Rapastinel information

Rapastinel
Clinical data
Other names	GLYX-13; BV-102
Routes of; administration	Intravenous
Drug class	Selective NMDA receptor modulator
ATC code	None;
Legal status
Legal status	US: Investigational New Drug;
Identifiers
	IUPAC name (S)-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-1-[(S)-1-((2S,3R)-2-amino-3-hydroxybutanoyl)pyrrolidine-2-carbonyl]pyrrolidine-2-carboxamide;
CAS Number	117928-94-6 ;
PubChem CID	14539800;
ChemSpider	25069944;
UNII	6A1X56B95E;
Chemical and physical data
Formula	C18H31N5O6
Molar mass	413.475 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C[C@H]([C@@H](C(=O)N1CCC[C@H]1C(=O)N2CCC[C@H]2C(=O)N[C@@H]([C@@H](C)O)C(=O)N)N)O;
	InChI InChI=1S/C18H31N5O6/c1-9(24)13(19)18(29)23-8-4-6-12(23)17(28)22-7-3-5-11(22)16(27)21-14(10(2)25)15(20)26/h9-14,24-25H,3-8,19H2,1-2H3,(H2,20,26)(H,21,27)/t9-,10-,11+,12+,13+,14+/m1/s1; Key:GIBQQARAXHVEGD-BSOLPCOYSA-N;

Rapastinel (INNTooltip International Nonproprietary Name) (former developmental code name GLYX-13) is a novel antidepressant that was under development by Allergan (previously Naurex) as an adjunctive therapy for the treatment of treatment-resistant depression.^[1]^[2] It is a centrally active, intravenously administered (non-orally active) amidated tetrapeptide that acts as a novel and selective modulator of the NMDA receptor.^[1]^[2]^[3] The drug is a rapid-acting and long-lasting antidepressant as well as robust cognitive enhancer by virtue of its ability to enhance NMDA receptor-mediated signal transduction and synaptic plasticity.^[1]^[2]^[3]

^ ^a ^b ^c Henter ID, Park LT, Zarate CA (May 2021). "Novel Glutamatergic Modulators for the Treatment of Mood Disorders: Current Status". CNS Drugs. 35 (5): 527–543. doi:10.1007/s40263-021-00816-x. PMC 8201267. PMID 33904154.
^ ^a ^b ^c Moskal JR, Burgdorf JS, Stanton PK, Kroes RA, Disterhoft JF, Burch RM, Khan MA (2016). "The Development of Rapastinel (Formerly GLYX-13); A Rapid Acting and Long Lasting Antidepressant". Current Neuropharmacology. 15 (1): 47–56. doi:10.2174/1570159x14666160321122703. PMC 5327451. PMID 26997507.
^ ^a ^b Donello JE, Banerjee P, Li YX, Guo YX, Yoshitake T, Zhang XL, et al. (March 2019). "Positive N-Methyl-D-Aspartate Receptor Modulation by Rapastinel Promotes Rapid and Sustained Antidepressant-Like Effects". The International Journal of Neuropsychopharmacology. 22 (3): 247–259. doi:10.1093/ijnp/pyy101. PMC 6403082. PMID 30544218.

[:0-1] Henter ID, Park LT, Zarate CA (May 2021). "Novel Glutamatergic Modulators for the Treatment of Mood Disorders: Current Status". CNS Drugs. 35 (5): 527–543. doi:10.1007/s40263-021-00816-x. PMC 8201267. PMID 33904154.

[pmid26997507-2] Moskal JR, Burgdorf JS, Stanton PK, Kroes RA, Disterhoft JF, Burch RM, Khan MA (2016). "The Development of Rapastinel (Formerly GLYX-13); A Rapid Acting and Long Lasting Antidepressant". Current Neuropharmacology. 15 (1): 47–56. doi:10.2174/1570159x14666160321122703. PMC 5327451. PMID 26997507.

[:1-3] Donello JE, Banerjee P, Li YX, Guo YX, Yoshitake T, Zhang XL, et al. (March 2019). "Positive N-Methyl-D-Aspartate Receptor Modulation by Rapastinel Promotes Rapid and Sustained Antidepressant-Like Effects". The International Journal of Neuropsychopharmacology. 22 (3): 247–259. doi:10.1093/ijnp/pyy101. PMC 6403082. PMID 30544218.

Rapastinel information

and 27 Related for: Rapastinel information

Rapastinel

Apimostinel

Zelquistinel

Glutamine

NMDA receptor

Zinc

Glutathione

Ketamine

Phenobarbital

Saffron

Furosemide

Chloroform

Ibogaine

Sodium thiopental

Aspartic acid

Nitrous oxide

Lanicemine

Toluene

Hydrochlorothiazide

Pethidine

Magnesium

Dextromethorphan

Meprobamate

Xenon

Methylene blue

Pentobarbital

Bumetanide

Clinical data


Other names	GLYX-13; BV-102
Routes of administration	Intravenous
Drug class	Selective NMDA receptor modulator
ATC code	None
Legal status
Legal status	US: Investigational New Drug
Identifiers
IUPAC name (S)-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-1-[(S)-1-((2S,3R)-2-amino-3-hydroxybutanoyl)pyrrolidine-2-carbonyl]pyrrolidine-2-carboxamide
CAS Number	117928-94-6^Y
PubChem CID	14539800
ChemSpider	25069944
UNII	6A1X56B95E
Chemical and physical data
Formula	C₁₈H₃₁N₅O₆
Molar mass	413.475 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES C[C@H]([C@@H](C(=O)N1CCC[C@H]1C(=O)N2CCC[C@H]2C(=O)N[C@@H]([C@@H](C)O)C(=O)N)N)O
InChI InChI=1S/C18H31N5O6/c1-9(24)13(19)18(29)23-8-4-6-12(23)17(28)22-7-3-5-11(22)16(27)21-14(10(2)25)15(20)26/h9-14,24-25H,3-8,19H2,1-2H3,(H2,20,26)(H,21,27)/t9-,10-,11+,12+,13+,14+/m1/s1 Key:GIBQQARAXHVEGD-BSOLPCOYSA-N