Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C29H36N6O6S.ClH |
Molecular Weight | 633.159 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CSCC[C@H](NC(=O)[C@@H](N)CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC3=CC=CC=C3)C(N)=O
InChI
InChIKey=BABSBRZDEYUBSD-RJPXAACDSA-N
InChI=1S/C29H36N6O6S.ClH/c1-42-12-11-22(33-27(39)20(30)14-18-16-32-21-10-6-5-9-19(18)21)28(40)35-24(15-25(36)37)29(41)34-23(26(31)38)13-17-7-3-2-4-8-17;/h2-10,16,20,22-24,32H,11-15,30H2,1H3,(H2,31,38)(H,33,39)(H,34,41)(H,35,40)(H,36,37);1H/t20-,22-,23-,24-;/m0./s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/mesh/68013758Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/21261669
Sources: https://www.ncbi.nlm.nih.gov/mesh/68013758
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/21261669
Tetragastrin is a C-terminal tetrapeptide (Trp–Met–Asp–Phe–NH2) of gastrin. It is the smallest peptide fragment of gastrin which has the same physiological and pharmacological activity as gastrin. It is used to test the secretion of digestive juice. It causes severe anxiety symptoms when administered to humans and is commonly used in scientific research to induce panic attacks for the purpose of testing new anxiolytic drugs. Tetragastrin is a selective cholecystokinin B (CCKB) receptor agonist. Tetragastrin is used as a gastric stimulant at a dose of 4 ug/kg, it was marketed in Japan under the brand name Gastopsin.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL298 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9057851 |
19.5 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Diagnostic | Gastopsin Approved UseGastric acid secretion stimulant. |
PubMed
Title | Date | PubMed |
---|---|---|
Anxiogenic effects of the CCK(B) agonist pentagastrin in humans and dose-dependent increase in plasma C-peptide levels. | 2002 Jun |
|
New anthranilic acid based antagonists with high affinity and selectivity for the human cholecystokinin receptor 1 (hCCK1-R). | 2011 Aug 25 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16573782
after overnight fasting, 4 ug/kg by intramuscular injection.
Route of Administration:
Intramuscular
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18088282
CCK-4 (0.3 and 1.5 uM) enhanced significantly the K(+)-stimulated release of [(3)H]GABA from rat amygdala slices.
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13050781
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130LLV7CL9
Created by
admin on Fri Dec 15 15:39:29 GMT 2023 , Edited by admin on Fri Dec 15 15:39:29 GMT 2023
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5609-49-4
Created by
admin on Fri Dec 15 15:39:29 GMT 2023 , Edited by admin on Fri Dec 15 15:39:29 GMT 2023
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ACTIVE MOIETY
SUBSTANCE RECORD