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82 Cards in this Set
- Front
- Back
Diganostic Use only for Hypothyroidism
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Thyrotropin Releasing Hormone
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Gonadotropin Releasing Hormone is used to
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diagnose infertility and delayed puberty
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Goserelin
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used to treat prostate and breast cancer, treat endometriosis, help thin endometrium prior to a hysterectomy
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Gonadotropin antagonists
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prevent ovulation and the LH surge
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an example of a GnRH antagonist
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Cetrorelix
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Corticotropin Releasing Factor is used
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diagnotist use for cases of pituitary defects that present as Cushing's Disease
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Growth Hormone Releasing Factor is used diagnostically for
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kids with idiopathic growth hormone deficiency
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Growth Hormone Releasing Hormone is used treatment wise for:
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GHD where the pituitary workds fine, but the hypothalamus doesn't secret adequate GRF
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Dopamine is also knowns at
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Prolactin Release Inhibitory Factor
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Dopamine is not used in hormone therapy because:
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too many peripheral effects of dopamine in blood vessels and it is broken down by MAO's or other enzymes
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a type of dopamine that was used in women with pituitary tumors
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bromocriptine
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a type of dopamine that had less side effects than bromocriptine
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cabergoline
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somatostatin does not treat
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cancer itself
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inhibition of glucagon secretion by somatostain is _______ than its inhibition of insulin secretion
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greater
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a condition that has too much growth hormone and causes an enlargemetn of large bones in the hands, feet, and face, with an enlargement of the nose and lips
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Acromegaly
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Why is 111 Indium added?
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the agent is administed such that radioactivity is selectively delivered to kill the cells overexpressing somatostatin receptors
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70 times more effective than native somatostain
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Octreotide
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is being tested for use in cancer and it seems to be 2 to 3 times more potent than octreotide
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Lan-7
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for Somatostain, replacing a L-AA with a D-AA makes the analog how many more times active
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6-8 times
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in somatostatin, D-AA at position 14 makes an analog that is much more selective for inhibition of growth hormone and of glucagon than for inhibiting insuline release, which suggests
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that the peripheral receptors for somatostatin are structurally different
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the reasons why growth hormone has a long half life
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1/ the hormone is much larger than its active region, so the extra size protects the active region from enyzmatic destruction.
2/ it does not move in the blood as a free molecule, rather it is adsorbed onto plasma proteins |
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Some uses of growth hormone
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1/ children whose growth is abnormally slow,
2/ adults with GH deficiency 3/ girl's with turner's syndroms 4/ body wasting due to HIV 5/ cardiac insufficiency |
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insulin like growth factors
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somatomedins
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somatomedins act together with GH to:
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promote cartilage growth, stimulated protein synthesis, stimulate thymidine incorporation into DNA, and stimulate cell division
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prolactin has what with GH?
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16% homology
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why are proteins glycosylated?
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1/ to increase stability or half life-longer duration of action
2/ to faciliate the secreton of proteins from a cell 3/ to create recognition sites for other molecules |
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effects of prolactin
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1/ promote mammary gland proliferation
2/ release progesterone which renders the uterus suitable for imbedding of the ovum |
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oxytocin is:
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a synthetic peptide given only with strict medical supervison to induce labor or delivery
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lypressin is:
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given as a nasal spray and is used to treat diabetes insipidus- pituitary release of ADH doesnt occur properly
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desmopressin is:
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given as a nasal spray, orally, or parenteraly. used to treat the symports of diabetes insipidus, and used to treat children who experience uncontrolled bed wetting.
Cys removed and D-Arg replaces L-Arg |
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terlipressin is:
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given to treat bleeding of the esophagus that may result in cirrohis of the liver. also causes an increase in blood pressure which causes bulges that can rupture
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function of Throid Stimulating Hormone from the pituitary:
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promote release of T4 and T3 from thyroid gland and stimulate uptake of iodide from blood into acinar cells
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thyroxin-binding globulin
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only have 1 high-affinity binding site for homrone
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transthretin
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also called t4- binding pre-albumin since it only carries one of the hormones. it has an affinity 1000 times less affinity for t4 than thyroxin binding globulin, but theres more of it
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albumin
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carries 10% t4 and 30% of t3
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from a single tg molecule, only ______ hormones are released
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2 to 5
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transthyretin binds where
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the cooh end of the hormone binds a pair of lys residues at the mouth of the funnel, even bound by t4, also binds four molecules of vitamin A
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details about the binding of the nuclear receptor of t3 and t4
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1/ the I at postitions 3 and 5 on the inner ring keep the 2nd ring perpendicular
2/ the spacer atom between the rings keeps the second ring at an angle of 120 3/ the cooh end of the hormone forms half of an ion pair with the receptor 4/ the 4-oh is also a crutial part of the binding site of the hormome 5/ better binding if 3' has an isopropyl group or a lipophilic halogen |
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normal functions of t3 and t4
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promote oxygen uptake , gluclose availability, protein synthesis, generate heat, and growth and development
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hypothyroidism consequences
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non toxic goiter: lack of hormone from thyroid causes increased release of TSH that stimulated the thyroid to enlarge in order compensate
may have to do with lack of I2 diet |
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cretinism
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a lack of iodine during early childhood means lack of CNS development and a stunting of growth due to abmormal bone formation
hypothyroidism |
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myxedema
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lack of iodine, or loss of the thyroid, or lack of TSH can cause mucopolysaccharide infiltration of the spaces between cells of the skin and muscle, also anemia, mental apathy, and sensitivity to cold
hypothyroidism |
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hyperthyroidism consequences
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increased heart rate and cardiac output, anorexia, poor thermoregulation, toxi goiter
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graves disease
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autoantibodies against one's own TSH receptors on acinar cells of the thyroid lead to and overproduction and release of t4 and t3
hyperthyroidism |
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hashimoto's disease
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autoantibodies against Tg or other thyroid cell proteins lead to infiltration of cytotoxic t-cells, and also plug up the machinery needed for iodine uptake and incorportation to hormones. - lack of hormone, resulting in overproduction of TSH and goiter
hypothyroidism |
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for hypothyroidism what kind of hormone replacement do you need?
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1/ thyroid USP= acetone powder of cow or pig thyroid gland
2/ synthetic t4 (levothyroxine)- slower onset of action since higher affinity for carrier proteins 3/ synthetic t3 (liothyronine)rapid onset of action, and short duration |
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hyperthyroidism needs what?
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a hormone antagonist to block the peroxidase enzyme so th atless hormone is made
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prodrug of MMI that is converted to MMI in vivo
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carbimazole
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synthesized by the adrenal cortex
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glucocorticoids and mineralcorticoids
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primarily regulate water and sodium ion retention to maintain blood volume and electrolyte balance
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mineralcorticoids
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bile acids are trans or cis
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cis
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beta orientation are represented by
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solid line, or solid wedge
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alpha orientation are represented by
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dashed line or wedge made of short dashed lines
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pregnenolone
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have to remove 6 C's two hydroxylation steps followed by cleavage of the side chain in front of c22 by enzyme
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five major classes of steroid hormones
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progesterone, glucocorticoids, mineralcorticoids, andrgens, and estrogens
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progesterone
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oxidize 3-oh to a ketone and then osimerize the double bond
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glucocorticoids
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four steps from progesterone- three additions of oh then oxidation to 11-keto
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adrenal cortex hormones
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cortisol and aldosterone
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mineralcorticoids
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from progesterone, oh at 21 and oh at 11, followed by oh at 18 and oxidation to 18 aldehyde
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too much cortisol can lead to:
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muscle wasting or retarded growth
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cortisols function:
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maintain blood glucose availability, primary target is liver and then brain
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cortisols main therapeutic interest
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to conrol inflammation and associated redness, swelling, pain, local vasodialation
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essential for activity of aldosterone or cortisol
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double bond-delta 4, 3 keto and 20 keto
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essential for glucocorticoid activity
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21-oh and 11-B-oh
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analogs for anit-inflammatory activity
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9-alpha-fluoro greatly enhances activity- has greater glucocorticoid activity, but way toooo much mineralcorticoid activity
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what does adding a double bond at the c-1 do?
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selectively increases glucocorticoid activity by a factor of 5 without any change in the mineralcorticoid activity
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what does a c-16 methyl group do to activity?
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either alpha or beta increases glucocorticoid activity and decreases mineralcorticoid activity
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has 25 x the activity of cortisol
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betamethasone - beta solid methyl
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has 30 x activity of cortisol
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dexamethasone- alpha is dotted wedge
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aldosterone antagonists
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progesterone, series or spirolactones
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how to avoid the anti-androgen effect
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replace the thioester with a different ester 7alpha-C-O-CH3
C |
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short acting glucocorticoids
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cortisone acetate and hydrocortisone (cortisol)
treat insufficient output by the adrenal cortex: rheumatic arthritis or joint pain and inflammatory disorders |
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intermediate acting glucocorticoids
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prednisone, prednisolone, methyprednisolone, triamcinolone (esp for asthma)
for more severe conditions that often require chronic treatment |
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long acting glucocorticoids
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betamethasone, dexamethasone
for chronic inflammation, chronic allergic diseases, autoimmune diseases, and some cancers |
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one of the most serious adverse effects of long term glucocorticoid therapy
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osteoporosis
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steroids ususally have _____ net charge
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no
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does a steroid have the same conformation when bound to its receptor is when it is in a crystal?
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about the same.... yes - can do computer assissted "rationa" drug design of steroid analogs
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glucocorticoid receptors and mineralcorticoid receptors start where?
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in the cytoplasm
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estrogen, androgen, and progesterone receptors are where?
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only in the nucleus
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steroids have threee principle active regions
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a hormone binding region, a DNA binding region, and an N-terminal region used to allow binding of other proteins that enhance or repress DNA binding
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6 hypothalamic hormones
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thyrotropin releasing hormone, gonadotropin releasing hormone, corticotropin releasing hormone, growth hormone releasing hormone, prolactin release inhibiting hormone, somatostain
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secreted from the posterior pituitary
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vasopressin and oxytocin
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