Page last updated: 2024-12-09

thyrotropin-releasing hormone

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

PR 546: no other info available 9/89 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

protirelin : A tripeptide composed of L-pyroglutamyl, L-histidyl and L-prolinamide residues joined in sequence. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID638678
CHEMBL ID1472
CHEBI ID35940
SCHEMBL ID33419
SCHEMBL ID19825647
MeSH IDM0021497

Synonyms (114)

Synonym
5-oxo-l-prolyl-l-histidyl-l-prolinamide
thyrotropic-releasing factor
CHEBI:35940 ,
tsh-releasing factor
l-pyroglutamyl-l-histidyl-l-prolineamide
(2s)-n-[(2s)-1-[(2s)-2-carbamoylpyrrolidin-1-yl]-3-(3h-imidazol-4-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
gtpl2139
relefact trh (tn)
D00176
protirelin (jp17/usan/inn)
protireline [inn-french]
lopremone
protirelina [inn-spanish]
l-pyroglutamyl-l-histidinyl-l-prolinamide
thypinone
abbott 38579
thyrel trh
protirelinum [inn-latin]
einecs 246-143-4
ccris 2593
synthetic trh
l-prolinamide, 5-oxo-l-prolyl-l-histidyl-
rifathyroin
thyrotropin-releasing factor
synthetic tsh-releasing factor
ro 8-6270/9
fda 1725
thyroliberin
protirelin
C03958
24305-27-9
NCGC00160616-01
nsc-760113
5-oxo-pro-his-pro-nh2
protirelin, synthetic
CHEMBL1472
relefact trh
1-[3-(1h-4-imidazolyl)-2-(5-oxotetrahydro-1h-2-pyrrolylcarboxamido)propanoyl]tetrahydro-1h-2-pyrrolecarboxamide
a-38579
bdbm50072394
abbott-38579
(2s)-n-[(2s)-1-[(2s)-2-carbamoylpyrrolidin-1-yl]-3-(1h-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
dtxcid403533
dtxsid0023533 ,
tox21_111939
cas-24305-27-9
pr-546
pr 546
117217-40-0
11096-37-0
S4680
AKOS015994636
protirelinum
unii-5y5f15120w
nsc 760113
5y5f15120w ,
protirelin [usan:inn:ban:jan]
protireline
protirelin [usan]
trh [mi]
protirelin [orange book]
protirelin [jan]
protirelin [who-dd]
protirelin [mart.]
protirelin [inn]
protirelin [vandf]
protirelin [ep monograph]
gtpl3836
[3h]-trh
[3h]trh (human, mouse, rat)
SCHEMBL33419
HS-2023
relefact-trh
2-pyrrolidinecarboxamide, n-[1-[(2-carbamoyl-1-pyrrolidinyl)carbonyl]-2-imidazol-4-ylethyl]-5-oxo-, (s,s,s)-
synthetic trf
l-pyroglutamyl-l-histidyl-l-proline amide
pyroglu-his-prolinamide
2-pyrrolidinecarboxamide, n-[1-[(2-carbamoyl-1-pyrrolidinyl)carbonyl]-2-imidazol-4-ylethyl]-5-oxo-,
synthetic thyrotropin-releasing factor
XNSAINXGIQZQOO-SRVKXCTJSA-N
prolinamide, 5-oxo-l-prolyl-l-histidyl-, l-
synthetic thyrotopin releasing factor
thyrefact
tsh-rf
thyrotropin-releasing factor (pig)
prolinamide, 1-[n-(5-oxo-l-prolyl)-l-histidyl]-, l-
stimu-tsh
(pyro)-l-glutamic acid-l-histidine-l-proline-nh2
1-(3-(1h-imidazol-5-yl)-2-([(5-oxo-2-pyrrolidinyl)carbonyl]amino)propanoyl)-2-pyrrolidinecarboxamide #
mfcd00038640
(2s)-n-[(1s)-2-[(2s)-2-carbamoylpyrrolidino]-1-(1h-imidazol-5-ylmethyl)-2-keto-ethyl]-5-keto-pyrrolidine-2-carboxamide
(2s)-n-[(2s)-1-[(2s)-2-aminocarbonylpyrrolidin-1-yl]-3-(1h-imidazol-5-yl)-1-oxidanylidene-propan-2-yl]-5-oxidanylidene-pyrrolidine-2-carboxamide
protirelin, european pharmacopoeia (ep) reference standard
pyroglutamyl-histidyl-prolinamide
trh-sr
HY-P0002
holo-transferrin
(s)-n-((s)-1-((s)-2-carbamoylpyrrolidin-1-yl)-3-(1h-imidazol-5-yl)-1-oxopropan-2-yl)-5-oxopyrrolidine-2-carboxamide
SCHEMBL19825647
DB09421
24305-27-9 (free base)
(s)-n-((s)-1-((s)-2-carbamoylpyrrolidin-1-yl)-3-(1h-imidazol-4-yl)-1-oxopropan-2-yl)-5-oxopyrrolidine-2-carboxamide
Q24726011
pglu-his-pro-nh2
BCP12450
CCG-268193
A858244
C74244
pyr-his-pro-nh2
siderophilin;partially saturated
human transferrin
EN300-27034140
(2s)-1-[(2s)-3-(1h-imidazol-5-yl)-2-{[(2s)-5-oxopyrrolidin-2-yl]formamido}propanoyl]pyrrolidine-2-carboxamide
AKOS040759052

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
human metaboliteAny mammalian metabolite produced during a metabolic reaction in humans (Homo sapiens).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
peptide hormoneAny peptide with hormonal activity in animals, whether endocrine, neuroendocrine, or paracrine.
tripeptideAny oligopeptide that consists of three amino-acid residues connected by peptide linkages.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency6.00700.000214.376460.0339AID720691
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Thyrotropin-releasing hormone receptorMus musculus (house mouse)IC50 (µMol)0.01190.00260.01190.0260AID1239064; AID1286881; AID1286882
Thyrotropin-releasing hormone receptorMus musculus (house mouse)Ki0.01650.01000.01650.0230AID210544; AID213191
Thyrotropin-releasing hormone receptorHomo sapiens (human)Ki0.02000.02000.02000.0200AID283905
Thyrotropin-releasing hormone receptorRattus norvegicus (Norway rat)Ki0.03120.02000.03120.0423AID239477; AID254556
Thyroliberin receptor Mus musculus (house mouse)IC50 (µMol)0.00700.00700.00700.0070AID1239065; AID1286882
Thyroliberin receptor Rattus norvegicus (Norway rat)IC50 (µMol)11.51150.02300.02300.0230AID384275; AID385236
Thyroliberin receptor Rattus norvegicus (Norway rat)Ki0.01000.01000.01000.0100AID254533; AID283906
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Thyrotropin-releasing hormone receptorMus musculus (house mouse)EC50 (µMol)0.00110.00050.00110.0032AID1239066; AID1286884; AID1286885; AID1286887; AID1286888; AID213190; AID213192
Thyrotropin-releasing hormone receptorHomo sapiens (human)EC50 (µMol)0.00300.00300.00300.0030AID283907
Thyrotropin-releasing hormone receptorRattus norvegicus (Norway rat)EC50 (µMol)0.00300.00300.00300.0030AID254657
Thyroliberin receptor Mus musculus (house mouse)EC50 (µMol)0.00140.00050.00140.0031AID1239067; AID1286885; AID1286888
Thyroliberin receptor Rattus norvegicus (Norway rat)EC50 (µMol)0.00300.00300.00300.0030AID254651; AID283908
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (2)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayThyrotropin-releasing hormone receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayThyrotropin-releasing hormone receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (2)

Processvia Protein(s)Taxonomy
protein bindingThyrotropin-releasing hormone receptorHomo sapiens (human)
thyrotropin-releasing hormone receptor activityThyrotropin-releasing hormone receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
plasma membraneThyrotropin-releasing hormone receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (104)

Assay IDTitleYearJournalArticle
AID1286887Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA2016European journal of medicinal chemistry, Mar-23, Volume: 111Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues.
AID1286881Displacement of [3H]-Me-His-TRH from mouse TRH-R1 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs2016European journal of medicinal chemistry, Mar-23, Volume: 111Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues.
AID229207Binding affinity for sigma receptors was evaluated by the inhibitory effect on [3H]DTG to rat whole brain membranes;NT means not tested.2000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
3,4-dihydro-2(1H)-quinolinone as a novel antidepressant drug: synthesis and pharmacology of 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-3,4- dihydro-5-methoxy-2(1H)-quinolinone and its derivatives.
AID118385Activity was evaluated in C57BL/10 mice by Morris water Maze test and mean latency for TRH was reported at 0.03 mg/Kg i.p. dosage.1995Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
Peptide mimetics of thyrotropin-releasing hormone based on a cyclohexane framework: design, synthesis, and cognition-enhancing properties.
AID254651Signaling (activation) potency for thyrotropin releasing hormone receptor 2 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.82005Journal of medicinal chemistry, Sep-22, Volume: 48, Issue:19
Thyrotropin-releasing hormone (TRH) analogues that exhibit selectivity to TRH receptor subtype 2.
AID1239073Plasma concentration in Sprague-Dawley rat assessed as TSH level at 10 umol/kg, iv after 15 mins by ELISA method (Rvb = 5.52 ng/ml)2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis of CNS active thyrotropin-releasing hormone (TRH)-like peptides: Biological evaluation and effect on cognitive impairment induced by cerebral ischemia in mice.
AID213191Ability to bind thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells.1998Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21
Thyrotropin releasing hormone analogs: a building block approach to the construction of tetracyclic peptidomimetics.
AID119197Time of recovery of righting reflux (RRT) in seconds was measured after iv administration of 2.5 mg/kg in mice for the promotional effect on recovery from coma.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel cerebroprotective agents with central nervous system stimulating activity. 2. Synthesis and pharmacology of the 1-(acylamino)-7-hydroxyindan derivatives.
AID1286883Selectivity index, ratio of IC50 for mouse TRH-R1 to IC50 for mouse TRH-R22016European journal of medicinal chemistry, Mar-23, Volume: 111Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues.
AID283908Agonist activity at TRHR2 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Modifications of the pyroglutamic acid and histidine residues in thyrotropin-releasing hormone (TRH) yield analogs with selectivity for TRH receptor type 2 over type 1.
AID119423Antihypoxic effect by the ratio of survival time (SVT) of test mice to that of control group at a dose of 0.3 mg/kg administered intraperitoneally.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel cerebroprotective agents with central nervous system stimulating activity. 2. Synthesis and pharmacology of the 1-(acylamino)-7-hydroxyindan derivatives.
AID189561Agonist activity relative to TRH (Thyroliberin) was evaluated in rat at a dose of 0.6 ng1981Journal of medicinal chemistry, Apr, Volume: 24, Issue:4
Potential thyroliberin affinity labels. 1. Chloroacetyl-substituted phenylalanylpyrrolidines.
AID237121Half-life of compound in rat brain homogenate was determined2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Centrally acting and metabolically stable thyrotropin-releasing hormone analogues by replacement of histidine with substituted pyridinium.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1239068Selectivity index, ratio of EC50 for agonist activity at mouse TRH-R1 expressed in HEK293 cells to EC50 for agonist activity at mouse TRH-R2 expressed in HEK293 cells2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis of CNS active thyrotropin-releasing hormone (TRH)-like peptides: Biological evaluation and effect on cognitive impairment induced by cerebral ischemia in mice.
AID223173Effect on the sleeping time of mice anesthetized with halothane (treated group)2000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
3,4-dihydro-2(1H)-quinolinone as a novel antidepressant drug: synthesis and pharmacology of 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-3,4- dihydro-5-methoxy-2(1H)-quinolinone and its derivatives.
AID1286889Reversal of pentobarbital-induced sleeping time in albino Swiss mouse at 10 umol/kg, iv administered 10 mins prior to pentobarbital injection2016European journal of medicinal chemistry, Mar-23, Volume: 111Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues.
AID119420Compound was tested for the anesthetic effect and the sleeping time (ST) was recorded at a dose of 3 mg/kg administered intraperitoneally.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel cerebroprotective agents with central nervous system stimulating activity. 2. Synthesis and pharmacology of the 1-(acylamino)-7-hydroxyindan derivatives.
AID384275Displacement of [3H]3-methylhistidyl-TRH from rat recombinant TRHR2 expressed in HEK2935 cells2008Journal of natural products, May, Volume: 71, Issue:5
Spongian diterpenes with thyrotropin releasing hormone receptor 2 binding affinity from Spongia sp.
AID237439Calculated partition coefficient (clogP)2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Centrally acting and metabolically stable thyrotropin-releasing hormone analogues by replacement of histidine with substituted pyridinium.
AID118392Activity was evaluated in C57BL/10 mice by Morris water Maze test and mean latency for TRH was reported at 10.0 mg/Kg i.p. dosage.1995Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
Peptide mimetics of thyrotropin-releasing hormone based on a cyclohexane framework: design, synthesis, and cognition-enhancing properties.
AID283907Agonist activity at TRHR1 expressed in HEK293EM cells assessed as activation potency by measuring CREB-luciferase reporter activity2007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Modifications of the pyroglutamic acid and histidine residues in thyrotropin-releasing hormone (TRH) yield analogs with selectivity for TRH receptor type 2 over type 1.
AID299831Apparent permeability across human Caco-2 cells2007Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14
Caco-2 cell permeability and stability of two d-glucopyranuronamide conjugates of thyrotropin-releasing hormone.
AID255368Selectivity for thyrotropin releasing hormone receptor 2 measured as ratio of Ki towards THR-R1 to that of THR-R22005Journal of medicinal chemistry, Sep-22, Volume: 48, Issue:19
Thyrotropin-releasing hormone (TRH) analogues that exhibit selectivity to TRH receptor subtype 2.
AID119410Time of recovery of spontaneous movement (SMT) in seconds was measured after iv administration of 0.625 mg/kg in mice for the promotional effect on recovery from coma.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel cerebroprotective agents with central nervous system stimulating activity. 2. Synthesis and pharmacology of the 1-(acylamino)-7-hydroxyindan derivatives.
AID222711Effect on recovery time for coma induced in mice by cerebral concussion (control group)2000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
3,4-dihydro-2(1H)-quinolinone as a novel antidepressant drug: synthesis and pharmacology of 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-3,4- dihydro-5-methoxy-2(1H)-quinolinone and its derivatives.
AID1239075Plasma concentration in Sprague-Dawley rat assessed as TSH level at 10 umol/kg, iv after 45 mins by ELISA method (Rvb = 5.52 ng/ml)2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis of CNS active thyrotropin-releasing hormone (TRH)-like peptides: Biological evaluation and effect on cognitive impairment induced by cerebral ischemia in mice.
AID1239063Half life in human plasma2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis of CNS active thyrotropin-releasing hormone (TRH)-like peptides: Biological evaluation and effect on cognitive impairment induced by cerebral ischemia in mice.
AID176901Dose that inhibited cataleptic effect of haloperidol in rat by 50%1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Synthesis of thyrotropin-releasing hormone analogues. 2. Tripeptides structurally greatly differing from TRH with high central nervous system activity.
AID222712Effect on recovery time for coma induced in mice by cerebral concussion (treated group)2000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
3,4-dihydro-2(1H)-quinolinone as a novel antidepressant drug: synthesis and pharmacology of 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-3,4- dihydro-5-methoxy-2(1H)-quinolinone and its derivatives.
AID118381Activity was evaluated in C57BL/10 mice by Morris water Maze test and mean latency for TRH was reported at 0.003 mg/Kg i.p. dosage.1995Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
Peptide mimetics of thyrotropin-releasing hormone based on a cyclohexane framework: design, synthesis, and cognition-enhancing properties.
AID237091Half-life of compound in rat plasma was determined2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Centrally acting and metabolically stable thyrotropin-releasing hormone analogues by replacement of histidine with substituted pyridinium.
AID1286885Agonist activity at mouse TRH-R2 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay2016European journal of medicinal chemistry, Mar-23, Volume: 111Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues.
AID1286890Displacement of [3H]-Me-His-TRH from wild type TRHR mouse brain membranes at 10 uM after 4 hrs by scintillation counting method2016European journal of medicinal chemistry, Mar-23, Volume: 111Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues.
AID168135Evaluated for hormonal (TSH) releasing activity in adult male albino rats after single intraperitoneal injection using radioimmunoassay1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Synthesis of thyrotropin-releasing hormone analogues. 1. Complete dissociation of central nervous system effects from thyrotropin-releasing activity.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID229703Evaluated for the potency ratio from the dose-response curve of TRH and compound by the parallel line assay method.1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Synthesis and central nervous system actions of thyrotropin-releasing hormone analogues containing a dihydroorotic acid moiety.
AID119429Antihypoxic effect tested by the ratio of survival time (SVT) of test mice to that of control group, dosed intraperitoneally at 30 mg/kg1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel cerebroprotective agents with central nervous system stimulating activity. 2. Synthesis and pharmacology of the 1-(acylamino)-7-hydroxyindan derivatives.
AID237437Calculated partition coefficient (clogP)2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Centrally acting and metabolically stable thyrotropin-releasing hormone analogues by replacement of histidine with substituted pyridinium.
AID385236Displacement of [3H]3-methylhistidyl-TRH from rat recombinant TRH2 receptor expressed in HEK2935 cells2008Journal of natural products, May, Volume: 71, Issue:5
Corymbones A and B, phloroglucinols with thyrotropin releasing hormone receptor 2 binding affinity from the flowers of Corymbia peltata.
AID1239066Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis of CNS active thyrotropin-releasing hormone (TRH)-like peptides: Biological evaluation and effect on cognitive impairment induced by cerebral ischemia in mice.
AID223176Effect on the sleeping time of mice before halothane load (control group)2000Journal of medicinal chemistry, Jan-27, Volume: 43, Issue:2
3,4-dihydro-2(1H)-quinolinone as a novel antidepressant drug: synthesis and pharmacology of 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-3,4- dihydro-5-methoxy-2(1H)-quinolinone and its derivatives.
AID118391Activity was evaluated in C57BL/10 mice by Morris water Maze test and mean latency for TRH was reported at 1.0 mg/Kg i.p. dosage.1995Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
Peptide mimetics of thyrotropin-releasing hormone based on a cyclohexane framework: design, synthesis, and cognition-enhancing properties.
AID119414Compound was tested for the anesthetic effect and the sleeping time (ST) was recorded at a dose of 0.3 mg/kg administered intraperitoneally.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel cerebroprotective agents with central nervous system stimulating activity. 2. Synthesis and pharmacology of the 1-(acylamino)-7-hydroxyindan derivatives.
AID299832Stability in Caco-2 cells after 20 mins2007Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14
Caco-2 cell permeability and stability of two d-glucopyranuronamide conjugates of thyrotropin-releasing hormone.
AID119427Antihypoxic effect by the ratio of survival time (SVT) of test mice to that of control group at a dose of 1 mg/kg administered intraperitoneally.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel cerebroprotective agents with central nervous system stimulating activity. 2. Synthesis and pharmacology of the 1-(acylamino)-7-hydroxyindan derivatives.
AID119565Antihypoxic effect by the survival time (SVT) in mice at a dose of 3 mg/kg administered intravenously in mice1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel cerebroprotective agents with central nervous system stimulating activity. 1. Synthesis and pharmacology of 1-amino-7-hydroxyindan derivatives.
AID252567Sleeping time of mice was determined after intravenous administration of compound at 15 umol/kg of Body Weight2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Centrally acting and metabolically stable thyrotropin-releasing hormone analogues by replacement of histidine with substituted pyridinium.
AID119184Time of recovery of righting reflux (RRT) in seconds was measured after administration of 2.5 mg/kg intravenously in mice for the promotional effect on recovery from coma1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel cerebroprotective agents with central nervous system stimulating activity. 1. Synthesis and pharmacology of 1-amino-7-hydroxyindan derivatives.
AID118387Activity was evaluated in C57BL/10 mice by Morris water Maze test and mean latency for TRH was reported at 0.1 mg/Kg i.p. dosage.1995Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
Peptide mimetics of thyrotropin-releasing hormone based on a cyclohexane framework: design, synthesis, and cognition-enhancing properties.
AID239477Inhibition of [3H][3-Me-His2]-TRH binding to thyrotropin releasing hormone receptor of rat forebrain2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Centrally acting and metabolically stable thyrotropin-releasing hormone analogues by replacement of histidine with substituted pyridinium.
AID1286882Displacement of [3H]-Me-His-TRH from mouse TRH-R2 expressed in HEK293 cells preincubated for 15 mins measured after 4 hrs2016European journal of medicinal chemistry, Mar-23, Volume: 111Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues.
AID1239067Agonist activity at mouse TRH-R2 expressed in HEK293 cells assessed as induction of changes in intracellular Ca2+ level by FLIPR method2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis of CNS active thyrotropin-releasing hormone (TRH)-like peptides: Biological evaluation and effect on cognitive impairment induced by cerebral ischemia in mice.
AID178275Anticataleptic effect at effective dose after intravenous administration in adult male Wistar rats.1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Synthesis of thyrotropin-releasing hormone analogues. 1. Complete dissociation of central nervous system effects from thyrotropin-releasing activity.
AID119401Time of recovery of spontaneous movement (SMT) in seconds was measured after administration of 2.5 mg/kg intravenously in mice for the promotional effect on recovery from coma1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel cerebroprotective agents with central nervous system stimulating activity. 1. Synthesis and pharmacology of 1-amino-7-hydroxyindan derivatives.
AID283906Displacement of [3H]N(1)-Me-His-TRH from TRHR22007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Modifications of the pyroglutamic acid and histidine residues in thyrotropin-releasing hormone (TRH) yield analogs with selectivity for TRH receptor type 2 over type 1.
AID210544Binding affinity against TRH-R receptor in AtT-20 mouse pituitary tumor cells1996Journal of medicinal chemistry, Apr-12, Volume: 39, Issue:8
Conformationally restricted TRH analogs: a probe for the pyroglutamate region.
AID1286893Displacement of [3H]-Me-His-TRH from wild type TRHR mouse brain membranes at 0.01 uM after 4 hrs by scintillation counting method2016European journal of medicinal chemistry, Mar-23, Volume: 111Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues.
AID118380Activity was evaluated in C57BL/10 mice by Morris water Maze test and mean latency for TRH was reported at 0.001 mg/Kg i.p. dosage.1995Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
Peptide mimetics of thyrotropin-releasing hormone based on a cyclohexane framework: design, synthesis, and cognition-enhancing properties.
AID1239065Displacement of [3H]-1-MeHis-TRH from mouse TRH-R2 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis of CNS active thyrotropin-releasing hormone (TRH)-like peptides: Biological evaluation and effect on cognitive impairment induced by cerebral ischemia in mice.
AID1286892Displacement of [3H]-Me-His-TRH from wild type TRHR mouse brain membranes at 0.1 uM after 4 hrs by scintillation counting method2016European journal of medicinal chemistry, Mar-23, Volume: 111Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues.
AID183241Inhibition of haloperidol catalepsy by less than 50% in a dose of 80 mg/kg, iv in adult male Wistar rats1984Journal of medicinal chemistry, Jun, Volume: 27, Issue:6
Synthesis of thyrotropin-releasing hormone analogues. 1. Complete dissociation of central nervous system effects from thyrotropin-releasing activity.
AID1239069Reduction in pentobarbital-induced sleeping time in Swiss mouse at 10 umol/kg, iv2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis of CNS active thyrotropin-releasing hormone (TRH)-like peptides: Biological evaluation and effect on cognitive impairment induced by cerebral ischemia in mice.
AID1239076Stability assessed as mouse recombinant TRH-degrading ectoenzyme-mediated compound degradation at 1 mM measured within 18 hrs by HPLC method2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis of CNS active thyrotropin-releasing hormone (TRH)-like peptides: Biological evaluation and effect on cognitive impairment induced by cerebral ischemia in mice.
AID171620Thyrotropin releasing activity (TSH) was evaluated by measuring the TSH response to the compound by radioimmunoassay in two doses in the rat1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Synthesis of thyrotropin-releasing hormone analogues. 2. Tripeptides structurally greatly differing from TRH with high central nervous system activity.
AID237435Partition coefficient (logP)2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Centrally acting and metabolically stable thyrotropin-releasing hormone analogues by replacement of histidine with substituted pyridinium.
AID119417Compound was tested for the anesthetic effect and the sleeping time (ST) was recorded at a dose of 1 mg/kg administered intraperitoneally.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel cerebroprotective agents with central nervous system stimulating activity. 2. Synthesis and pharmacology of the 1-(acylamino)-7-hydroxyindan derivatives.
AID252621Maximal changes in rat hippocampal acetylcholine concentration after administration of compound through a microdialysis probe2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Centrally acting and metabolically stable thyrotropin-releasing hormone analogues by replacement of histidine with substituted pyridinium.
AID1239064Displacement of [3H]-1-MeHis-TRH from mouse TRH-R1 expressed in HEK293 cells incubated up to 4 hrs by scintillation counting method2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis of CNS active thyrotropin-releasing hormone (TRH)-like peptides: Biological evaluation and effect on cognitive impairment induced by cerebral ischemia in mice.
AID1286880Selectivity ratio of EC50 for mouse TRH-R1 to EC50 for mouse TRH-R2 by ELISA2016European journal of medicinal chemistry, Mar-23, Volume: 111Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues.
AID118395Activity was evaluated in C57BL/10 mice by Morris water Maze test and mean latency for TRH was reported at 3.0 mg/Kg i.p. dosage.1995Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
Peptide mimetics of thyrotropin-releasing hormone based on a cyclohexane framework: design, synthesis, and cognition-enhancing properties.
AID1286884Agonist activity at mouse TRH-R1 expressed in HEK293 cells assessed as Ca2+ release by FLIPR assay2016European journal of medicinal chemistry, Mar-23, Volume: 111Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues.
AID119411Time of recovery of spontaneous movement (SMT) in seconds was measured after iv administration of 1.25 mg/kg in mice for the promotional effect on recovery from coma.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel cerebroprotective agents with central nervous system stimulating activity. 2. Synthesis and pharmacology of the 1-(acylamino)-7-hydroxyindan derivatives.
AID254657Signaling (activation) potency for thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells with CREB-luciferase reporter upon incubation with the compound for 6 hr at 37 degree C and pH 7.8; Range = 0.002-0.004 uM2005Journal of medicinal chemistry, Sep-22, Volume: 48, Issue:19
Thyrotropin-releasing hormone (TRH) analogues that exhibit selectivity to TRH receptor subtype 2.
AID1286886Selectivity ratio of EC50 for mouse TRH-R1 to EC50 for mouse TRH-R2 by FLIPR assay2016European journal of medicinal chemistry, Mar-23, Volume: 111Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues.
AID283905Displacement of [3H]N(1)-Me-His-TRH from TRHR12007Bioorganic & medicinal chemistry, Jan-01, Volume: 15, Issue:1
Modifications of the pyroglutamic acid and histidine residues in thyrotropin-releasing hormone (TRH) yield analogs with selectivity for TRH receptor type 2 over type 1.
AID119555Antihypoxic effect by the survival time (SVT) in mice at a dose of 100 mg/kg administered orally in mice; NT indicates not tested1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel cerebroprotective agents with central nervous system stimulating activity. 1. Synthesis and pharmacology of 1-amino-7-hydroxyindan derivatives.
AID299834Stability in Caco-2 cells assessed as half life2007Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14
Caco-2 cell permeability and stability of two d-glucopyranuronamide conjugates of thyrotropin-releasing hormone.
AID1286888Agonist activity at mouse TRH-R2 expressed in HEK293 cells assessed as IP1 formation after 1 hr by ELISA2016European journal of medicinal chemistry, Mar-23, Volume: 111Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues.
AID237548Capacity factor of compound was determined by immobilized artificial membrane chromatography2004Journal of medicinal chemistry, Nov-18, Volume: 47, Issue:24
Centrally acting and metabolically stable thyrotropin-releasing hormone analogues by replacement of histidine with substituted pyridinium.
AID119432Antihypoxic effect by the ratio of survival time (SVT) of test mice to that of control group at a dose of 3 mg/kg administered intraperitoneally.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel cerebroprotective agents with central nervous system stimulating activity. 2. Synthesis and pharmacology of the 1-(acylamino)-7-hydroxyindan derivatives.
AID1286906Stability of the compound assessed as recombinant mouse TRH-DE-mediated hydrolysis at 1 mM at 18 hrs by HPLC analysis2016European journal of medicinal chemistry, Mar-23, Volume: 111Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues.
AID1286891Displacement of [3H]-Me-His-TRH from wild type TRHR mouse brain membranes at 1 uM after 4 hrs by scintillation counting method2016European journal of medicinal chemistry, Mar-23, Volume: 111Synthesis and biology of ring-modified l-Histidine containing thyrotropin-releasing hormone (TRH) analogues.
AID190955The thyrotropin (TSH) releasing activity was measured as serum TSH at 0.5 ug/rat dose (i.v.)1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Synthesis and central nervous system actions of thyrotropin-releasing hormone analogues containing a dihydroorotic acid moiety.
AID254556Inhibitory constant against thyrotropin releasing hormone receptor 1 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH; Range = 0.001-0.003 uM2005Journal of medicinal chemistry, Sep-22, Volume: 48, Issue:19
Thyrotropin-releasing hormone (TRH) analogues that exhibit selectivity to TRH receptor subtype 2.
AID119196Time of recovery of righting reflux (RRT) in seconds was measured after iv administration of 1.25 mg/kg in mice for the promotional effect on recovery from coma.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel cerebroprotective agents with central nervous system stimulating activity. 2. Synthesis and pharmacology of the 1-(acylamino)-7-hydroxyindan derivatives.
AID119739Reduction of hexobarbital induced sleeping time in mice.1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Synthesis of thyrotropin-releasing hormone analogues. 2. Tripeptides structurally greatly differing from TRH with high central nervous system activity.
AID213190Ability to activate thyroliberin endocrine receptor (TRH-R) using AtT-20 mouse pituitary tumor cells prelabelled with myo-[3H] inositol1998Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21
Thyrotropin releasing hormone analogs: a building block approach to the construction of tetracyclic peptidomimetics.
AID118383Activity was evaluated in C57BL/10 mice by Morris water Maze test and mean latency for TRH was reported at 0.01 mg/Kg i.p. dosage.1995Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
Peptide mimetics of thyrotropin-releasing hormone based on a cyclohexane framework: design, synthesis, and cognition-enhancing properties.
AID190954The thyrotropin (TSH) releasing activity was measured as serum TSH at 0.125 ug/rat dose (i.v.)1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Synthesis and central nervous system actions of thyrotropin-releasing hormone analogues containing a dihydroorotic acid moiety.
AID119195Time of recovery of righting reflux (RRT) in seconds was measured after iv administration of 0.625 mg/kg in mice for the promotional effect on recovery from coma.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel cerebroprotective agents with central nervous system stimulating activity. 2. Synthesis and pharmacology of the 1-(acylamino)-7-hydroxyindan derivatives.
AID182521Ability of 80 mg/kg to inhibit the cataleptic effect of haloperidol in rat1986Journal of medicinal chemistry, Sep, Volume: 29, Issue:9
Synthesis of thyrotropin-releasing hormone analogues. 2. Tripeptides structurally greatly differing from TRH with high central nervous system activity.
AID119412Time of recovery of spontaneous movement (SMT) in seconds was measured after iv administration of 2.5 mg/kg in mice for the promotional effect on recovery from coma.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Novel cerebroprotective agents with central nervous system stimulating activity. 2. Synthesis and pharmacology of the 1-(acylamino)-7-hydroxyindan derivatives.
AID190956The thyrotropin (TSH) releasing activity was measured as serum TSH at 0.03125 ug/rat dose (i.v.)1990Journal of medicinal chemistry, Aug, Volume: 33, Issue:8
Synthesis and central nervous system actions of thyrotropin-releasing hormone analogues containing a dihydroorotic acid moiety.
AID213192Effective concentration required to activate TRH-R receptor in AtT-20 mouse pituitary tumor cells1996Journal of medicinal chemistry, Apr-12, Volume: 39, Issue:8
Conformationally restricted TRH analogs: a probe for the pyroglutamate region.
AID118389Activity was evaluated in C57BL/10 mice by Morris water Maze test and mean latency for TRH was reported at 0.3 mg/Kg i.p. dosage.1995Journal of medicinal chemistry, Jul-21, Volume: 38, Issue:15
Peptide mimetics of thyrotropin-releasing hormone based on a cyclohexane framework: design, synthesis, and cognition-enhancing properties.
AID254533Inhibitory constant against thyrotropin releasing hormone receptor 2 expressed in HEK 293EM cells upon incubation at 37 degree C for 1 hr at pH 7.4 using [3H]Ntau(1)-Me-His-TRH2005Journal of medicinal chemistry, Sep-22, Volume: 48, Issue:19
Thyrotropin-releasing hormone (TRH) analogues that exhibit selectivity to TRH receptor subtype 2.
AID1239074Plasma concentration in Sprague-Dawley rat assessed as TSH level at 10 umol/kg, iv after 30 mins by ELISA method (Rvb = 5.52 ng/ml)2015Bioorganic & medicinal chemistry, Sep-01, Volume: 23, Issue:17
Synthesis of CNS active thyrotropin-releasing hormone (TRH)-like peptides: Biological evaluation and effect on cognitive impairment induced by cerebral ischemia in mice.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346296Rat TRH1 receptor (Thyrotropin-releasing hormone receptors)1996Physiological reviews, Jan, Volume: 76, Issue:1
Molecular and cellular biology of thyrotropin-releasing hormone receptors.
AID1346810Rat TRH2 receptor (Thyrotropin-releasing hormone receptors)1996Physiological reviews, Jan, Volume: 76, Issue:1
Molecular and cellular biology of thyrotropin-releasing hormone receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (26)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905 (19.23)18.7374
1990's8 (30.77)18.2507
2000's7 (26.92)29.6817
2010's5 (19.23)24.3611
2020's1 (3.85)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 89.72

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index89.72 (24.57)
Research Supply Index3.33 (2.92)
Research Growth Index4.58 (4.65)
Search Engine Demand Index154.90 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (89.72)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (7.41%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other25 (92.59%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (6)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Pilot, Randomized Double-Blind Placebo-Controlled Crossover Study of Synthetic Thyrotropin Releasing Hormone (TRH) Administration for the Treatment of Fatigue in Patients With Cancer [NCT00790296]Phase 211 participants (Actual)Interventional2006-12-31Terminated(stopped due to Interim analyses showed statistically and clinically significant results.)
Evaluation of The Development of Central Resistance to Thyroid Hormone After Prolonged Exposure to Excess Thyroid Hormone in Thyroid Cancer Patients [NCT04868045]Phase 10 participants (Actual)Interventional2021-04-27Withdrawn(stopped due to Lack of accrual)
[NCT00004840]996 participants Interventional1998-05-31Completed
The Thyroid Axis in Older Individuals With Persistent Subclinical Hypothyroidism: a Mechanistic, Randomized, Double-Blind, Cross-Over Study of Levothyroxine and Liothyronine Administration [NCT02399475]14 participants (Actual)Interventional2015-01-01Completed
Study of Thyrotropin Releasing Hormone in Patients With Thyroid or Pituitary Abnormalities [NCT00054756]Phase 296 participants (Actual)Interventional2003-02-07Completed
[NCT00004778]Phase 31,090 participants Interventional1993-08-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00054756 (1) [back to overview]TSH Response to TRH
NCT00790296 (1) [back to overview]Change in Visual Analog Scale for Energy (VAS-E)Score From Baseline to 7 Hrs Post Study Medication Infusion
NCT02399475 (4) [back to overview]Free T4 Level
NCT02399475 (4) [back to overview]Total T3 Level
NCT02399475 (4) [back to overview]TSH Area Under the Curve
NCT02399475 (4) [back to overview]TSH Max

TSH Response to TRH

Serum TSH Levels in Response to TRH Administration (NCT00054756)
Timeframe: 180 minutes from infusion

InterventionmcIU/mL (Mean)
Thyrotropin Releasing Hormone11.47

[back to top]

Change in Visual Analog Scale for Energy (VAS-E)Score From Baseline to 7 Hrs Post Study Medication Infusion

1 to 100 scale with 1 referring to No Energy and 100 referring to Normal Energy. (NCT00790296)
Timeframe: Baseline and 7 hours post study medication infusion

InterventionScores on a scale (Mean)
Thyrotropin-releasing Hormone (TRH)14.67
Saline-1.67

[back to top]

Free T4 Level

Free thyroxine level when TSH level is at goal on therapy. (NCT02399475)
Timeframe: An average of 7 months after initiating therapy

Interventionng/dL (Mean)
Levothyroxine1.65
Liothyronine0.46

[back to top]

Total T3 Level

Total triiodothyronine level when TSH is at goal on therapy (NCT02399475)
Timeframe: An average of 7 months

Interventionng/mL (Mean)
Levothyroxine1.12
Liothyronine1.98

[back to top]

TSH Area Under the Curve

TSH area under the curve within 60 minutes of TRH stimulation when TSH is at goal (NCT02399475)
Timeframe: 0, 5, 10, 15, 20, 30, and 60 min post TRH

InterventionμIU*min/mL (Mean)
Levothyroxine267.8
Liothyronine266.2

[back to top]

TSH Max

The maximum concentration of TSH after TRH stimulation when TSH is at goal (NCT02399475)
Timeframe: Between 0 and 180 min after TRH stimulation

InterventionmIU/L (Mean)
Levothyroxine5.5
Liothyronine5.4

[back to top]