits.
p.7
Nuclear Receptors and Gene Regulation
What occurs when a steroid hormone binds to an unbound steroid receptor?
The receptor dimerizes and is transported to the nucleus.
p.3
G Protein-Coupled Receptors (GPCRs)
腎上腺性受體的TMD5和TMD6有什麼特別之處？
它們的胞內loop中存在最大差異，影響G蛋白的結合。
p.12
Nuclear Receptors and Gene Regulation
What physiological functions do thyroid hormones regulate?
Brain development, thermogenesis, increased heart function, and increased cellular metabolism.
p.2
Receptor Desensitization and Downregulation
受體的磷酸化對去敏感化有何影響?
受體的磷酸化會導致其與 G 蛋白無法偶合，從而減少反應。
p.19
Ion Channel Receptors and Neurotransmission
What is unique about the Glycine binding site on NMDA receptors?
It is strychnine-insensitive.
p.1
cAMP and cGMP Signaling
cGMP的作用是什麼？
cGMP活化cGMP依賴的蛋白激酶，進行磷酸化反應，影響細胞功能。
p.1
Receptor Desensitization and Downregulation
如何終止cAMP的信號反應？
cAMP被磷酸二酯酶（PDE）降解，或通過主動運輸送出細胞外。
p.23
Nuclear Receptors and Gene Regulation
What happens when RAR binds to RXR?
They form a heterodimer that binds to RARE (response element) to activate gene transcription.
p.4
Opioid Receptors and Pain Regulation
What is the pharmacological effect of Pirenzepine?
It antagonizes muscarinic receptors, blocking gastric acid secretion.
p.14
Nuclear Receptors and Gene Regulation
What is the active form of Vitamin D called?
Calcitriol (1,25-dihydroxycholecalciferol).
p.2
G Protein-Coupled Receptors (GPCRs)
孤兒受體 (Orphan receptor) 是什麼?
與其他已確認的受體結構相似，但尚未發現其內源性配體的受體。
p.16
Ion Channel Receptors and Neurotransmission
What is the mechanism of action of trimethaphan?
It acts as a ganglionic blocker by first activating and then inhibiting the nicotinic receptors.
p.13
Nuclear Receptors and Gene Regulation
What is the primary function of PPAR-γ?
To promote adipocyte differentiation and increase insulin sensitivity.
p.21
Enzyme-Catalyzed Secondary Messengers
What is the induced-fit effect in enzyme activity?
It refers to the enzyme's ability to change shape to better fit the substrate.
p.16
Ion Channel Receptors and Neurotransmission
What are the side effects of neuromuscular blockers like succinylcholine?
They can cause hypotension, muscle twitching, and histamine release leading to skin itching or bronchospasm.
p.15
Ion Channel Receptors and Neurotransmission
What type of ion channel is the Nicotinic acetylcholine receptor?
Ligand-gated ion channel (LGIC).
p.25
Enzyme-Catalyzed Secondary Messengers
What happens to adenosine in the presence of adenosine deaminase?
Adenosine is hydrolyzed to inosine, which can metabolize to purine.
p.8
Nuclear Receptors and Gene Regulation
What occurs when an antagonist binds to the nuclear receptor?
It destabilizes the LBD and recruits corepressors, leading to receptor inactivation.
p.13
Nuclear Receptors and Gene Regulation
How do PPAR receptors transmit signals?
By forming heterodimers with retinoid X receptors (RXR) and binding to response elements.
p.25
Enzyme-Catalyzed Secondary Messengers
What is the consequence of high adenosine concentration?
It can harm B cells and lead to decreased immunity.
p.8
Nuclear Receptors and Gene Regulation
What is the structure of AF-2 in the ligand binding domain?
It consists of 12 alpha-helices (H1-H12) stacked in an antiparallel manner, forming a hydrophobic binding pocket.
p.20
Ion Channel Receptors and Neurotransmission
What is the primary function of L-type calcium channels?
They are long-lasting channels primarily involved in muscle contraction.
p.17
Ion Channel Receptors and Neurotransmission
What is the role of zinc-activated channels (ZAC)?
They open in response to Zn2+, Cu2+, and H+, allowing cations to flow in.
p.15
Ion Channel Receptors and Neurotransmission
What is the role of GABA A receptors?
They mediate inhibitory neurotransmission.
p.25
Enzyme-Catalyzed Secondary Messengers
What role do antimetabolite drugs play?
They act as reversible enzyme inhibitors, affecting nucleotide conversion to triphosphate form.
p.26
Ion Channel Receptors and Neurotransmission
What role do Zn and Cu play in relation to P2X receptors?
They act as allosteric regulators of channel activity.
p.1
cAMP and cGMP Signaling
一氧化氮（NO）如何影響cGMP的生成？
NO進入細胞後與細胞質的guanylyl cyclase結合，促進cGMP生成。
p.23
Nuclear Receptors and Gene Regulation
What is the process of synthesizing all-trans retinoic acid (ATRA) from retinol?
Retinol is oxidized to retinaldehyde and then to all-trans retinoic acid (ATRA) by dehydrogenases.
p.12
Nuclear Receptors and Gene Regulation
What happens when there is a mutation in TR-α?
It can lead to growth retardation and constipation.
p.24
G Protein-Coupled Receptors (GPCRs)
What are the two states of GPCR?
Active state and inactive state.
p.12
Nuclear Receptors and Gene Regulation
What is the consequence of a mutation in TR-β?
Specific tissues lose sensitivity to T3, leading to compensatory increases in T3 and TSH levels, causing goiter.
p.24
G Protein-Coupled Receptors (GPCRs)
What is the function of the α-subunit in GPCR signaling?
It activates enzymes like adenylyl cyclase, leading to the production of secondary messengers like cAMP.
p.1
cAMP and cGMP Signaling
威爾鋼（sildenafil）如何影響cGMP的水平？
威爾鋼抑制PDE5，減少cGMP的降解，增加細胞內cGMP的量。
p.24
G Protein-Coupled Receptors (GPCRs)
What are agonists and antagonists in the context of GPCR?
Agonists activate the receptor, while antagonists inhibit receptor activity.
p.25
Enzyme-Catalyzed Secondary Messengers
How does sulfanilamide function as an antibiotic?
It competitively inhibits the synthesis of folic acid in bacteria.
p.4
G Protein-Coupled Receptors (GPCRs)
What is the role of M2 muscarinic receptors in the heart?
They decrease heart rate and have a negative chronotropic effect.
p.24
G Protein-Coupled Receptors (GPCRs)
What is the significance of the hydrophobic and hydrophilic regions in GPCR?
Hydrophobic regions interact with the cell membrane, while hydrophilic regions interact with the aqueous environment.
p.23
Nuclear Receptors and Gene Regulation
What are the therapeutic applications of retinoids?
They are used to treat skin diseases, acne, psoriasis, and certain cancers.
p.21
Enzyme-Catalyzed Secondary Messengers
What effect does the proximity effect have on enzyme reactions?
It brings two substrates closer together to facilitate effective collisions.
p.14
Nuclear Receptors and Gene Regulation
What are some functions of Calcitriol?
Regulates parathyroid hormone synthesis, cell differentiation, immune function, and calcium absorption.
p.2
G Protein-Coupled Receptors (GPCRs)
如何鑑定孤兒受體的內源性配體?
透過 cDNA screen assay 方法篩選候選配體並檢測其活性。
p.7
Nuclear Receptors and Gene Regulation
What is the primary function of nuclear receptors?
To regulate physiological functions, mitosis, differentiation, embryonic development, organ system metabolism, and homeostasis.
p.26
Ion Channel Receptors and Neurotransmission
What is the sensitivity of the Ka inate receptor to Domoic acid compared to AMPA?
Ka inate is more sensitive than AMPA.
p.2
Receptor Desensitization and Downregulation
β-受體去敏感化的機轉是什麼?
當致效劑結合後，受體結構改變，導致 G 蛋白無法與受體偶合，反應降低。
p.17
Ion Channel Receptors and Neurotransmission
What is the mechanism of glycine receptors?
They are ligand-gated ion channels that allow Cl- to flow in, leading to hyperpolarization (IPSP).
p.2
Receptor Desensitization and Downregulation
受體的下調節作用是什麼?
長期暴露於致效劑後，受體數量減少，需時間合成新受體才能恢復正常反應。
p.17
Ion Channel Receptors and Neurotransmission
What are some effects of activating glycine receptors?
They can lead to muscle relaxation, sedation, and anesthesia.
p.24
G Protein-Coupled Receptors (GPCRs)
What does GPCR stand for?
G Protein-Coupled Receptor.
p.1
Phospholipase C and Calcium Signaling
G_q如何影響細胞內鈣離子？
G_q激活磷脂酶C，生成DAG和IP3，IP3促進內質網釋放Ca²⁺。
p.19
Ion Channel Receptors and Neurotransmission
What is the role of NMDA receptors in neuronal plasticity?
They regulate long-term potentiation (LTP) and long-term depression (LTD).
p.20
Ion Channel Receptors and Neurotransmission
What is the significance of the α1 subunit in L-type calcium channels?
It is a transmembrane protein that forms the Ca²⁺ ion channel.
p.9
Nuclear Receptors and Gene Regulation
What is the primary function of Estrogen Receptor (ER)?
Regulates the estrous cycle, pregnancy, breast development, secondary sexual characteristics, cognition, emotions, bone density, and fat distribution.
p.7
Nuclear Receptors and Gene Regulation
What is the role of coactivators in nuclear receptor function?
They are recruited to regulate gene transcription after the receptor binds to DNA response elements.
p.24
G Protein-Coupled Receptors (GPCRs)
What happens to the G-protein upon activation of GPCR?
The G-protein undergoes a conformational change and exchanges GDP for GTP.
p.15
Ion Channel Receptors and Neurotransmission
What is the response time of ligand-gated ion channels?
They respond rapidly, typically within milliseconds.
p.9
Nuclear Receptors and Gene Regulation
What is the role of coactivators in ER signaling?
They bind to the activated ER-α through AF-1 to facilitate gene transcription.
p.26
Ion Channel Receptors and Neurotransmission
What is the effect of Lidocaine on Na channels?
It blocks Na influx by entering the cell in its non-ionized form.
p.15
Ion Channel Receptors and Neurotransmission
What is the effect of the 5-HT3 receptor?
It causes depolarization and excitatory postsynaptic potential (EPSP).
p.5
Opioid Receptors and Pain Regulation
What are the three subtypes of opioid receptors?
MOP-μ (mu), DOP-δ (delta), KOP-κ (kappa).
p.4
G Protein-Coupled Receptors (GPCRs)
What is the function of M3 muscarinic receptors?
They cause smooth muscle contraction and gland secretion.
p.5
Opioid Receptors and Pain Regulation
What physiological effects are associated with the μ2 receptor?
Respiratory depression and euphoria.
p.22
Enzyme-Catalyzed Secondary Messengers
不可逆性抑制是什麼？
時間依賴去活性作用，與酵素蛋白質的胺基酸殘基形成共價鍵。
p.1
cAMP and cGMP Signaling
心房利鈉因子（ANF）如何影響cGMP的生成？
ANF結合到細胞膜上的受體，活化guanylyl cyclase，促進cGMP生成。
p.23
Nuclear Receptors and Gene Regulation
What is the primary function of Retinoic Acid Receptor (RAR)?
To regulate embryonic development, organogenesis, cell differentiation, and apoptosis.
p.25
Enzyme-Catalyzed Secondary Messengers
How do drugs designed with 'masked phosphate groups' work?
They convert to mono phosphate in the body and finally to tri phosphate for therapeutic effect.
p.4
G Protein-Coupled Receptors (GPCRs)
What is the effect of 5-HT4, 5-HT6, and 5-HT7 receptors?
They stimulate adenylyl cyclase, leading to increased cAMP.
p.19
Ion Channel Receptors and Neurotransmission
What is the effect of Mg2+ on NMDA receptors?
It prevents Ca2+ influx, providing neuroprotection.
p.19
Ion Channel Receptors and Neurotransmission
What is the primary function of AMPA receptors?
Mediating fast synaptic transmission.
p.22
Enzyme-Catalyzed Secondary Messengers
如何證實催化中心的胺基酸是重要活化位？
使用site-directed mutagenesis實驗改變催化中心的胺基酸。
p.19
Ion Channel Receptors and Neurotransmission
What happens to Na+ and K+ during AMPA receptor activation?
Na+ influx increases and K+ efflux decreases.
p.24
G Protein-Coupled Receptors (GPCRs)
What types of ligands can activate GPCRs?
Biogenic amines, amino acids, neuropeptides, hormones, and endogenous opioids.
p.9
Nuclear Receptors and Gene Regulation
How do PR-A and PR-B differ in terms of amino acid sequences?
PR-B has 165 more amino acids than PR-A and contains an additional AF-3 regulatory domain.
p.12
Nuclear Receptors and Gene Regulation
What is the role of the hinge region in TR?
It provides flexibility for the dimer to bind to TRE in different orientations.
p.9
Nuclear Receptors and Gene Regulation
What is the controversy surrounding the use of hormone therapy involving progesterone and estrogen?
It may increase the incidence of breast cancer.
p.18
Ion Channel Receptors and Neurotransmission
What type of receptor is GABA A?
A ligand-gated ion channel that allows Cl- to flow in, leading to hyperpolarization.
p.18
G Protein-Coupled Receptors (GPCRs)
What is the significance of the α and γ subunits in GABA receptors?
They influence the affinity of drugs for the receptor and their effects, such as sedation or anxiolytic properties.
p.15
Ion Channel Receptors and Neurotransmission
What is the main characteristic of voltage-gated ion channels?
They open or close in response to changes in membrane potential.
p.25
Enzyme-Catalyzed Secondary Messengers
What is the function of HIV reverse transcriptase inhibitors?
They inhibit the synthesis of DNA in HIV, affecting viral replication.
p.4
G Protein-Coupled Receptors (GPCRs)
What is the significance of the homology groups in serotonin receptors?
They indicate the similarity in amino acid sequences, affecting receptor function.
p.25
Enzyme-Catalyzed Secondary Messengers
What is the effect of captopril and enalaprilat?
They act as ACE inhibitors, leading to lowered blood pressure.
p.5
Opioid Receptors and Pain Regulation
What are the endogenous opioid peptides mentioned?
Enkephalin, endorphin, dynorphin.
p.25
Enzyme-Catalyzed Secondary Messengers
What is the role of physostigmine?
It inhibits acetylcholinesterase, increasing acetylcholine levels for treating glaucoma.
p.5
G Protein-Coupled Receptors (GPCRs)
What is the effect of dimerization of opioid receptors?
It decreases the affinity of agonists for the receptor, impairing signal transduction.
p.19
Ion Channel Receptors and Neurotransmission
Which substances enhance AMPA receptor activity?
Paracetamol and cyclothiazide.
p.22
Enzyme-Catalyzed Secondary Messengers
開發合理化抑制劑的步驟是什麼？
隨機篩選化合物、天然物，然後修飾結構成為lead結構。
p.12
Nuclear Receptors and Gene Regulation
What occurs in the absence of ligand binding to TR?
TR dimers bind to TRE with corepressor complexes, inhibiting gene transcription.
p.18
Ion Channel Receptors and Neurotransmission
What is the role of the GABA C receptor?
It has strong and prolonged effects, primarily found in the retina and spinal cord, and is less affected by most agonists/antagonists.
p.26
Ion Channel Receptors and Neurotransmission
How do Gs and Gi proteins affect ion channels?
Gs increases cAMP and opens Ca channels, while Gi decreases cAMP and opens K channels.
p.7
Nuclear Receptors and Gene Regulation
What happens when an agonist binds to an inactive nonsteroid nuclear receptor dimer?
Corepressors are exchanged for coactivators, activating transcription.
p.15
Ion Channel Receptors and Neurotransmission
What ions do ligand-gated channels typically allow to flow?
Ions flow according to their concentration gradient.
p.9
Nuclear Receptors and Gene Regulation
What is the mechanism of action for the Estrogen Receptor dimer?
It enters the nucleus, binds to Estrogen Response Elements (ERE), and recruits coactivators to enhance transcription.
p.4
G Protein-Coupled Receptors (GPCRs)
What are the effects of M1 muscarinic receptors?
They increase cognitive function and DA release, and are linked to Alzheimer's disease.
p.23
Nuclear Receptors and Gene Regulation
What is the effect of ATRA on acute promyelocytic leukemia (APL)?
ATRA causes corepressors to dissociate from RAR, promoting gene transcription and differentiation of immature cells.
p.12
Nuclear Receptors and Gene Regulation
In what forms do thyroid hormone receptors exist?
As homodimers and heterodimers.
p.12
Nuclear Receptors and Gene Regulation
What happens when TR binds to its ligand?
It undergoes a conformational change that releases corepressors and recruits coactivators, promoting gene transcription.
p.5
G Protein-Coupled Receptors (GPCRs)
What is the mechanism of action for opioid receptors?
They inhibit adenylate cyclase, leading to decreased cAMP levels and hyperpolarization of the cell.
p.18
Second Messenger Pathways
How do neurosteroids affect GABA?
They enhance GABA-mediated inhibitory effects.
p.23
Nuclear Receptors and Gene Regulation
What is the role of corepressors in the absence of ligands for RAR?
Corepressors inhibit gene transcription by binding to the RAR dimer.
p.12
Nuclear Receptors and Gene Regulation
How do T3 and T4 interact with TR?
They form hydrogen bonds with specific amino acids in the receptor.
p.15
Ion Channel Receptors and Neurotransmission
What is the effect of Glycine receptors?
They mediate hyperpolarization and inhibitory postsynaptic potential (IPSP).
p.23
Nuclear Receptors and Gene Regulation
What is the significance of RXR in relation to retinoic acid?
RXR forms heterodimers with RAR and other nuclear receptors, influencing gene expression.
p.9
Nuclear Receptors and Gene Regulation
What is the significance of the interaction between Progesterone Receptor (PR) and Estrogen Receptor (ER)?
It can inhibit ER-mediated gene expression and alter estrogen signaling pathways.
p.23
Nuclear Receptors and Gene Regulation
What distinguishes permissive from non-permissive heterodimers involving RXR?
Permissive heterodimers activate gene expression when a ligand binds to either receptor, while non-permissive require a ligand to bind specifically to RXR.
p.5
Opioid Receptors and Pain Regulation
What is the effect of opioids on substance P release?
Opioids can inhibit the release of substance P, reducing pain signaling.
p.18
G Protein-Coupled Receptors (GPCRs)
What is the function of GABA B receptors?
They are G protein-coupled receptors that allow K+ to flow out, leading to inhibition.
p.18
Opioid Receptors and Pain Regulation
What is the effect of the competitive antagonist bicuculline?
It blocks GABA A receptors, leading to convulsions.
p.5
Opioid Receptors and Pain Regulation
What is the role of the NOP receptor?
It is related to opioid-like effects and pain regulation.
p.22
Enzyme-Catalyzed Secondary Messengers
TPCK和TLCK的作用是什麼？
分別是與serine protease和trypsin產生親和性標記的不可逆性抑制劑。
p.18
Enzyme-Catalyzed Secondary Messengers
What are benzodiazepines and barbiturates in relation to GABA?
They are positive allosteric modulators that increase GABA activity without directly activating the receptor.
p.18
Receptor Desensitization and Downregulation
What is the role of flumazenil?
It is a competitive antagonist that reverses benzodiazepine overdose by binding to the same allosteric site.
p.5
Opioid Receptors and Pain Regulation
What are some selective agonists for opioid receptors?
Morphine, sufentanil, DAMGO.
p.18
Nuclear Receptors and Gene Regulation
What is the effect of GABA A receptor activation on NMDA receptors?
Activation of GABA A receptors can offset the effects of NMDA receptors, which are involved in learning and memory.
