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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
Storage
1.) Where are pituitary and hypothalamus hormones stored?
In large peptides
Release
1.) How are pituitary and hypothalamus hormones released? (2)
Peptide cleavage from proteases and peptidases
Degradation
1.) how are pituitary and hypothalamus hormones degraded/metabolized?
Via hydrolysis/ proteolytic degradation
The 3 ways hormone RELEASE is controlled
1.) Stimulatory signals
2.) Inhibitory signals
3.) Feedback inhibition
Stimulatory signals
a.) come from (2)
b.) indication
a.) ANTERIOR pituitary and hypothalamus
b.) "go" release hormones
Inhibitory signal
a.) come from
b.) indication
a.) hypothalamus
b.) "stop" release hormones
feedback inhibition
a.) definition
This is when the end product makes a steroid product to stop the synthesizing organ from making a hormone signal
Role of circulatory system
Transports hormones to the end product
Nomenclature
a.) hypothalamic releasing factor
b.) hypothalamic inhibitory factor
c.) anterior stimulating factor
a.) liberin
b.) statin
c.) tropin
Tropin
anterior stimulating factor
Statin
Hypothalamic inhibitory factor
Liberin
Hypothalamic releasing factor
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
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
How are pituitary and hypothalamic hormones used therapeutically? (2)
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
Oxytocin
a.) indication
b.) type of hormone
Oxytocin
a.) induce labor, eject millk
b.) posterior pituitary hormone
Vasopressin
a.) indication (2)
b.) type of hormone
a.) water resorption; vasoconstriction in diabetes insipidus
b.) pituitary hormone
Indications of desmopressin (4)
1.) Antidiuretic for diabetes insipidus
2.) management polyuria from head trauma
3.) management excessive bleeding from patients with hemophilia A
4.) von Williebrand disease
3 types of pituitary hormones
1.) oxytocin
2.) vasopressin
3.) desmopressin

*also lypressin, terlipressin
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
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
Feedback mechanism of ovulation (hormones + targets)
Estrogen and progesterone target the anterior pituitary and hypothalamus
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
Feedback mechanism of spermatogenesis (hormone and target)
Testosterone targets the testes
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
Which hormone has a pGlu-His-Pro-NH2 sequence?
Hypothalamic hormones: TRH
Which hormone involves cyclic nonapeptide?
Posterior pituitary hormones (Oxytocin, Vasopressin, Desmopressin)
Which hormone is involved with type-II beta turn?
hypothalamic hormone LH-RH
How to tighten the U-turn on LH-RH
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
How to widen the U-turn of LH-RH
Replace the Glycine6 with L-amino acid. Widening the distance between N-terminus and C-terminus decreases binding
What do you call an LH-RH analog that is more potent than the endogenous LH-RH?
Super agonist
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)
What position is important for super agonists to work?
6 position of the LH-RH analog. Replace it with a hydrophobic D-amino acid
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
Main components of an LH-RH antagonist (2)
Hydrophobic, D-amino acid, especially cyclic D-Phe on 2 position
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
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
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
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
1,2,3 10 positions
LH-RH antagonist