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41 Cards in this Set
- Front
- Back
Biosynthesis
1.) Where are pituitary and hypothalamus hormones synthesized? |
In the POSTERIOR pituitary and hypothalamus
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Storage
1.) Where are pituitary and hypothalamus hormones stored? |
In large peptides
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Release
1.) How are pituitary and hypothalamus hormones released? (2) |
Peptide cleavage from proteases and peptidases
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Degradation
1.) how are pituitary and hypothalamus hormones degraded/metabolized? |
Via hydrolysis/ proteolytic degradation
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The 3 ways hormone RELEASE is controlled
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1.) Stimulatory signals
2.) Inhibitory signals 3.) Feedback inhibition |
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Stimulatory signals
a.) come from (2) b.) indication |
a.) ANTERIOR pituitary and hypothalamus
b.) "go" release hormones |
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Inhibitory signal
a.) come from b.) indication |
a.) hypothalamus
b.) "stop" release hormones |
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feedback inhibition
a.) definition |
This is when the end product makes a steroid product to stop the synthesizing organ from making a hormone signal
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Role of circulatory system
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Transports hormones to the end product
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Nomenclature
a.) hypothalamic releasing factor b.) hypothalamic inhibitory factor c.) anterior stimulating factor |
a.) liberin
b.) statin c.) tropin |
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Tropin
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anterior stimulating factor
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Statin
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Hypothalamic inhibitory factor
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Liberin
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Hypothalamic releasing factor
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Chain of command: Thyroid hormone
1.) Hypothalamus 2.) Anterior Pituitary 3.) End organ + hormone |
Thyroid hormone
1.) Hypothalamus - TRH (thyroliberin) 2.) Anterior pituitary - TSH (thyrotropin) 3.) End organ - Thyroid hormone: T3/T4 |
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Chain of command: Reproductive hormones (x2)
a.) Hypothalamus b.) Anterior Pituitary c.) End organ + hormone |
Reproductive hormones (x2)
a.) Hypothalamus - FSH-RH and LH-RH b.) Anterior pituitary - FSH and LH c.) End organ - Ovaries and Tests: Progesterone, estrogen, testosterone |
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How are pituitary and hypothalamic hormones used therapeutically? (2)
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1.) To treat diseases (growth, cancer, infertility) by acting as hormone replacement therapy
2.) As a diagnostic tool to see if the hormones are produced in the right amount |
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Oxytocin
a.) indication b.) type of hormone |
Oxytocin
a.) induce labor, eject millk b.) posterior pituitary hormone |
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Vasopressin
a.) indication (2) b.) type of hormone |
a.) water resorption; vasoconstriction in diabetes insipidus
b.) pituitary hormone |
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Indications of desmopressin (4)
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1.) Antidiuretic for diabetes insipidus
2.) management polyuria from head trauma 3.) management excessive bleeding from patients with hemophilia A 4.) von Williebrand disease |
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3 types of pituitary hormones
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1.) oxytocin
2.) vasopressin 3.) desmopressin *also lypressin, terlipressin |
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TRH
a.) origin b.) MOA c.) SAR (3) + characteristics of each d.) antagonist |
TRH - Thyrotropin RELEASING hormone
a.) hypothalamus b.) binds to anterior pituitary to cause TSH release, which goes to the thyroid gland to make T3/T4 c.) pGlu-His-Pro-NH2. The amide on the pyroglutamic acid is for H-bonding. The histidine is flat and basic for binding. The c-terminal amide is for stability from carboxypeptidases and participates in H-bonding d.) replace histidine with phenylalanine |
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Ovulation
a.) hypothalamus b.) anterior pituitary c.) end organ |
a.) hypothalamus releases Gn-RH/ LH-RH, which goes to the anterior pituitary
b.) anterior pituitary releases FSH and LH, which go to the ovaries c.) ovaries make estrogen and progesterone |
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Feedback mechanism of ovulation (hormones + targets)
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Estrogen and progesterone target the anterior pituitary and hypothalamus
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Spermatogenesis
a.) hypothalamus b.) anterior pituitary c.) end organ |
a.) hypothalamus releases Gn-RH/LH-RH to the anterior pituitary
b.) anterior pituitary releases FSH and LH to the testes c.) testes make testosterone |
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Feedback mechanism of spermatogenesis (hormone and target)
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Testosterone targets the testes
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D-amino acid
a.) incorporation causes antagonist activity and which hormone? (2) b.) incorporation causes increased intrinsic activity, potency, and duration and on which hormone? |
D-amino acid
a.) switch D-cysteine from L-cysteine in posterior pituitary hormone (oxytocin) = antagonist; hypothalamic LH-RH antagonist (D-Phe on 2 position) b.) switch D-Phe (or other hydrophobic aa) from glycine6 on LH-RH increases intrinsic activity and binding by tightening the "U" of the Type-II beta-turn. Super agonist |
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Which hormone has a pGlu-His-Pro-NH2 sequence?
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Hypothalamic hormones: TRH
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Which hormone involves cyclic nonapeptide?
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Posterior pituitary hormones (Oxytocin, Vasopressin, Desmopressin)
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Which hormone is involved with type-II beta turn?
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hypothalamic hormone LH-RH
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How to tighten the U-turn on LH-RH
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Replace the Glycine6 with D-amino acid that is hydrophobic (D-phenylalanine). Tightening the space between the N-terminus and C-terminus increases intrinsic activity, duration, potency, binding. Super agonist
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How to widen the U-turn of LH-RH
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Replace the Glycine6 with L-amino acid. Widening the distance between N-terminus and C-terminus decreases binding
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What do you call an LH-RH analog that is more potent than the endogenous LH-RH?
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Super agonist
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super agonist LH-RH
a.) MOA b.) indication (2) |
a.) LH-RH super agonist binds tightly to the LH-RH receptor on the anterior pituitary, causing a release of FSH and LH. This goes to the ovaries to increase production of estrogen, progesterone, and testosterone. Then the LH-RH receptors in the anterior pituitary sense over-saturation and get down-regulated, resulting in decrease of FSH and LH
b.) this is good to stop tumors or treat infertility (stop patient's hormones so doctor can take over and start hormone treatment) |
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What position is important for super agonists to work?
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6 position of the LH-RH analog. Replace it with a hydrophobic D-amino acid
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LH-antagonist
a.) position 1 b.) position 2 c.) position 3 d.) position 10 |
a.) position 1 is hydrophobic for increased transport into cell membranes. It also has N-blocked amino acid to protect it from aminopeptidase
b.) position 2 is hydrophobic for increased transport into cell membranes. It also has a aromatic D-amino acid for antagonist activity c.) position 3 has D-amino acid to protect from aminopeptidase d.) position 10 switches glycine to D-amino acid to protect from carboxypeptidase |
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Main components of an LH-RH antagonist (2)
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Hydrophobic, D-amino acid, especially cyclic D-Phe on 2 position
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LH-RH super agonist
a.) onset b.) receptor c.) permanence d.) duration |
a.) decreases stimulatory response within 4 weeks
b.) down-regulation of receptors c.) reversible castration for desired conditions d.) short-lived flare upon use |
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LH-RH antagonist
a.) onset b.) receptor c.) permanence d.) duration |
a.) gonadal suppression within hours
b.) no downregulation of receptors (unlike super agonists) c.) when withdrawn, rapid restoration of gonadal function d.) needs to be constantly present to suppress gonad function |
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Somatostatin
a.) hormone b.) roles (3) c.) indication (2) |
Somatostatin
a.) hypothalamic hormone b.) inhibits GH secretion, decreases TSH, regulates insulin and glucagon c.) acromegaly, tumors |
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Bone-growth
a.) hypothalamus b.) anterior pituitary c.) target organ |
a.) GH-RH comes from hypothalamus, goes to anterior pituitary
b.) GH secretes from anterior pituitary c.) epiphyses/ ends of the long bone = growth |
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1,2,3 10 positions
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LH-RH antagonist
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