Movatterモバイル変換


[0]ホーム

URL:


Jump to content
WikipediaThe Free Encyclopedia
Search

RG7713

From Wikipedia, the free encyclopedia
Vasopressin V1A receptor antagonist

Pharmaceutical compound
RG7713
Clinical data
Other namesRG-7713; RO5028442; RO-5028442; Ro 5028442
Routes of
administration
Intravenous injection[1][2]
Drug classVasopressionVA receptorantagonist
Identifiers
  • [6-chloro-1-[2-(dimethylamino)ethyl]indol-3-yl]-spiro[1H-2-benzofuran-3,4'-piperidine]-1'-ylmethanone
CAS Number
PubChemCID
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC25H28ClN3O2
Molar mass437.97 g·mol−1
3D model (JSmol)
  • CN(C)CCN1C=C(C2=C1C=C(C=C2)Cl)C(=O)N3CCC4(CC3)C5=CC=CC=C5CO4
  • InChI=1S/C25H28ClN3O2/c1-27(2)13-14-29-16-21(20-8-7-19(26)15-23(20)29)24(30)28-11-9-25(10-12-28)22-6-4-3-5-18(22)17-31-25/h3-8,15-16H,9-14,17H2,1-2H3
  • Key:QZXVLRCMAHJVIP-UHFFFAOYSA-N

RG7713, orRG-7713, also known asRO5028442, is asmall-moleculevasopressionV1A receptorantagonist which is or was under development for the treatment ofpervasive developmental disorders orautism.[2][3][4] It is administered byintravenous injection.[1][2]

The drug iscentrally penetrant and is devoid ofantagonism of the vasopressinV2 andoxytocin receptors.[5] Clinical studies found induction of subtle improvements but also subtle deficits in social communication surrogates with RG7713 in adult men with high-functioning autism.[5][4] A 2024meta-analysis of vasopressin V1A receptor antagonists including RG7713 for autism found that they may not be effective in the treatment of the core symptoms of autism.[6]

As of December 2018, no recent development has been reported.[2] It reachedphase 1clinical trials.[2]Balovaptan (RG7314) has been described as a follow-up compound of RG7713 and reached later-stage clinical trials but was found to be ineffective.[3][6][7]

See also

[edit]

References

[edit]
  1. ^abLászló K, Vörös D, Correia P, Fazekas CL, Török B, Plangár I, et al. (September 2023)."Vasopressin as Possible Treatment Option in Autism Spectrum Disorder".Biomedicines.11 (10): 2603.doi:10.3390/biomedicines11102603.PMC 10603886.PMID 37892977.
  2. ^abcde"RG 7713".AdisInsight. 28 December 2018. Retrieved27 October 2024.
  3. ^abChadman KK, Fernandes S, DiLiberto E, Feingold R (August 2019). "Do animal models hold value in Autism spectrum disorder (ASD) drug discovery?".Expert Opinion on Drug Discovery.14 (8):727–734.doi:10.1080/17460441.2019.1621285.PMID 31132011.
  4. ^abHong MP, Erickson CA (August 2019). "Investigational drugs in early-stage clinical trials for autism spectrum disorder".Expert Opinion on Investigational Drugs.28 (8):709–718.doi:10.1080/13543784.2019.1649656.PMID 31352835.
  5. ^abLacivita E, Perrone R, Margari L, Leopoldo M (November 2017). "Targets for Drug Therapy for Autism Spectrum Disorder: Challenges and Future Directions".Journal of Medicinal Chemistry.60 (22):9114–9141.doi:10.1021/acs.jmedchem.7b00965.PMID 29039668.
  6. ^abKimi S, Maiti R, Srinivasan A, Mishra BR, Hota D (February 2024). "Efficacy and safety of V1a receptor antagonists in autism spectrum disorder: A meta-analysis".International Journal of Developmental Neuroscience.84 (1):3–13.doi:10.1002/jdn.10297.PMID 37641183.
  7. ^Jacob S, Veenstra-VanderWeele J, Murphy D, McCracken J, Smith J, Sanders K, et al. (March 2022). "Efficacy and safety of balovaptan for socialisation and communication difficulties in autistic adults in North America and Europe: a phase 3, randomised, placebo-controlled trial".The Lancet. Psychiatry.9 (3):199–210.doi:10.1016/S2215-0366(21)00429-6.PMID 35151410.
Oxytocin
Vasopressin
V1A
V1B
V2
Unsorted
Others
Retrieved from "https://en.wikipedia.org/w/index.php?title=RG7713&oldid=1258396526"
Categories:
Hidden categories:

[8]ページ先頭

©2009-2025 Movatter.jp