Page last updated: 2024-11-12

astressin

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

Description

astressin : A 30-membered homodetic cyclic peptide comprising the sequence D-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Nle-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-Glu-Ala-His-Lys-Asn-Arg-Lys-Leu-Nle-Glu-Ile-Ile-NH2 cyclised by an amide bridge, formed by condensation of the side-chain carboxy group of the Glu residue at position 19 and the side-chain amino group of the Lys residue at position 22. [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 CID16133798
CHEBI ID76649
MeSH IDM0272750

Synonyms (10)

Synonym
gtpl925
astressin
170809-51-5
d-phe-his-leu-leu-arg-glu-val-leu-glu-nle-ala-arg-ala-glu-gln-leu-ala-gln-cyclo-(glu-ala-his-lys)-asn-arg-lys-leu-nle-glu-ile-ile-nh2
[d-phe(12), nle(21,38), glu(30), lys(33)]-crf (12-41)
fhllrevle-nle-araeqlaq-cyclo-(eahk)nrkl-nle-eii-nh2
CHEBI:76649
AKOS024456701
[d-phe12, nle21,38, glu30, lys33]-crf (12-41)
l-isoleucinamide,d-phenylalanyl-l-histidyl-l-leucyl-l-leucyl-l-arginyl-l-a-glutamyl-l-valyl-l-leucyl-l-a-glutamyl-l-norleucyl-l-alanyl-l-arginyl-l-alanyl-l-a-glutamyl-l-glutaminyl-l-leucyl-l-alanyl-l-

Research Excerpts

Overview

Astressin is an amino-terminal truncated analog of CRF that retains high affinity binding to the extracellular domain of the receptor. It is believed to act as a neutral competitive antagonist of receptor activation.

ExcerptReferenceRelevance
"Astressin is an amino-terminal truncated analog of CRF that retains high affinity binding to the extracellular domain of the receptor and is believed to act as a neutral competitive antagonist of receptor activation."( Distinct conformations of the corticotropin releasing factor type 1 receptor adopted following agonist and antagonist binding are differentially regulated.
Grigoriadis, DE; Hoare, SR; Junger, S; Kohout, TA; Maki, RA; Perry, SJ; Struthers, RS, 2005
)
1.05

Treatment

Pretreatment with astressin, VIP antagonist, atropine, L-NAME, and ODQ prevented the increase in gastric retention caused by exercise in rats. Astressin-treated animals showed a near complete developmental arrest, which confirmed that development requires CRF.

ExcerptReferenceRelevance
"Astressin-treated animals showed a near complete developmental arrest, which confirmed that development requires CRF."( Corticotropin-releasing factor regulates the development in the direct developing frog, Eleutherodactylus coqui.
Buchholz, DR; Kulkarni, SS; Singamsetty, S, 2010
)
1.08
"Astressin treatment also induced sexual receptivity in nonresponders, animals that do not normally come into heat when treated with hormones, and this effect persisted in subsequent weekly tests in the absence of any further astressin treatment."( Disinhibition of female sexual behavior by a CRH receptor antagonist in Syrian hamsters.
Corp, ES; Davenport, MD; Jones, JE; Keene, AC; Pick, RR; Wade, GN, 2002
)
1.04
"Pretreatment with astressin, VIP antagonist, atropine, L-NAME, and ODQ prevented the increase in gastric retention caused by exercise in rats."( Acute exercise inhibits gastric emptying of liquids in rats: influence of the NO-cGMP pathway.
Cavalcante, AKM; de Andrade, CR; Feitosa JĂșnior, VN; Santos, AA; Silva, MTB; Siqueira, RCL, 2018
)
0.8
"Pretreatment with astressin tended to decrease plasma cortisol levels."( Role of corticotrophin-releasing factor in the stress-induced dilation of esophageal intercellular spaces.
Cho, YJ; Im, SK; Kim, JH; Lee, DM; Lee, KJ; Yim, HE, 2011
)
0.69

Dosage Studied

ExcerptRelevanceReference
" Dose-response curves were constructed for the chorion cell cultures with CRH or 8-bromo-cAMP."( Regulation of 15-hydroxy prostaglandin dehydrogenase by corticotrophin-releasing hormone through a calcium-dependent pathway in human chorion trophoblast cells.
Challis, JR; McKeown, KJ, 2003
)
0.32
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (2)

RoleDescription
corticotropin-releasing factor receptor antagonistA hormone antagonist that blocks corticotropin-releasing factor receptors
neuroprotective agentAny compound that can be used for the treatment of neurodegenerative disorders.
[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
homodetic cyclic peptideA homodetic cyclic peptide is a cyclic peptide in which the ring consists solely of amino-acid residues in peptide linkages.
polypeptideA peptide containing ten or more amino acid residues.
[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 (6)

Assay IDTitleYearJournalArticle
AID1345797Rat CRF2 receptor (Corticotropin-releasing factor receptors)1999The Journal of pharmacology and experimental therapeutics, Feb, Volume: 288, Issue:2
Comparison of an agonist, urocortin, and an antagonist, astressin, as radioligands for characterization of corticotropin-releasing factor receptors.
AID1345736Human CRF1 receptor (Corticotropin-releasing factor receptors)1998European journal of biochemistry, Nov-15, Volume: 258, Issue:1
Corticotropin-releasing factor receptor type 1 from Tupaia belangeri--cloning, functional expression and tissue distribution.
AID1345736Human CRF1 receptor (Corticotropin-releasing factor receptors)2001The Journal of pharmacology and experimental therapeutics, Jan, Volume: 296, Issue:1
Different binding modes of amphibian and human corticotropin-releasing factor type 1 and type 2 receptors: evidence for evolutionary differences.
AID1345736Human CRF1 receptor (Corticotropin-releasing factor receptors)1999The Journal of pharmacology and experimental therapeutics, Feb, Volume: 288, Issue:2
Comparison of an agonist, urocortin, and an antagonist, astressin, as radioligands for characterization of corticotropin-releasing factor receptors.
AID1345725Mouse CRF2 receptor (Corticotropin-releasing factor receptors)1999The Journal of pharmacology and experimental therapeutics, Feb, Volume: 288, Issue:2
Comparison of an agonist, urocortin, and an antagonist, astressin, as radioligands for characterization of corticotropin-releasing factor receptors.
AID1345772Human CRF2 receptor (Corticotropin-releasing factor receptors)2001The Journal of pharmacology and experimental therapeutics, Jan, Volume: 296, Issue:1
Different binding modes of amphibian and human corticotropin-releasing factor type 1 and type 2 receptors: evidence for evolutionary differences.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (165)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's22 (13.33)18.2507
2000's98 (59.39)29.6817
2010's42 (25.45)24.3611
2020's3 (1.82)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 21.95

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

MetricThis Compound (vs All)
Research Demand Index21.95 (24.57)
Research Supply Index5.14 (2.92)
Research Growth Index4.71 (4.65)
Search Engine Demand Index25.99 (26.88)
Search Engine Supply Index2.71 (0.95)

This Compound (21.95)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (1.18%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other168 (98.82%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Effects of Urocortins on Forearm Arterial Blood Flow in Healthy Volunteers [NCT01049542]6 participants (Actual)Interventional2010-05-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]