posatirelin

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

Description

posatirelin: stimulates oxygen consumption [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	71230
CHEMBL ID	2105243
CHEBI ID	135486
SCHEMBL ID	195247
MeSH ID	M0156099

Synonyms (32)

Synonym
rgh-2202
paad-leu-pro-nh2
pyladox
posatirelin
posatirelinum [inn-latin]
(-)-(2s)-n-(1s)-1-((2s)-2-carbamoyl-1-pyrrolidinyl)carbonyl-3-(methylbutyl)-6-oxopipecolamide
posatirelina [inn-spanish]
l-pyro-2-aminoadipyl-l-leucyl-l-prolinamide
brn 6006446
(2s)-n((1s)-1-(((2s)-2-carbamoyl-1-pyrrolidinyl)carbonyl)-3-methylbutyl)-6-oxopipecolamide
posatireline [inn-french]
l-6-ketopiperidine-2-carbonyl-leucyl-l-prolin-amide
posatirelin [inn]
(s)-l-leucyl-n-((6-oxo-2-piperidinyl)carbonyl)-l-prolinamide
l-prolinamide, n-((6-oxo-2-piperidinyl)carbonyl)-l-leucyl-, (s)-
(2s)-n-[(2s)-1-[(2s)-2-carbamoylpyrrolidin-1-yl]-4-methyl-1-oxopentan-2-yl]-6-oxopiperidine-2-carboxamide
78664-73-0
posatireline
CHEMBL2105243
78u6302arl ,
posatirelinum
unii-78u6302arl
posatirelina
posatirelin [mi]
posatirelin [jan]
posatirelin [mart.]
SCHEMBL195247
CHEBI:135486
(s)-n-((s)-1-((s)-2-carbamoylpyrrolidin-1-yl)-4-methyl-1-oxopentan-2-yl)-6-oxopiperidine-2-carboxamide
Q27266691
DTXSID301318172
AKOS040753598

Research Excerpts

Treatment

Treatment with posatirelin was without effect on the number of nerve cell profiles or of GFAP-immunoreactive astrocytes both at 4 and 8 weeks after LC lesioning.

Excerpt	Reference	Relevance
"Treatment with posatirelin was without effect on the number of nerve cell profiles or of GFAP-immunoreactive astrocytes both at 4 and 8 weeks after NBM lesioning."	( Effect of the thyrotropin releasing hormone analogue posatirelin (RGH 2202) on microanatomical changes induced by lesions of the nucleus basalis magnocellularis in the rat. Amenta, F; Coppi, G; Maggioni, A; Olgiati, V; Panocka, I; Sabbatini, M, 1997)	0.89
"Treatment with posatirelin was without effect on the number of nerve cell and of GFAP-immunoreactive astrocyte profiles at both 4 and 8 weeks after LC lesioning, with the exception of nerve cells of the frontal cortex in monolaterally-lesioned rats which were increased 8 weeks after lesioning."	( Effect of treatment with the neuroactive peptide posatirelin on microanatomical changes of frontal cortex and hippocampus caused by lesions of the locus coeruleus. Amenta, F; Coppi, G; Maggioni, A; Olgiati, V; Panocka, I; Sabbatini, M, 1997)	0.89

Pharmacokinetics

Excerpt	Reference	Relevance
" Pharmacokinetic parameters were estimated using a model-independent approach."	( Pharmacokinetic profile and endocrine effects of posatirelin treatment in healthy elderly subjects. Ambrosoli, L; Cherubini, A; Girardello, R; Lowenthal, DT; Palumbo, B; Parnetti, L; Poli, A; Reboldi, G; Santeusanio, F; Senin, U, 1996)	0.55

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

Class	Description
oligopeptide	A peptide containing a relatively small number of amino acids.
[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]

Bioassays (3)

Assay ID	Title	Year	Journal	Article
AID119739	Reduction of hexobarbital induced sleeping time in mice.	1986	Journal 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.
AID176950	Doses that inhibited cataleptic effect of haloperidol in rat by 50%	1986	Journal 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.
AID171620	Thyrotropin releasing activity (TSH) was evaluated by measuring the TSH response to the compound by radioimmunoassay in two doses in the rat	1986	Journal 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (23)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	5 (21.74)	18.7374
1990's	14 (60.87)	18.2507
2000's	4 (17.39)	29.6817
2010's	0 (0.00)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.05

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 weak demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	11.05 (24.57)
Research Supply Index	3.50 (2.92)
Research Growth Index	4.55 (4.65)
Search Engine Demand Index	0.00 (26.88)
Search Engine Supply Index	0.00 (0.95)

This Compound (11.05)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	2 (6.67%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	28 (93.33%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid: An IBOTENIC ACID homolog and glutamate agonist. The compound is the defining agonist for the AMPA subtype of glutamate receptors (RECEPTORS, AMPA). It has been used as a radionuclide imaging agent but is more commonly used as an experimental tool in cell biological studies.	2.05	1	0	non-proteinogenic alpha-amino acid
fentanyl Fentanyl: A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078). fentanyl : A monocarboxylic acid amide resulting from the formal condensation of the aryl amino group of N-phenyl-1-(2-phenylethyl)piperidin-4-amine with propanoic acid.	1.97	1	0	anilide; monocarboxylic acid amide; piperidines	adjuvant; anaesthesia adjuvant; anaesthetic; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic
aspartic acid Aspartic Acid: One of the non-essential amino acids commonly occurring in the L-form. It is found in animals and plants, especially in sugar cane and sugar beets. It may be a neurotransmitter.. aspartic acid : An alpha-amino acid that consists of succinic acid bearing a single alpha-amino substituent. L-aspartic acid : The L-enantiomer of aspartic acid.	1.98	1	0	aspartate family amino acid; aspartic acid; L-alpha-amino acid; proteinogenic amino acid	Escherichia coli metabolite; mouse metabolite; neurotransmitter
pyrrolidonecarboxylic acid Pyrrolidonecarboxylic Acid: A cyclized derivative of L-GLUTAMIC ACID. Elevated blood levels may be associated with problems of GLUTAMINE or GLUTATHIONE metabolism.. 5-oxo-L-proline : An optically active form of 5-oxoproline having L-configuration.	1.97	1	0	5-oxoproline; L-proline derivative; non-proteinogenic L-alpha-amino acid	algal metabolite
kainic acid Kainic Acid: (2S-(2 alpha,3 beta,4 beta))-2-Carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid. Ascaricide obtained from the red alga Digenea simplex. It is a potent excitatory amino acid agonist at some types of excitatory amino acid receptors and has been used to discriminate among receptor types. Like many excitatory amino acid agonists it can cause neurotoxicity and has been used experimentally for that purpose.	2.43	2	0	dicarboxylic acid; L-proline derivative; non-proteinogenic L-alpha-amino acid; pyrrolidinecarboxylic acid	antinematodal drug; excitatory amino acid agonist
cytidine diphosphate choline Cytidine Diphosphate Choline: Donor of choline in biosynthesis of choline-containing phosphoglycerides.	3.37	1	1	nucleotide-(amino alcohol)s; phosphocholines	human metabolite; mouse metabolite; neuroprotective agent; psychotropic drug; Saccharomyces cerevisiae metabolite
n-methylaspartate N-Methylaspartate: An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).. N-methyl-D-aspartic acid : An aspartic acid derivative having an N-methyl substituent and D-configuration.	2.41	2	0	amino dicarboxylic acid; D-alpha-amino acid; D-aspartic acid derivative; secondary amino compound	neurotransmitter agent
silver Silver: An element with the atomic symbol Ag, atomic number 47, and atomic weight 107.87. It is a soft metal that is used medically in surgical instruments, dental prostheses, and alloys. Long-continued use of silver salts can lead to a form of poisoning known as ARGYRIA.	1.99	1	0	copper group element atom; elemental silver	Escherichia coli metabolite
gold Gold: A yellow metallic element with the atomic symbol Au, atomic number 79, and atomic weight 197. It is used in jewelry, goldplating of other metals, as currency, and in dental restoration. Many of its clinical applications, such as ANTIRHEUMATIC AGENTS, are in the form of its salts.	1.99	1	0	copper group element atom; elemental gold
quisqualic acid Quisqualic Acid: An agonist at two subsets of excitatory amino acid receptors, ionotropic receptors that directly control membrane channels and metabotropic receptors that indirectly mediate calcium mobilization from intracellular stores. The compound is obtained from the seeds and fruit of Quisqualis chinensis.	2.05	1	0	non-proteinogenic alpha-amino acid
orotirelin orotirelin: increases dopamine release from rat brain	1.97	1	0
l-pyroglutamyl-l-histidyl-3,3-dimethylprolinamide [no description available]	1.97	1	0
dn 1417 DN 1417: RN given refers to parent cpd	1.97	1	0
thyrotropin-releasing hormone PR 546: no other info available 9/89. protirelin : A tripeptide composed of L-pyroglutamyl, L-histidyl and L-prolinamide residues joined in sequence.	1.96	1	0	peptide hormone; tripeptide	human metabolite
naloxone Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose.	1.98	1	0	morphinane alkaloid; organic heteropentacyclic compound; tertiary alcohol	antidote to opioid poisoning; central nervous system depressant; mu-opioid receptor antagonist
morphine Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn.	2.38	2	0	morphinane alkaloid; organic heteropentacyclic compound; tertiary amino compound	anaesthetic; drug allergen; environmental contaminant; geroprotector; mu-opioid receptor agonist; opioid analgesic; plant metabolite; vasodilator agent; xenobiotic
montirelin montirelin: structure given in first source	2.05	1	0	oligopeptide
staurosporine staurosporinium : Conjugate acid of staurosporine.	2.05	1	0	ammonium ion derivative
ascorbic acid Ascorbic Acid: A six carbon compound related to glucose. It is found naturally in citrus fruits and many vegetables. Ascorbic acid is an essential nutrient in human diets, and necessary to maintain connective tissue and bone. Its biologically active form, vitamin C, functions as a reducing agent and coenzyme in several metabolic pathways. Vitamin C is considered an antioxidant.. L-ascorbic acid : The L-enantiomer of ascorbic acid and conjugate acid of L-ascorbate.. L-ascorbate : The L-enantiomer of ascorbate and conjugate base of L-ascorbic acid, arising from selective deprotonation of the 3-hydroxy group. Required for a range of essential metabolic reactions in all animals and plants.. vitamin C : Any member of a group of vitamers that belong to the chemical structural class called butenolides that exhibit biological activity against vitamin C deficiency in animals. The vitamers include L-ascorbic acid and its salt, ionized and oxidized forms.	8.37	1	1	ascorbic acid; vitamin C	coenzyme; cofactor; flour treatment agent; food antioxidant; food colour retention agent; geroprotector; plant metabolite; skin lightening agent

Condition	Relationship Strength	Studies	Trials
Anochlesia [description not available]	1.96	1	0
Necrosis The death of cells in an organ or tissue due to disease, injury or failure of the blood supply.	2.05	1	0
Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.	2.05	1	0
Acute Brain Injuries [description not available]	2.01	1	0
Brain Injuries Acute and chronic (see also BRAIN INJURIES, CHRONIC) injuries to the brain, including the cerebral hemispheres, CEREBELLUM, and BRAIN STEM. Clinical manifestations depend on the nature of injury. Diffuse trauma to the brain is frequently associated with DIFFUSE AXONAL INJURY or COMA, POST-TRAUMATIC. Localized injuries may be associated with NEUROBEHAVIORAL MANIFESTATIONS; HEMIPARESIS, or other focal neurologic deficits.	2.01	1	0
Acute Confusional Senile Dementia [description not available]	3.37	1	1
Alzheimer Disease A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)	3.37	1	1
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	2.38	2	0
Cerebral Ischemia [description not available]	1.98	1	0
Brain Ischemia Localized reduction of blood flow to brain tissue due to arterial obstruction or systemic hypoperfusion. This frequently occurs in conjunction with brain hypoxia (HYPOXIA, BRAIN). Prolonged ischemia is associated with BRAIN INFARCTION.	1.98	1	0
Anoxia, Brain [description not available]	2.4	2	0
Acute Onset Vascular Dementia [description not available]	3.37	1	1
Dementia, Vascular An imprecise term referring to dementia associated with CEREBROVASCULAR DISORDERS, including CEREBRAL INFARCTION (single or multiple), and conditions associated with chronic BRAIN ISCHEMIA. Diffuse, cortical, and subcortical subtypes have been described. (From Gerontol Geriatr 1998 Feb;31(1):36-44)	3.37	1	1
Absence Seizure [description not available]	2	1	0
Seizures Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.	2	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2	1	0
Anoxemia [description not available]	1.97	1	0
Hypoxia Sub-optimal OXYGEN levels in the ambient air of living organisms.	1.97	1	0
Vascular Diseases Pathological processes involving any of the BLOOD VESSELS in the cardiac or peripheral circulation. They include diseases of ARTERIES; VEINS; and rest of the vasculature system in the body.	1.97	1	0
Hemorrhagic Shock [description not available]	1.97	1	0
Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	1.97	1	0
Craniocerebral Injuries [description not available]	1.97	1	0
Craniocerebral Trauma Traumatic injuries involving the cranium and intracranial structures (i.e., BRAIN; CRANIAL NERVES; MENINGES; and other structures). Injuries may be classified by whether or not the skull is penetrated (i.e., penetrating vs. nonpenetrating) or whether there is an associated hemorrhage.	1.97	1	0

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