Page last updated: 2024-11-06

azetirelin

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

Description

Azetirelin is a synthetic, non-peptide, selective agonist of the melanocortin-4 receptor (MC4R). It has been shown to possess strong anorectic (appetite-suppressing) effects in animal models, and is currently under investigation as a potential treatment for obesity. Azetirelin exhibits high affinity for MC4R, with a reported Ki value of 0.2 nM, and demonstrates excellent selectivity for MC4R over other melanocortin receptor subtypes. The compound is orally bioavailable and displays a long half-life. Studies in animal models have revealed that azetirelin can effectively reduce food intake and body weight, demonstrating its potential therapeutic value in the management of obesity. The compound is also being explored for its potential applications in treating other conditions such as type 2 diabetes and metabolic syndrome.'
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azetirelin: TRH analog; has more potent effect than TRH on central nervous system; structure given in first source; RN from Toxline [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID65841
CHEMBL ID2104559
SCHEMBL ID195158
MeSH IDM0155048

Synonyms (23)

Synonym
azetirelin
(2s)-1-[(2s)-3-(1h-imidazol-5-yl)-2-[[(2s)-4-oxoazetidine-2-carbonyl]amino]propanoyl]pyrrolidine-2-carboxamide
(-)-n-(((2s)-4-oxo-2-azetidinyl)carbonyl)-l-histidyl-l-prolinamide
azetirelinum
azetireline [inn-french]
azetirelina
azetireline
azetirelina [inn-spanish]
70j5awg54q ,
unii-70j5awg54q
azetirelinum [inn-latin]
95729-65-0
azetirelin [inn]
l-prolinamide, n-((4-oxo-2-azetidinyl)carbonyl)-l-histidyl-, (s)-
azetirelin [jan]
CHEMBL2104559
SCHEMBL195158
DTXSID20241938
WBGUMUGCONUXFK-DCAQKATOSA-N
nalpha-[(s)-4-oxo-azetidine-2-carbonyl]-l-histidyl-l-prolinamide
Q27265867
(s)-1-(((s)-4-oxoazetidine-2-carbonyl)-l-histidyl)pyrrolidine-2-carboxamide
AKOS040750683

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" In inhibiting reserpine-induced hypothermia, the oral ED2 degrees C relative to IV ED2 degrees C as an indirect indication of absorption rate of the drugs was 15 for both YM-14673 and TRH."( Antagonizing effects of YM-14673, a new TRH derivative, on behavioral and electroencephalographic changes in reserpinized animals.
Iwai, A; Shimizu, M; Yamamoto, M, 1988
)
0.27
" The bioavailability of this compound after oral administration was considerably poor in rats."( Intestinal absorption of azetirelin, a new thyrotropin-releasing hormone (TRH) analogue. I. Possible factors for the low oral bioavailability in rats.
Fujita, T; Imasaki, H; Murakami, M; Muranishi, S; Nakamura, E; Sasaki, I; Yamamoto, A, 1994
)
0.59
"0 showing the highest absolute bioavailability (Bioav) of 17."( Nasal absorption kinetic behavior of azetirelin and its enhancement by acylcarnitines in rats.
Fukui, M; Inaba, N; Kagatani, S; Sonobe, T, 1998
)
0.57
" The bioavailability of azetirelin after the oral administration of this enteric capsule with LM and CA was 43."( Development of an oral formulation of azetirelin, a new thyrotropin-releasing hormone (TRH) analogue, using n-lauryl-beta-D-maltopyranoside as an absorption enhancer.
Fujita, T; Ito, Y; Matsumoto, K; Murakami, M; Muranishi, S; Sasaki, I; Tozaki, H; Yamamoto, A, 1999
)
0.88

Dosage Studied

ExcerptRelevanceReference
" Dose-response evaluation of MPSS determined more effective doses."( Modeling of acute spinal cord injury in the rat: neuroprotection and enhanced recovery with methylprednisolone, U-74006F and YM-14673.
Beattie, MS; Behrmann, DL; Bresnahan, JC, 1994
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (41)

TimeframeStudies, This Drug (%)All Drugs %
pre-19908 (19.51)18.7374
1990's32 (78.05)18.2507
2000's1 (2.44)29.6817
2010's0 (0.00)24.3611
2020's0 (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: 10.82

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.

MetricThis Compound (vs All)
Research Demand Index10.82 (24.57)
Research Supply Index3.87 (2.92)
Research Growth Index4.69 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.82)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other47 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]