Sar9, Met (O2)11-Substance P
Identification
- Generic Name
- Sar9, Met (O2)11-Substance P
- DrugBank Accession Number
- DB05875
- Background
Sar9, Met (O2)11-Substance P is a neurokinin-1 receptor agonist. It is an analog of the naturally occurring human neuropeptide Substance P, which can be found throughout the body, including in the airways of humans and many other species.
- Type
- Small Molecule
- Groups
- Investigational
- Structure
- Weight
- Average: 1393.68
Monoisotopic: 1392.733625766 - Chemical Formula
- C64H100N18O15S
- Synonyms
- (Sar(9),met(O2)(11))SP
- (Sar(9))SP sulfone
- 9-Sar-11-met(O2)-substance P
- 9-Sar-substance P sulfone
- 9-Sarcosyl-11-methionine(O2)-substance P
- Bolton hunter-9-sar-11-met(02)-substance P
- Sarcosyl(9)-substance P sulfone
Pharmacology
- Indication
Investigated for use/treatment in acute respiratory distress syndrome (ARDS) and viral infection.
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- Pharmacodynamics
Not Available
- Mechanism of action
The endogenous receptor for Substance P is neurokinin 1 receptor (NK1-receptor, NK1R). Substance P has been shown to stimulate cellular growth in cell culture [2], and it was shown that Substance P could promote wound healing of non-healing ulcers in humans. [3] It has also been shown to reverse diabetes in mice.
- Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAclidinium The serum concentration of Aclidinium can be increased when it is combined with Sar9, Met (O2)11-Substance P. Ambenonium Ambenonium may increase the neuromuscular blocking activities of Sar9, Met (O2)11-Substance P. Aprotinin Aprotinin may increase the neuromuscular blocking activities of Sar9, Met (O2)11-Substance P. Benzonatate The serum concentration of Sar9, Met (O2)11-Substance P can be increased when it is combined with Benzonatate. Betaine Betaine may increase the neuromuscular blocking activities of Sar9, Met (O2)11-Substance P. - Food Interactions
- Not Available
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- International/Other Brands
- Homspera / Viprovex
Categories
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 8V0QAFPRXV
- CAS number
- 110880-55-2
- InChI Key
- OUPXSLGGCPUZJJ-SARDKLJWSA-N
- InChI
- InChI=1S/C64H100N18O15S/c1-38(2)34-46(57(89)74-42(54(69)86)28-33-98(4,96)97)73-53(85)37-80(3)62(94)48(36-40-18-9-6-10-19-40)79-58(90)47(35-39-16-7-5-8-17-39)78-56(88)43(24-26-51(67)83)75-55(87)44(25-27-52(68)84)76-59(91)50-23-15-32-82(50)63(95)45(21-11-12-29-65)77-60(92)49-22-14-31-81(49)61(93)41(66)20-13-30-72-64(70)71/h5-10,16-19,38,41-50H,11-15,20-37,65-66H2,1-4H3,(H2,67,83)(H2,68,84)(H2,69,86)(H,73,85)(H,74,89)(H,75,87)(H,76,91)(H,77,92)(H,78,88)(H,79,90)(H4,70,71,72)/t41-,42-,43-,44-,45-,46-,47-,48-,49-,50-/m0/s1
- IUPAC Name
- (2S)-2-{[(2S)-1-[(2S)-6-amino-2-{[(2S)-1-[(2S)-2-amino-5-carbamimidamidopentanoyl]pyrrolidin-2-yl]formamido}hexanoyl]pyrrolidin-2-yl]formamido}-N-[(1S)-3-carbamoyl-1-{[(1S)-1-{[(1S)-1-[({[(1S)-1-{[(1S)-1-carbamoyl-3-methanesulfonylpropyl]carbamoyl}-3-methylbutyl]carbamoyl}methyl)(methyl)carbamoyl]-2-phenylethyl]carbamoyl}-2-phenylethyl]carbamoyl}propyl]pentanediamide
- SMILES
- CC(C)C[C@H](NC(=O)CN(C)C(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CCCNC(N)=N)C(=O)N[C@@H](CCS(C)(=O)=O)C(N)=O
References
- General References
- Grimsholm O, Rantapaa-Dahlqvist S, Dalen T, Forsgren S: Observations favouring the occurrence of local production and marked effects of bombesin/gastrin-releasing peptide in the synovial tissue of the human knee joint--comparisons with substance P and the NK-1 receptor. Neuropeptides. 2008 Apr;42(2):133-45. doi: 10.1016/j.npep.2007.12.008. [Article]
- Rothstein RD, Johnson E, Ouyang A: Substance P: mechanism of action and receptor distribution at the feline ileocecal sphincter region. Am J Physiol. 1989 Sep;257(3 Pt 1):G447-53. [Article]
- Link [Link]
- External Links
- PubChem Substance
- 347910285
- ChemSpider
- 143685
- BindingDB
- 50335566
- ChEMBL
- CHEMBL1651026
- Wikipedia
- Substance_P
Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
- Not Available
- Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.04 mg/mL ALOGPS logP -0.33 ALOGPS logP -7.8 Chemaxon logS -4.5 ALOGPS pKa (Strongest Acidic) 11.48 Chemaxon pKa (Strongest Basic) 11.87 Chemaxon Physiological Charge 3 Chemaxon Hydrogen Acceptor Count 20 Chemaxon Hydrogen Donor Count 15 Chemaxon Polar Surface Area 541.98 Å2 Chemaxon Rotatable Bond Count 42 Chemaxon Refractivity 368.55 m3·mol-1 Chemaxon Polarizability 144.97 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 0 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Oxygen binding
- Specific Function
- Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
- Gene Name
- CYP19A1
- Uniprot ID
- P11511
- Uniprot Name
- Aromatase
- Molecular Weight
- 57882.48 Da
References
- Gobbetti A, Zerani M, Di Fiore MM, Botte V: Relationships among GnRH, substance P, prostaglandins, sex steroids and aromatase activity in the brain of the male lizard Podarcis sicula sicula during reproduction. J Reprod Fertil. 1994 Aug;101(3):523-9. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Identical protein binding
- Specific Function
- Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.
- Gene Name
- BCHE
- Uniprot ID
- P06276
- Uniprot Name
- Cholinesterase
- Molecular Weight
- 68417.575 Da
References
- Lockridge O: Substance P hydrolysis by human serum cholinesterase. J Neurochem. 1982 Jul;39(1):106-10. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Prostaglandin-endoperoxide synthase activity
- Specific Function
- Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and...
- Gene Name
- PTGS2
- Uniprot ID
- P35354
- Uniprot Name
- Prostaglandin G/H synthase 2
- Molecular Weight
- 68995.625 Da
References
- Koon HW, Zhao D, Zhan Y, Rhee SH, Moyer MP, Pothoulakis C: Substance P stimulates cyclooxygenase-2 and prostaglandin E2 expression through JAK-STAT activation in human colonic epithelial cells. J Immunol. 2006 Apr 15;176(8):5050-9. [Article]
- Sio SW, Ang SF, Lu J, Moochhala S, Bhatia M: Substance P upregulates cyclooxygenase-2 and prostaglandin E metabolite by activating ERK1/2 and NF-kappaB in a mouse model of burn-induced remote acute lung injury. J Immunol. 2010 Nov 15;185(10):6265-76. doi: 10.4049/jimmunol.1001739. Epub 2010 Oct 6. [Article]
- Gallicchio M, Rosa AC, Benetti E, Collino M, Dianzani C, Fantozzi R: Substance P-induced cyclooxygenase-2 expression in human umbilical vein endothelial cells. Br J Pharmacol. 2006 Mar;147(6):681-9. [Article]
Drug created at November 18, 2007 18:28 / Updated at June 12, 2020 16:52