描述
A synthetic pentapeptide that mimics the actions of endogenous gastrin when given parenterally. It works by stimulating the secretion of gastric acid, pepsin, and intrinsic factor. It has also been used as a diagnostic aid.
一般参考文献
Weintraub HS, Rudolph A: Combination therapy for managing difficult-to-treat patients with stage 2 hypertension: focus on valsartan-based combinations. Am J Ther. 2011 Nov;18(6):e227-43. doi: 10.1097/MJT.0b013e3181da0437.
指示
Used as a diagnostic aid for evaluation of gastric acid secretory function
药效学
Pentagastrin is indicated as a diagnostic aid for evaluation of gastric acid secretory function. It is effective in testing for anacidity (achlorhydria) in patients with suspected pernicious anemia, atrophic gastritis, or gastric carcinoma. It is also effective in determining the reduction in acid output after operations for peptic ulcer, such as vagotomy or gastric resection.
作用机制
The exact mechanism by which pentagastrin stimulates gastric acid, pepsin, and intrinsic factor secretion is unknown; however, since pentagastrin is an analogue of natural gastrin, it is believed that it excites the oxyntic cells of the stomach to secrete to their maximum capacity. Pentagastrin stimulates pancreatic secretion, especially when administered in large intramuscular doses. Pentagastrin also increases gastrointestinal motility by a direct effect on the intestinal smooth muscle. However, it delays gastric emptying time probably by stimulation of terminal antral contractions, which enhance retropulsion.
吸收
Rapidly absorbed after parenteral administration.
分类
description:This compound belongs to the class of organic compounds known as hybrid peptides. These are compounds containing at least two different types of amino acids (alpha, beta, gamma, delta) linked to each other through a peptide bond.
direct-parent:Hybrid peptides
kingdom:Organic compounds
superclass:Organic acids and derivatives
class:Peptidomimetics
subclass:Hybrid peptides
alternative-parent:3-alkylindoles
alternative-parent:Alpha amino acid amides
alternative-parent:Amphetamines and derivatives
alternative-parent:Aspartic acid and derivatives
alternative-parent:Azacyclic compounds
alternative-parent:Beta amino acids and derivatives
alternative-parent:Carbamate esters
alternative-parent:Carbonyl compounds
alternative-parent:Carboxylic acids
alternative-parent:Dialkylthioethers
alternative-parent:Heteroaromatic compounds
alternative-parent:Hydrocarbon derivatives
alternative-parent:Methionine and derivatives
alternative-parent:Monocarboxylic acids and derivatives
alternative-parent:N-acyl amines
alternative-parent:N-acyl-alpha amino acids and derivatives
alternative-parent:Organic carbonic acids and derivatives
alternative-parent:Organic oxides
alternative-parent:Organonitrogen compounds
alternative-parent:Organopnictogen compounds
alternative-parent:Phenylalanine and derivatives
alternative-parent:Primary carboxylic acid amides
alternative-parent:Secondary carboxylic acid amides
alternative-parent:Substituted pyrroles
alternative-parent:Sulfenyl compounds
alternative-parent:Tryptamines and derivatives
substituent:3-alkylindole
substituent:Alpha-amino acid amide
substituent:Alpha-amino acid or derivatives
substituent:Amphetamine or derivatives
substituent:Aromatic heteropolycyclic compound
substituent:Aspartic acid or derivatives
substituent:Azacycle
substituent:Benzenoid
substituent:Beta amino acid or derivatives
substituent:Carbamic acid ester
substituent:Carbonic acid derivative
substituent:Carbonyl group
substituent:Carboxamide group
substituent:Carboxylic acid
substituent:Carboxylic acid derivative
substituent:Dialkylthioether
substituent:Fatty acyl
substituent:Fatty amide
substituent:Heteroaromatic compound
substituent:Hybrid peptide
substituent:Hydrocarbon derivative
substituent:Indole
substituent:Indole or derivatives
substituent:Methionine or derivatives
substituent:Monocarboxylic acid or derivatives
substituent:Monocyclic benzene moiety
substituent:N-acyl-alpha amino acid or derivatives
substituent:N-acyl-amine
substituent:N-substituted-alpha-amino acid
substituent:Organic nitrogen compound
substituent:Organic oxide
substituent:Organic oxygen compound
substituent:Organoheterocyclic compound
substituent:Organonitrogen compound
substituent:Organooxygen compound
substituent:Organopnictogen compound
substituent:Organosulfur compound
substituent:Phenylalanine or derivatives
substituent:Primary carboxylic acid amide
substituent:Pyrrole
substituent:Secondary carboxylic acid amide
substituent:Substituted pyrrole
substituent:Sulfenyl compound
substituent:Thioether
substituent:Triptan
种类
Amino Acids, Peptides, and Proteins
D000602
Diagnostic Agents
Gastrins
D005755
Gastrointestinal Hormones
D005768
Hormones
D006728
Hormones, Hormone Substitutes, and Hormone Antagonists
D006730
Nerve Tissue Proteins
D009419
Neuropeptides
D009479
Oligopeptides
D009842
Pentagastrin, antagonists & inhibitors
Peptide Hormones
D036361
Peptides
D010455
Proteins
D011506
Tests for Gastric Secretion
同义词
language:english; code:inn/usan; name;Pentagastrin
产品
name:Pentagastrin
labeller:Anazao Health Corporation
ndc-id:
ndc-product-code:51808-207
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2012-06-19
ended-marketing-on:
dosage-form:Solution
strength:250 ug/1.6mL
route:Intravenous
fda-application-number:
generic:false
over-the-counter:false
approved:false
country:US
source:FDA NDC
name:Peptavlon Liq Inj 0.25mg/ml
labeller:Wyeth Ayerst Canada Inc.
ndc-id:
ndc-product-code:
dpd-id:02043319
ema-product-code:
ema-ma-number:
started-marketing-on:1994-12-31
ended-marketing-on:1998-09-18
dosage-form:Liquid
strength:
route:Intramuscular; Intravenous; Subcutaneous
fda-application-number:
generic:false
over-the-counter:false
approved:true
country:Canada
source:DPD
混合物
name:Pentagastrin
ingredients:Pentagastrin
name:Peptavlon Liq Inj 0.25mg/ml
ingredients:Pentagastrin
generic:否; url:; name;Wyeth ayerst laboratories
受影响的生物体
Humans and other mammals
剂量
form:Solution
route:Intravenous
strength:250 ug/1.6mL
form:Liquid
route:Intramuscular; Intravenous; Subcutaneous
strength:
atc代码
Tests for gastric secretion
OTHER DIAGNOSTIC AGENTS
DIAGNOSTIC AGENTS
VARIOUS
实验性质
Melting Point
229 dec °C
PhysProp
logP
1.6
resource：Drugs Product Database (DPD)
identifier：2659
resource：ChEBI
identifier：31974
resource：PubChem Compound
identifier：9853654
resource：PubChem Substance
identifier：46507747
resource：KEGG Drug
identifier：D01631
resource：ChemSpider
identifier：8029364
resource：BindingDB
identifier：50024321
resource：PharmGKB
identifier：PA450849
resource：Therapeutic Targets Database
identifier：DNC001170
resource：IUPHAR
identifier：870
resource：Guide to Pharmacology
identifier：870
resource：Wikipedia
identifier：Pentagastrin
resource：ChEMBL
identifier：CHEMBL1328
resource：ZINC
identifier：ZINC000008214644
resource：RxCUI
identifier：7993
目标
id:BE0001158
name:Gastrin/cholecystokinin type B receptor
organism:Humans
action:agonist
Radu D, Ahlin A, Svanborg P, Lindefors N: Anxiogenic effects of the CCK(B) agonist pentagastrin in humans and dose-dependent increase in plasma C-peptide levels. Psychopharmacology (Berl). 2002 Jun;161(4):396-403. Epub 2002 Apr 17.
Khan S, Liberzon I, Abelson JL: Effect of repeat exposure on neuroendocrine and symptom responses to pentagastrin. Psychiatry Res. 2004 May 30;126(3):189-95.
Makovec F, Peris W, Revel L, Giovanetti R, Mennuni L, Rovati LC: Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives. J Med Chem. 1992 Jan;35(1):28-38.
Singh P, Walker JP, Townsend CM Jr, Thompson JC: Role of gastrin and gastrin receptors on the growth of a transplantable mouse colon carcinoma (MC-26) in BALB/c mice. Cancer Res. 1986 Apr;46(4 Pt 1):1612-6.
Nishida A, Kobayashi-Uchida A, Akuzawa S, Takinami Y, Shishido T, Kamato T, Ito H, Yamano M, Yuki H, Nagakura Y, et al.: Gastrin receptor antagonist YM022 prevents hypersecretion after long-term acid suppression. Am J Physiol. 1995 Nov;269(5 Pt 1):G699-705.
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.
known-action:yes
name:Gastrin/cholecystokinin type B receptor
general-function:Type b gastrin/cholecystokinin receptor binding
specific-function:Receptor for gastrin and cholecystokinin. The CKK-B receptors occur throughout the central nervous system where they modulate anxiety, analgesia, arousal, and neuroleptic activity. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.Isoform 2 is constitutively activated and may regulate cancer cell proliferation via a gastrin-independent mechanism.
gene-name:CCKBR
locus:11p15.4
cellular-location:Cell membrane
transmembrane-regions:58-79
88-109
132-150
171-189
220-242
334-355
374-394
signal-regions:
theoretical-pi:10.24
molecular-weight:48418.51
chromosome-location:11
organism:Humans
external-identifiers:HUGO Gene Nomenclature Committee (HGNC)HGNC:1571GenAtlasCCKBRGenBank Gene DatabaseL08112GenBank Protein Database306489IUPHAR77Guide to Pharmacology77UniProtKBP32239UniProt AccessionGASR_HUMAN
synonyms:CCK-B receptorCCK2-RCCKRBCholecystokinin-2 receptor
amino-acid-sequence:>lcl|BSEQ0002303|Gastrin/cholecystokinin type B receptor
MELLKLNRSVQGTGPGPGASLCRPGAPLLNSSSVGNLSCEPPRIRGAGTRELELAIRITL
YAVIFLMSVGGNMLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTF
IFGTVICKAVSYLMGVSVSVSTLSLVAIALERYSAICRPLQARVWQTRSHAARVIVATWL
LSGLLMVPYPVYTVVQPVGPRVLQCVHRWPSARVRQTWSVLLLLLLFFIPGVVMAVAYGL
ISRELYLGLRFDGDSDSDSQSRVRNQGGLPGAVHQNGRCRPETGAVGEDSDGCYVQLPRS
RPALELTALTAPGPGSGSRPTQAKLLAKKRVVRMLLVIVVLFFLCWLPVYSANTWRAFDG
PGAHRALSGAPISFIHLLSYASACVNPLVYCFMHRRFRQACLETCARCCPRPPRARPRAL
PDEDPPTPSIASLSRLSYTTISTLGPG
gene-sequence:>lcl|BSEQ0019073|Gastrin/cholecystokinin type B receptor (CCKBR)
ATGGAGCTGCTAAAGCTGAACCGGAGCGTGCAGGGAACCGGACCCGGGCCGGGGGCTTCC
CTGTGCCGCCCGGGGGCGCCTCTCCTCAACAGCAGCAGTGTGGGCAACCTCAGCTGCGAG
CCCCCTCGCATTCGCGGAGCCGGGACACGAGAATTGGAGCTGGCCATTAGAATCACTCTT
TACGCAGTGATCTTCCTGATGAGCGTTGGAGGAAATATGCTCATCATCGTGGTCCTGGGA
CTGAGCCGCCGCCTGAGGACTGTCACCAATGCCTTCCTCCTCTCACTGGCAGTCAGCGAC
CTCCTGCTGGCTGTGGCTTGCATGCCCTTCACCCTCCTGCCCAATCTCATGGGCACATTC
ATCTTTGGCACCGTCATCTGCAAGGCGGTTTCCTACCTCATGGGGGTGTCTGTGAGTGTG
TCCACGCTAAGCCTCGTGGCCATCGCACTGGAGCGGTACAGCGCCATCTGCCGACCACTG
CAGGCACGAGTGTGGCAGACGCGCTCCCACGCGGCTCGCGTGATTGTAGCCACGTGGCTG
CTGTCCGGACTACTCATGGTGCCCTACCCCGTGTACACTGTCGTGCAACCAGTGGGGCCT
CGTGTGCTGCAGTGCGTGCATCGCTGGCCCAGTGCGCGGGTCCGCCAGACCTGGTCCGTA
CTGCTGCTTCTGCTCTTGTTCTTCATCCCGGGTGTGGTTATGGCCGTGGCCTACGGGCTT
ATCTCTCGCGAGCTCTACTTAGGGCTTCGCTTTGACGGCGACAGTGACAGCGACAGCCAA
AGCAGGGTCCGAAACCAAGGCGGGCTGCCAGGGGCTGTTCACCAGAACGGGCGTTGCCGG
CCTGAGACTGGCGCGGTTGGCGAAGACAGCGATGGCTGCTACGTGCAACTTCCACGTTCC
CGGCCTGCCCTGGAGCTGACGGCGCTGACGGCTCCTGGGCCGGGATCCGGCTCCCGGCCC
ACCCAGGCCAAGCTGCTGGCTAAGAAGCGCGTGGTGCGAATGTTGCTGGTGATCGTTGTG
CTTTTTTTTCTGTGTTGGTTGCCAGTTTATAGTGCCAACACGTGGCGCGCCTTTGATGGC
CCGGGTGCACACCGAGCACTCTCGGGTGCTCCTATCTCCTTCATTCACTTGCTGAGCTAC
GCCTCGGCCTGTGTCAACCCCCTGGTCTACTGCTTCATGCACCGTCGCTTTCGCCAGGCC
TGCCTGGAAACTTGCGCTCGCTGCTGCCCCCGGCCTCCACGAGCTCGCCCCAGGGCTCTT
CCCGATGAGGACCCTCCCACTCCCTCCATTGCTTCGCTGTCCAGGCTTAGCTACACCACC
ATCAGCACACTGGGCCCTGGCTGA
pfams:PF000017tm_1
go-classifiers:componentcytosolcomponentintegral component of plasma membranecomponentplasma membranefunction1-phosphatidylinositol-3-kinase regulator activityfunctioncholecystokinin receptor activityfunctiongastrin receptor activityfunctionphosphatidylinositol phospholipase C activityfunctiontype B gastrin/cholecystokinin receptor bindingprocesscell proliferationprocesscell surface receptor signaling pathwayprocesscholecystokinin signaling pathwayprocessdigestionprocessdigestive tract developmentprocessfeeding behaviorprocessgastric acid secretionprocessgland developmentprocessphospholipase C-activating G-protein coupled receptor signaling pathwayprocesspositive regulation of cell proliferationprocesspositive regulation of cytosolic calcium ion concentrationprocessregulation of phosphatidylinositol 3-kinase activityprocesssensory perception
酶
BE0002180CholinesteraseHumansinducerA177856873393Chernysheva SV, Iaremko EE: [Cholinergic and hormonal correlations in the regulation of the secretory function of the small intestine]. Fiziol Zh SSSR Im I M Sechenova. 1983 Jun;69(6):827-31.unknownCholinesteraseIdentical protein bindingEsterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.BCHE3q26.1-q26.2Secreted1-287.4768417.5753HumansHUGO Gene Nomenclature Committee (HGNC)HGNC:983GenAtlasBCHEGenBank Gene DatabaseM32391GenBank Protein Database1311630Guide to Pharmacology2471UniProtKBP06276UniProt AccessionCHLE_HUMAN3.1.1.8Acylcholine acylhydrolaseButyrylcholine esteraseCHE1Choline esterase IIPseudocholinesterase>lcl|BSEQ0016706|Cholinesterase
MHSKVTIICIRFLFWFLLLCMLIGKSHTEDDIIIATKNGKVRGMNLTVFGGTVTAFLGIP
YAQPPLGRLRFKKPQSLTKWSDIWNATKYANSCCQNIDQSFPGFHGSEMWNPNTDLSEDC
LYLNVWIPAPKPKNATVLIWIYGGGFQTGTSSLHVYDGKFLARVERVIVVSMNYRVGALG
FLALPGNPEAPGNMGLFDQQLALQWVQKNIAAFGGNPKSVTLFGESAGAASVSLHLLSPG
SHSLFTRAILQSGSFNAPWAVTSLYEARNRTLNLAKLTGCSRENETEIIKCLRNKDPQEI
LLNEAFVVPYGTPLSVNFGPTVDGDFLTDMPDILLELGQFKKTQILVGVNKDEGTAFLVY
GAPGFSKDNNSIITRKEFQEGLKIFFPGVSEFGKESILFHYTDWVDDQRPENYREALGDV
VGDYNFICPALEFTKKFSEWGNNAFFYYFEHRSSKLPWPEWMGVMHGYEIEFVFGLPLER
RDNYTKAEEILSRSIVKRWANFAKYGNPNETQNNSTSWPVFKSTEQKYLTLNTESTRIMT
KLRAQQCRFWTSFFPKVLEMTGNIDEAEWEWKAGFHRWNNYMMDWKNQFNDYTSKKESCV
GL>lcl|BSEQ0016707|Cholinesterase (BCHE)
ATGCATAGCAAAGTCACAATCATATGCATCAGATTTCTCTTTTGGTTTCTTTTGCTCTGC
ATGCTTATTGGGAAGTCACATACTGAAGATGACATCATAATTGCAACAAAGAATGGAAAA
GTCAGAGGGATGAACTTGACAGTTTTTGGTGGCACGGTAACAGCCTTTCTTGGAATTCCC
TATGCACAGCCACCTCTTGGTAGACTTCGATTCAAAAAGCCACAGTCTCTGACCAAGTGG
TCTGATATTTGGAATGCCACAAAATATGCAAATTCTTGCTGTCAGAACATAGATCAAAGT
TTTCCAGGCTTCCATGGATCAGAGATGTGGAACCCAAACACTGACCTCAGTGAAGACTGT
TTATATCTAAATGTATGGATTCCAGCACCTAAACCAAAAAATGCCACTGTATTGATATGG
ATTTATGGTGGTGGTTTTCAAACTGGAACATCATCTTTACATGTTTATGATGGCAAGTTT
CTGGCTCGGGTTGAAAGAGTTATTGTAGTGTCAATGAACTATAGGGTGGGTGCCCTAGGA
TTCTTAGCTTTGCCAGGAAATCCTGAGGCTCCAGGGAACATGGGTTTATTTGATCAACAG
TTGGCTCTTCAGTGGGTTCAAAAAAATATAGCAGCCTTTGGTGGAAATCCTAAAAGTGTA
ACTCTCTTTGGAGAAAGTGCAGGAGCAGCTTCAGTTAGCCTGCATTTGCTTTCTCCTGGA
AGCCATTCATTGTTCACCAGAGCCATTCTGCAAAGTGGATCCTTTAATGCTCCTTGGGCG
GTAACATCTCTTTATGAAGCTAGGAACAGAACGTTGAACTTAGCTAAATTGACTGGTTGC
TCTAGAGAGAATGAGACTGAAATAATCAAGTGTCTTAGAAATAAAGATCCCCAAGAAATT
CTTCTGAATGAAGCATTTGTTGTCCCCTATGGGACTCCTTTGTCAGTAAACTTTGGTCCG
ACCGTGGATGGTGATTTTCTCACTGACATGCCAGACATATTACTTGAACTTGGACAATTT
AAAAAAACCCAGATTTTGGTGGGTGTTAATAAAGATGAAGGGACAGCTTTTTTAGTCTAT
GGTGCTCCTGGCTTCAGCAAAGATAACAATAGTATCATAACTAGAAAAGAATTTCAGGAA
GGTTTAAAAATATTTTTTCCAGGAGTGAGTGAGTTTGGAAAGGAATCCATCCTTTTTCAT
TACACAGACTGGGTAGATGATCAGAGACCTGAAAACTACCGTGAGGCCTTGGGTGATGTT
GTTGGGGATTATAATTTCATATGCCCTGCCTTGGAGTTCACCAAGAAGTTCTCAGAATGG
GGAAATAATGCCTTTTTCTACTATTTTGAACACCGATCCTCCAAACTTCCGTGGCCAGAA
TGGATGGGAGTGATGCATGGCTATGAAATTGAATTTGTCTTTGGTTTACCTCTGGAAAGA
AGAGATAATTACACAAAAGCCGAGGAAATTTTGAGTAGATCCATAGTGAAACGGTGGGCA
AATTTTGCAAAATATGGGAATCCAAATGAGACTCAGAACAATAGCACAAGCTGGCCTGTC
TTCAAAAGCACTGAACAAAAATATCTAACCTTGAATACAGAGTCAACAAGAATAATGACG
AAACTACGTGCTCAACAATGTCGATTCTGGACATCATTTTTTCCAAAAGTCTTGGAAATG
ACAGGAAATATTGATGAAGCAGAATGGGAGTGGAAAGCAGGATTCCATCGCTGGAACAAT
TACATGATGGACTGGAAAAATCAATTTAACGATTACACTAGCAAGAAAGAAAGTTGTGTG
GGTCTCTAAPF00135COesterasePF08674AChE_tetracomponentblood microparticlecomponentendoplasmic reticulum lumencomponentextracellular regioncomponentmembranecomponentnuclear envelope lumenfunctionacetylcholinesterase activityfunctionbeta-amyloid bindingfunctioncatalytic activityfunctioncholine bindingfunctioncholinesterase activityfunctionenzyme bindingfunctionidentical protein bindingprocessacetylcholine catabolic processprocesscellular protein metabolic processprocesscholine metabolic processprocesscocaine metabolic processprocesslearningprocessnegative regulation of cell proliferationprocessnegative regulation of synaptic transmissionprocessneuroblast differentiationprocessresponse to alkaloidprocessresponse to drugprocessresponse to folic acidprocessresponse to glucocorticoidprocesssynaptic transmissionunknown