Page last updated: 2024-11-12

ristocetin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Ristocetin: An antibiotic mixture of two components, A and B, obtained from Nocardia lurida (or the same substance produced by any other means). It is no longer used clinically because of its toxicity. It causes platelet agglutination and blood coagulation and is used to assay those functions in vitro. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ristocetin : A heterodetic cyclic peptide that is produced by species of Amycolatopsis and Nocardia. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID16204749
CHEBI ID85129
MeSH IDM0019134

Synonyms (15)

Synonym
ristocetina [inn-spanish]
einecs 215-770-5
ristocetin
antibiotic obtained from cultures of nocardia lurida, or the same substance produced by any other means
ristocetin a
1404-55-3
riston
spontin
zp3e6s00il ,
unii-zp3e6s00il
ristocetina
ristocetin [usp:inn:ban]
CHEBI:85129
DTXSID30894853
AKOS040747397

Research Excerpts

Overview

Ristocetin is an activator of the von Willebrand factor that interacts with glycoprotein (GP) Ib/IX/V. It generates thromboxane A2 via phospholipase A2 activation, resulting in the release of CD40 ligand from human platelets.

ExcerptReferenceRelevance
"Ristocetin is an activator of the von Willebrand factor that interacts with glycoprotein (GP) Ib/IX/V, which generates thromboxane A2 via phospholipase A2 activation, resulting in the release of the soluble CD40 ligand (sCD40L) from human platelets."( Synergy by Ristocetin and CXCL12 in Human Platelet Activation: Divergent Regulation by Rho/Rho-Kinase and Rac.
Doi, T; Enomoto, Y; Hori, T; Iida, H; Iwama, T; Kozawa, O; Matsushima-Nishiwaki, R; Mizutani, D; Ogura, S; Onuma, T; Tanabe, K; Tokuda, H; Ueda, K, 2023
)
2.02
"Ristocetin is an antimicrobial substance that induces vWF-mediated aggregation of platelets."( Perhaps it's not the platelet: Ristocetin uncovers the potential role of von Willebrand factor in impaired platelet aggregation following traumatic brain injury.
Calfee, CS; Callcut, RA; Cohen, MJ; Conroy, AS; Fields, AT; Hendrickson, CM; Kornblith, LZ; Robles, AJ, 2018
)
1.49
"Ristocetin A is a class III glycopeptide antibiotic that is used in the diagnosis of von Willebrand disease and which has served as a lead compound for the development of new antimicrobial therapeutics."( Structure of ristocetin A in complex with a bacterial cell-wall mimetic.
Loll, PJ; Nahoum, V; Spector, S, 2009
)
1.44

Effects

ExcerptReferenceRelevance
"A ristocetin A CSP has been prepared 'in-house' and effectively applied in packed capillary SFC to separate the enantiomers of dichlorprop (R(s) = 1.4), ketoprofen (R(s) = 0.9) and warfarin (R(s) = 0.9)."( Enantioselective supercritical fluid chromatography using ristocetin A chiral stationary phases.
Owens, PK; Svensson, LA, 2000
)
1.11

Actions

Ristocetin did not increase the aggregatory potential of mutant vWF-A1, in contrast to native forms. It also promotes interaction of VWF with GP Ib-IX-V; it thus provides a model for changes in VWF conformation and function that may occur in vivo.

ExcerptReferenceRelevance
"Ristocetin also promotes the interaction of VWF with GpIb and is able to induce platelet aggregation, and thus is largely used to mimic this effect in vitro."( Ristocetin-induced self-aggregation of von Willebrand factor.
Arcovito, A; Arcovito, G; De Cristofaro, R; De Spirito, M; Di Stasio, E; Lancellotti, S; Maulucci, G; Missori, M; Papi, M, 2010
)
2.52
"Ristocetin did not increase the aggregatory potential of mutant vWF-A1, in contrast to native forms."( Platelet aggregation by membrane-expressed A1 domains of von Willebrand Factor is dependent on residues Asp 560 and Gly 561.
Cruz, MA; Robson, SC; Schulte am Esch, J, 2003
)
1.04
"Ristocetin was found to increase the rate of VWF proteolysis approximately two-fold; the differential between blood groups was retained in the presence of ristocetin."( An influence of ABO blood group on the rate of proteolysis of von Willebrand factor by ADAMTS13.
Bowen, DJ, 2003
)
1.04
"Ristocetin also promotes interaction of VWF with GP Ib-IX-V; it thus provides a model for changes in VWF conformation and function that may occur in vivo."( Evidence from limited proteolysis of a ristocetin-induced conformational change in human von Willebrand factor that promotes its binding to platelet glycoprotein Ib-IX-V.
Kang, M; Kermode, JC; Wilson, L,
)
1.12

Treatment

ExcerptReferenceRelevance
"Treatment of ristocetin-reacted platelets with either chymotrypsin, 100 microgram/ml, or trypsin, 75 microgram/ml, resulted in the partial release of the membrane-bound radioactivity."( Platelet-binding of the von Willebrand factor.
Green, D; Muller, HP, 1978
)
0.61

Toxicity

ExcerptReferenceRelevance
" LD50 of eremomycin on its intravenous administration to albino mice amounted to 1760 (1460-2130) mg/kg."( [Preclinical toxicological study of the new antibiotic eremomycin. Its acute toxicity for laboratory animals].
Gol'dberg, LE; Shepelevtseva, NG; Shevniuk, LA; Stepanova, ES; Vertogradova, TP, 1987
)
0.27

Pharmacokinetics

ExcerptReferenceRelevance
" In general, as the pI decreased, the clearance, urinary recovery, and volume of distribution decreased, whereas the half-life increased."( Charge and lipophilicity govern the pharmacokinetics of glycopeptide antibiotics.
Mico, BA; Nisbet, LJ; Pitkin, DH; Sitrin, RD, 1986
)
0.27
" All the patients underwent a pharmacokinetic analysis at presentation in order to study potential differences in recovery, clearance (CL) or terminal half-life (THL) following administration of von Willebrand factor (VWF) concentrate."( Pharmacokinetic studies with FVIII/von Willebrand factor concentrate can be a diagnostic tool to distinguish between subgroups of patients with acquired von Willebrand syndrome.
Inbal, A; Kotler, A; Lubetsky, A; Luboshitz, J; Schliamser, L; Tamarin, I, 2001
)
0.31
" We review the current literature regarding pharmacokinetic studies of von Willebrand factor (VWF) concentrates used to treat VWD."( Time to think outside the box? Proposals for a new approach to future pharmacokinetic studies of von Willebrand factor concentrates in people with von Willebrand disease.
Favaloro, EJ; Kershaw, G; Lloyd, J; McLachlan, AJ, 2007
)
0.34

Bioavailability

ExcerptReferenceRelevance
" A new VWF A1-domain binding aptamer, BT200, demonstrated good subcutaneous bioavailability and a long half-life in non-human primates."( The von Willebrand factor A-1 domain binding aptamer BT200 elevates plasma levels of von Willebrand factor and factor VIII: a first-in-human trial.
Beliveau, M; Bileck, A; Derhaschnig, U; Firbas, C; Gager, G; Gelbenegger, G; Gilbert, JC; Grafeneder, J; Jilma, B; Jilma-Stohlawetz, P; Kovacevic, KD; Quehenberger, P; Schörgenhofer, C; Zhu, S, 2022
)
0.72

Dosage Studied

Light transmission aggregometry may detect impaired ristocetin-induced platelet agglutination, enabling dosage of aspirin to be adjusted. The dosage of concentrates was tailored from in vitro measurements to achieve post-infusion levels above the lower normal limit (50 U/dL) for at least 3 hours.

ExcerptRelevanceReference
" When used in IRMA, these antibodies demonstrated the same abnormalities as heterologous antisera in variant VWD: decreased binding affinity or nonparallelism of the dose-response curves."( Familial incidence of precipitating antibodies in von Willebrand's disease: a study of four cases.
Ciavarella, N; Dammacco, F; Lavergne, JM; Mannucci, PM; Meyer, D; Molinari, A; Ruggeri, ZM, 1979
)
0.26
" Dose-response and dose-rate curves were constructed for ADP- and epinephrine-induced aggregation."( Low molecular weight heparin as an anticoagulant for in vitro platelet function studies.
Heyns, AD; van Wyk, V, 1990
)
0.28
" The platelet count concurrently decreased to approximately 50% of its baseline value but could not be further decreased either by raising the initial PG-1 dosage tenfold or by administering a second, equal dose 24 hours after the initial injection."( Effects of an antiplatelet glycoprotein Ib antibody on hemostatic function in the guinea pig.
Becker, BH; Miller, JL, 1989
)
0.28
" The dosage of concentrates was tailored from in vitro measurements to achieve post-infusion levels of ristocetin cofactor above the lower normal limit (50 U/dL) for at least 3 hours."( Correction of the bleeding time in treated patients with severe von Willebrand disease is not solely dependent on the normal multimeric structure of plasma von Willebrand factor.
Altieri, D; Castillo, R; Mannucci, PM; Moia, M; Monteagudo, J; Rebulla, P, 1987
)
0.49
" A dose-response 125I-vWF-platelet binding occurred with increasing ristocetin concentrations which was unchanged by the addition of collagen."( Platelet-collagen interaction: inhibition by ristocetin and enhancement by von Willebrand factor-platelet binding.
Bell, WR; Bettigole, RE; LaDuca, FM; Robson, EB, 1986
)
0.77
" In VIII R:Ag assays, the freeze-dried concentrates gave nonparallel dose-response curves compared with plasma, indicating alterations in molecular form during purification."( Factor VIII-related activities in therapeutic concentrates.
Barrowcliffe, TW; Furlong, RA; Holt, JC; Kemball-Cook, G; Morris, G; Peake, IR, 1981
)
0.26
" Dose-response measurement of platelet aggregation by GSNO was performed using an aggregometer."( S-nitrosoglutathione preserves platelet function during in vitro ventricular assist device circulation.
Aledia, AS; Chen, JC; Eng, J; Jones, BU; King, BO; Roum, JH; Serna, DL; Tran, LM,
)
0.13
" As the bleeding tendency is moderate in VWD type 2 and severe in type 3 and because the FVIII:C levels are subnormal in type 2 but very low in type 3 VWD patients, new guidelines using VWF:RCo unit dosing for the acute and prophylactic treatment of bleeding episodes are proposed."( Managing patients with von Willebrand disease type 1, 2 and 3 with desmopressin and von Willebrand factor-factor VIII concentrate in surgical settings.
Berneman, Z; Gadisseur, A; Michiels, JJ; Schroyens, W; van Vliet, HH, 2009
)
0.35
" Moreover, light transmission aggregometry may detect impaired ristocetin-induced platelet agglutination, enabling dosage of aspirin to be adjusted."( Assessment of platelet function with light transmission aggregometry in 24 patients supported with a continuous-flow left ventricular assist device: a single-center experience.
Barandon, L; Calderon, J; Fiore, M; James, C; Mouton, C; Ouattara, A; Picard, F, 2014
)
0.64
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
antibacterial drugA drug used to treat or prevent bacterial infections.
platelet-activating factor receptor agonistAn agonist that binds to and activates platelet-activating factor receptors.
bacterial metaboliteAny prokaryotic metabolite produced during a metabolic reaction in bacteria.
antimicrobial agentA substance that kills or slows the growth of microorganisms, including bacteria, viruses, fungi and protozoans.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (4)

ClassDescription
tetrasaccharide derivativeAn oligosaccharide derivative that is formally obtained from a tetrasaccharide.
macrocycleA cyclic compound containing nine or more atoms as part of the cyclic system.
heterodetic cyclic peptideA heterodetic cyclic peptide is a peptide consisting only of amino-acid residues, but in which the linkages forming the ring are not solely peptide bonds; one or more is an isopeptide, disulfide, ester, or other bond.
glycopeptideAny carbohydrate derivative that consists of glycan moieties covalently attached to the side chains of the amino acid residues that constitute the peptide.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Research

Studies (1,426)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990801 (56.17)18.7374
1990's270 (18.93)18.2507
2000's206 (14.45)29.6817
2010's128 (8.98)24.3611
2020's21 (1.47)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 62.33

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index62.33 (24.57)
Research Supply Index7.34 (2.92)
Research Growth Index4.25 (4.65)
Search Engine Demand Index109.23 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (62.33)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials23 (1.52%)5.53%
Reviews87 (5.74%)6.00%
Case Studies115 (7.59%)4.05%
Observational4 (0.26%)0.25%
Other1,286 (84.88%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]