Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C7H7NO2.C6H14N4O2 |
| Molecular Weight | 311.3369 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=CC=C(C=C1)C(O)=O.N[C@@H](CCCNC(N)=N)C(O)=O
InChI
InChIKey=QYWIRGMTYYEDBZ-VWMHFEHESA-N
InChI=1S/C7H7NO2.C6H14N4O2/c8-6-3-1-5(2-4-6)7(9)10;7-4(5(11)12)2-1-3-10-6(8)9/h1-4H,8H2,(H,9,10);4H,1-3,7H2,(H,11,12)(H4,8,9,10)/t;4-/m.0/s1
| Molecular Formula | C6H14N4O2 |
| Molecular Weight | 174.201 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
| Molecular Formula | C7H7NO2 |
| Molecular Weight | 137.136 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
L-arginine is a nonessential amino acid that may play an important role in the treatment of cardiovascular disease due to its antiatherogenic, anti-ischemic, antiplatelet, and antithrombotic properties. It has been promoted as a growth stimulant and as a treatment for erectile dysfunction in men. L-arginine is a nonessential amino acid that may play an important role in the treatment of heart disease due to its block arterial plaque buildup, blood clots, platelet clumping, and to increase blood flow through the coronary artery. L-arginine is commonly sold as a health supplement claiming to improve vascular health and treat erectile dysfunction in men. L-arginine, which is promoted as a human growth stimulant, has also been used in bodybuilding. In the 1800s, it was first isolated from animal horn.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: Q5T6X5 Gene ID: 222545.0 Gene Symbol: GPRC6A Target Organism: Homo sapiens (Human) |
44.1 µM [EC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Diagnostic | R-GENE 10 Approved UseR-Gene 10 is indicated as an intravenous stimulant to the pituitary for the release of human growth hormone in patients where the measurement of pituitary reserve for HGH can be of diagnostic usefulness. It can be used as a diagnostic aid in such conditions as panhypopituitarism, pituitary dwarfism, chromophobe adenoma, postsurgical craniopharyngioma, hypophysectomy, pituitary trauma, acromegaly, gigantism and problems of growth and stature.
If the insulin hypoglycemia test has indicated a deficiency of pituitary reserve for HGH, a test with R-Gene 10 is advisable to confirm the negative response. This can be done after a waiting period of one day. As patients may not respond to R-Gene 10 (Arginine Hydrochloride Injection, USP) during the first test, the unresponsive patient should be tested again to confirm the negative result. A second test can be performed after a waiting period of one day. Some patients who respond to R-Gene 10 do not respond to insulin and vice versa. The rate of false positive responses for R-Gene 10 is approximately 32%, and the rate of false negatives is approximately 27%. Launch Date1973 |
|||
| Diagnostic | R-GENE 10 Approved UseR-Gene 10 is indicated as an intravenous stimulant to the pituitary for the release of human growth hormone in patients where the measurement of pituitary reserve for HGH can be of diagnostic usefulness. It can be used as a diagnostic aid in such conditions as panhypopituitarism, pituitary dwarfism, chromophobe adenoma, postsurgical craniopharyngioma, hypophysectomy, pituitary trauma, acromegaly, gigantism and problems of growth and stature.
If the insulin hypoglycemia test has indicated a deficiency of pituitary reserve for HGH, a test with R-Gene 10 is advisable to confirm the negative response. This can be done after a waiting period of one day. As patients may not respond to R-Gene 10 (Arginine Hydrochloride Injection, USP) during the first test, the unresponsive patient should be tested again to confirm the negative result. A second test can be performed after a waiting period of one day. Some patients who respond to R-Gene 10 do not respond to insulin and vice versa. The rate of false positive responses for R-Gene 10 is approximately 32%, and the rate of false negatives is approximately 27%. Launch Date1973 |
|||
| Diagnostic | R-GENE 10 Approved UseR-Gene 10 is indicated as an intravenous stimulant to the pituitary for the release of human growth hormone in patients where the measurement of pituitary reserve for HGH can be of diagnostic usefulness. It can be used as a diagnostic aid in such conditions as panhypopituitarism, pituitary dwarfism, chromophobe adenoma, postsurgical craniopharyngioma, hypophysectomy, pituitary trauma, acromegaly, gigantism and problems of growth and stature.
If the insulin hypoglycemia test has indicated a deficiency of pituitary reserve for HGH, a test with R-Gene 10 is advisable to confirm the negative response. This can be done after a waiting period of one day. As patients may not respond to R-Gene 10 (Arginine Hydrochloride Injection, USP) during the first test, the unresponsive patient should be tested again to confirm the negative result. A second test can be performed after a waiting period of one day. Some patients who respond to R-Gene 10 do not respond to insulin and vice versa. The rate of false positive responses for R-Gene 10 is approximately 32%, and the rate of false negatives is approximately 27%. Launch Date1973 |
|||
| Diagnostic | R-GENE 10 Approved UseR-Gene 10 is indicated as an intravenous stimulant to the pituitary for the release of human growth hormone in patients where the measurement of pituitary reserve for HGH can be of diagnostic usefulness. It can be used as a diagnostic aid in such conditions as panhypopituitarism, pituitary dwarfism, chromophobe adenoma, postsurgical craniopharyngioma, hypophysectomy, pituitary trauma, acromegaly, gigantism and problems of growth and stature.
If the insulin hypoglycemia test has indicated a deficiency of pituitary reserve for HGH, a test with R-Gene 10 is advisable to confirm the negative response. This can be done after a waiting period of one day. As patients may not respond to R-Gene 10 (Arginine Hydrochloride Injection, USP) during the first test, the unresponsive patient should be tested again to confirm the negative result. A second test can be performed after a waiting period of one day. Some patients who respond to R-Gene 10 do not respond to insulin and vice versa. The rate of false positive responses for R-Gene 10 is approximately 32%, and the rate of false negatives is approximately 27%. Launch Date1973 |
|||
| Preventing | Unknown Approved UseUnknown |
|||
| Preventing | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
6219 μM |
30 g single, intravenous dose: 30 g route of administration: Intravenous experiment type: SINGLE co-administered: |
ARGININE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
882 μM |
6 g single, intravenous dose: 6 g route of administration: Intravenous experiment type: SINGLE co-administered: |
ARGININE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
310 μM |
6 g single, oral dose: 6 g route of administration: Oral experiment type: SINGLE co-administered: |
ARGININE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
265435 M × min |
30 g single, intravenous dose: 30 g route of administration: Intravenous experiment type: SINGLE co-administered: |
ARGININE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
38223 M × min |
6 g single, intravenous dose: 6 g route of administration: Intravenous experiment type: SINGLE co-administered: |
ARGININE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
24788 M × min |
6 g single, oral dose: 6 g route of administration: Oral experiment type: SINGLE co-administered: |
ARGININE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
41.6 min |
30 g single, intravenous dose: 30 g route of administration: Intravenous experiment type: SINGLE co-administered: |
ARGININE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
59.6 min |
6 g single, intravenous dose: 6 g route of administration: Intravenous experiment type: SINGLE co-administered: |
ARGININE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
|
77.5 min |
6 g single, oral dose: 6 g route of administration: Oral experiment type: SINGLE co-administered: |
ARGININE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
100% EXPERIMENT https://www.jci.org/articles/view/103568 |
ARGININE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
3.9 g/kg single, intravenous Accidental dose Dose: 3.9 g/kg Route: intravenous Route: single Dose: 3.9 g/kg Sources: |
unhealthy, 1.75 |
Disc. AE: Cardiopulmonary arrest, Metabolic acidosis... AEs leading to discontinuation/dose reduction: Cardiopulmonary arrest Sources: Metabolic acidosis (acute) Hyponatremia (severe) |
200 mg/kg 3 times / day multiple, oral Highest studied dose Dose: 200 mg/kg, 3 times / day Route: oral Route: multiple Dose: 200 mg/kg, 3 times / day Sources: |
unhealthy, 24 |
|
15 g 2 times / day multiple, oral Studied dose Dose: 15 g, 2 times / day Route: oral Route: multiple Dose: 15 g, 2 times / day Sources: |
healthy, 34 ± 2.6 |
|
7 g 3 times / day multiple, oral Studied dose Dose: 7 g, 3 times / day Route: oral Route: multiple Dose: 7 g, 3 times / day Sources: |
unhealthy, 43± 16 |
DLT: Gastrointestinal discomfort... Dose limiting toxicities: Gastrointestinal discomfort (20%) Sources: |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Cardiopulmonary arrest | Disc. AE | 3.9 g/kg single, intravenous Accidental dose Dose: 3.9 g/kg Route: intravenous Route: single Dose: 3.9 g/kg Sources: |
unhealthy, 1.75 |
| Metabolic acidosis | acute Disc. AE |
3.9 g/kg single, intravenous Accidental dose Dose: 3.9 g/kg Route: intravenous Route: single Dose: 3.9 g/kg Sources: |
unhealthy, 1.75 |
| Hyponatremia | severe Disc. AE |
3.9 g/kg single, intravenous Accidental dose Dose: 3.9 g/kg Route: intravenous Route: single Dose: 3.9 g/kg Sources: |
unhealthy, 1.75 |
| Gastrointestinal discomfort | 20% DLT |
7 g 3 times / day multiple, oral Studied dose Dose: 7 g, 3 times / day Route: oral Route: multiple Dose: 7 g, 3 times / day Sources: |
unhealthy, 43± 16 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Postabsorptive plasma citrulline concentration is a marker of absorptive enterocyte mass and intestinal failure in humans. | 2000 Dec |
|
| Internal ribosome entry site-mediated translation of a mammalian mRNA is regulated by amino acid availability. | 2001 Apr 13 |
|
| Increased affinity of c-Myb for CREB-binding protein (CBP) after CBP-induced acetylation. | 2001 Feb 2 |
|
| Amino acid residues outside of the pore region contribute to N-type calcium channel permeation. | 2001 Feb 23 |
|
| Arginine-rich peptides. An abundant source of membrane-permeable peptides having potential as carriers for intracellular protein delivery. | 2001 Feb 23 |
|
| Human glutathione transferase T2-2 discloses some evolutionary strategies for optimization of substrate binding to the active site of glutathione transferases. | 2001 Feb 23 |
|
| Current strategies for the management of neonatal urea cycle disorders. | 2001 Jan |
|
| Fibroblast growth factor-2 stimulates endothelial nitric oxide synthase expression and inhibits apoptosis by a nitric oxide-dependent pathway in Nb2 lymphoma cells. | 2001 Jan |
|
| Differential effects of glucagon-like peptide-1 (7-36)amide versus cholecystokinin on arginine-induced islet hormone release in vivo and in vitro. | 2001 Jan |
|
| Regulation of potassium channel Kir 1.1 (ROMK) abundance in the thick ascending limb of Henle's loop. | 2001 Jan |
|
| Agmatine enhances the NADPH oxidase activity of neuronal NO synthase and leads to oxidative inactivation of the enzyme. | 2001 Jan |
|
| Altered endothelium-dependent relaxations in lambs with high pulmonary blood flow and pulmonary hypertension. | 2001 Jan |
|
| Altered TNF-alpha, glucose, insulin, and amino acids in islets of Langerhans cultured in a microgravity model system. | 2001 Jan |
|
| Regulatory role of arginase I and II in nitric oxide, polyamine, and proline syntheses in endothelial cells. | 2001 Jan |
|
| Buffering action of endogenous nitric oxide on the adrenocortical secretagogue effect of endothelins in the rat. | 2001 Jan |
|
| In vitro studies of a prolactin antagonist, hPRL-G129R in human breast cancer cells. | 2001 Jan |
|
| Exercise training in coronary artery disease and coronary vasomotion. | 2001 Jan 2 |
|
| Pharmacological profile of T-1032, a novel specific phosphodiesterase type 5 inhibitor, in isolated rat aorta and rabbit corpus cavernosum. | 2001 Jan 5 |
|
| The role of nitric oxide in bradycardia of rats with obstructive cholestasis. | 2001 Jan 5 |
|
| Membrane binding motif of the P-type cardiotoxin. | 2001 Jan 5 |
|
| Crystal structure and novel recognition motif of rho ADP-ribosylating C3 exoenzyme from Clostridium botulinum: structural insights for recognition specificity and catalysis. | 2001 Jan 5 |
|
| The function of Arg-94 in the oxidation and decarboxylation of glutaryl-CoA by human glutaryl-CoA dehydrogenase. | 2001 Jan 5 |
|
| Rapid kinetic studies link tetrahydrobiopterin radical formation to heme-dioxy reduction and arginine hydroxylation in inducible nitric-oxide synthase. | 2001 Jan 5 |
|
| Translocation of jellyfish green fluorescent protein via the Tat system of Escherichia coli and change of its periplasmic localization in response to osmotic up-shock. | 2001 Mar 16 |
|
| Phage display-selected sequences of the heavy-chain CDR3 loop of the anti-digoxin antibody 26-10 define a high affinity binding site for position 16-substituted analogs of digoxin. | 2001 Mar 16 |
|
| The molecular mechanism for the genetic disorder familial defective apolipoprotein B100. | 2001 Mar 23 |
|
| Scanning mutagenesis reveals roles for helix n of the bacteriophage T7 RNA polymerase thumb subdomain in transcription complex stability, pausing, and termination. | 2001 Mar 30 |
|
| Substrate-binding clusters of the K+-transporting Kdp ATPase of Escherichia coli investigated by amber suppression scanning mutagenesis. | 2001 Mar 30 |
|
| Peptide leucine arginine, a potent immunomodulatory peptide isolated and structurally characterized from the skin of the Northern Leopard frog, Rana pipiens. | 2001 Mar 30 |
|
| Identification of the collagen-binding site of the von Willebrand factor A3-domain. | 2001 Mar 30 |
|
| The modulation of oxygen radical production by nitric oxide in mitochondria. | 2001 Mar 9 |
|
| Identification of the bile acid-binding site of the ileal lipid-binding protein by photoaffinity labeling, matrix-assisted laser desorption ionization-mass spectrometry, and NMR structure. | 2001 Mar 9 |
Sample Use Guides
In Vivo Use Guide
Curator's Comment: I.V route is possible: The recommended adult dose is 30 g arginine hydrochloride (300 mL of R-Gene 10) administered by intravenous infusion over 30 minutes. The total dose should not exceed 30 g arginine hydrochloride.
https://www.drugs.com/dosage/r-gene-10.html
L-arginine has been studied at oral doses of 6 to 30 g/day for a variety of conditions. Many formulations have been used.
Route of Administration:
Oral
A strong inward current in X. laevis oocytes expressing 5.24 (C terminus of the homologous goldfish 5.24 receptor) when L-Arg (L-arginine) was applied at 10 uM. When testing chimera h6A/5.24 (h6A/5.24, containing the ligand binding amino-terminal domain (ATD) of hGPRC6A with the signal transducing transmembrane and C terminus of the homologous goldfish 5.24 receptor) in this system, the responses were obtained with L-Arg at 100 uM.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 21:08:23 GMT 2025
by
admin
on
Mon Mar 31 21:08:23 GMT 2025
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| Record UNII |
3R2D6N19T5
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| Record Status |
Validated (UNII)
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| Record Version |
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3R2D6N19T5
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9926733
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1010241
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