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procaine

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Description

Procaine is a local anesthetic that blocks nerve conduction by inhibiting the influx of sodium ions into nerve cells. It is synthesized by reacting p-aminobenzoic acid with diethylaminoethanol. Procaine is typically administered by injection and is used to provide pain relief during medical procedures, such as dental work, surgery, and childbirth. It is also used to treat certain types of pain, such as chronic pain and neuralgia. Procaine is an important drug because it is effective, safe, and relatively inexpensive. It is studied to develop new and improved local anesthetics, and to investigate its potential therapeutic uses, such as in the treatment of cancer and inflammatory diseases.'

Procaine: A local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1016). [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

procaine : A benzoate ester, formally the result of esterification of 4-aminobenzoic acid with 2-diethylaminoethanol but formed experimentally by reaction of ethyl 4-aminobenzoate with 2-diethylaminoethanol. [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 CID4914
CHEMBL ID569
CHEBI ID8430
SCHEMBL ID3524
MeSH IDM0017615

Synonyms (165)

Synonym
BRD-K24616672-003-05-2
.beta.-(diethylamino)ethyl p-aminobenzoate
gerovital h-3
jenacain
novocain
duracaine
nsc169497
.beta.-diethylaminoethyl 4-aminobenzoate
novocaine
procain
2-diethylaminoethyl 4-aminobenzoate
nissocaine
procaine, base
norocaine
vitamin h3
spinocaine
4-aminobenzoic acid diethylaminoethyl ester
wln: zr dvo2n2&2
2-(diethylamino)ethyl p-aminobenzoate
gerovital
diethylaminoethyl p-aminobenzoate
scurocaine
p-aminobenzoic acid 2-diethylaminoethyl ester
nsc-169497
p-aminobenzoyldiethylaminoethanol
benzoic acid, p-amino-, 2-(diethylamino)ethyl ester
DIVK1C_000120
KBIO1_000120
SPECTRUM_000838
procaine [inn:ban]
stoff h3
procainum [inn-latin]
nsc 169497
einecs 200-426-9
hsdb 3388
4-aminobenzoesaeure-beta-diethylaminoethylester
2-diethylaminoethylester kyseliny p-aminobenzoove [czech]
beta-diethylaminoethyl 4-aminobenzoate
procaina [inn-spanish]
brn 0913480
factor h3
lopac-p-9879
cas-51-05-8
NCGC00015864-02
NCGC00015864-01
sp-01
anticort (tm)
sp01
BPBIO1_000179
BSPBIO_002231
IDI1_000120
PRESTWICK2_000041
2-(diethylamino)ethyl 4-aminobenzoate
benzoic acid,4-amino,2-diethylaminoethyl ester procain base
inchi=1/c13h20n2o2/c1-3-15(4-2)9-10-17-13(16)11-5-7-12(14)8-6-11/h5-8h,3-4,9-10,14h2,1-2h
benzoic acid, 4-amino-, 2-(diethylamino)ethyl ester
AB00053531
C07375
procaine
59-46-1
2-diethylaminoethyl p-aminobenzoate
DB00721
beta-(diethylamino)ethyl p-aminobenzoate
beta-(diethylamino)ethyl 4-aminobenzoate
4-aminobenzoic acid 2-diethylaminoethyl ester
STK177303
KBIOGR_000975
KBIO2_003886
KBIO2_006454
KBIOSS_001318
KBIO2_001318
KBIO3_001731
PRESTWICK0_000041
SPBIO_001331
SPBIO_002082
SPECTRUM4_000488
NINDS_000120
SPECTRUM3_000556
SPECTRUM2_001296
PRESTWICK1_000041
PRESTWICK3_000041
BSPBIO_000161
LOPAC0_000966
SPECTRUM5_001186
MLS001304095 ,
NCGC00162298-01
smr000718771
CHEBI:8430 ,
procainum
procaina
NCGC00015864-04
AKOS000115407
2-(diethylamino)ethyl-4-aminobenzoate
CHEMBL569
procaine (inn)
D08422
FT-0654843
A832329
2-(diethylamino)ethyl 4-aminobenzoate;procaine
2-(diethylamino)ethyl 4-aminobenzoate hydrochloride;procaine hcl
A19427
4-14-00-01138 (beilstein handbook reference)
2-diethylaminoethylester kyseliny p-aminobenzoove
4z8y51m438 ,
unii-4z8y51m438
BBL005106
P1961
4-aminobenzoic acid 2-(diethylamino)ethyl ester
CCG-205046
S4668
NCGC00015864-03
4-amino-benzoic acid 2-diethylamino-ethyl ester
AE-641/00560024
procaine [vandf]
procaine [mi]
procaine [who-dd]
procaine [inn]
procaine [hsdb]
procaine base
EPITOPE ID:115010
gtpl4291
AB00053531-09
HY-B0546
SCHEMBL3524
2-(n,n-diethylamino)ethyl 4-amino-benzoate
DTXSID7045021 ,
4-aminobenzoic acid 2-(diethylamino)ethyl ester;hydrochloride
cid_5795
2-(diethylamino)ethyl 4-aminobenzoate;hydrochloride
sampl3, g2
bdbm64452
2-(diethylamino)ethyl 4-azanylbenzoate;hydrochloride
DS-1216
aminocaine (salt/mix)
gerovital h3 (salt/mix)
allocaine (salt/mix)
neocaine (salt/mix)
novocaine (salt/mix)
p-aminobenzoic acid, 2-(diethylamino)ethyl ester
scurocaine (salt/mix)
sevicaine (salt/mix)
.beta.-(diethylamino)ethyl 4-aminobenzoate
neotonocaine (salt/mix)
novocain (salt/mix)
AB00053531_11
AB00053531_12
mfcd00007893
SBI-0050939.P004
A16131
benzoic acid,4-amino-,2-(diethylamino)ethyl ester
Q423741
BRD-K24616672-003-10-2
SDCCGSBI-0050939.P005
NCGC00015864-18
HMS3885F16
SY030284
benzoic acid, 4-amino- 2-(diethylamino)ethyl ester
EN300-33930
4-aminobenzoic acid 2-(diethylamino) ethyl ester;novocaine
dtxcid5025021
procaina (inn-spanish)
c05ad05
s01ha05
n01ba02
procainum (inn-latin)

Research Excerpts

Overview

Procaine is an anesthetic drug with demethylant properties, mainly used by dentists in oral surgeries. Procaine is a controversial substance which has been used for "antiageing" effects including cognitive improvement for more than 50 years.

ExcerptReferenceRelevance
"Procaine is an anesthetic drug with demethylant properties, mainly used by dentists in oral surgeries."( Procaine Inhibits Osteo/Odontogenesis through Wnt/β-Catenin Inactivation.
Almadén, Y; Diaz-Tocados, JM; Herencia, C; Jurado, L; Martín-Alonso, C; Martínez-Moreno, JM; Montes de Oca, A; Muñoz-Castañeda, JR; Rodríguez, M; Rodríguez-Ortiz, ME; Vergara, N, 2016
)
2.6
"Oxybuprocaine (OBPC) is a widely used topical anesthetic in eye clinic, and prolonged and repeated usage of OBPC might be cytotoxic to the cornea, especially to the outmost corneal epithelium. "( The cytotoxic effect of oxybuprocaine on human corneal epithelial cells by inducing cell cycle arrest and mitochondria-dependent apoptosis.
Fan, TJ; Fan, WY; Wang, DP; Wen, Q, 2017
)
1.26
"Procaine (PCA) is a conventional chemotherapeutic agent for osteosarcoma. "( Procaine Inhibits Proliferation and Migration and Promotes Cell Apoptosis in Osteosarcoma Cells by Upregulation of MicroRNA-133b.
Huang, H; Li, H; Song, M; Wu, S; Ying, B; Ying, H, 2017
)
3.34
"Procaine is a controversial substance which has been used for "antiageing" effects including cognitive improvement for more than 50 years.Preparations which contain procaine as a component are claimed to prevent, reverse and interrupt dementia. "( Procaine treatments for cognition and dementia.
Bereczki, D; Szatmári, S, 2008
)
3.23
"Procaine is a local anesthetic that preferentially stimulates limbic structures."( Gender differences in limbic responsiveness, by SPECT, following a pharmacologic challenge in healthy subjects.
Adinoff, B; Alexander, D; Best, SE; Chandler, P; Devous, MD; Harris, TS; Payne, K; Williams, MJ, 2003
)
1.04
"Procaine is a substance which is known to specifically inhibit the calcium-induced calcium release mechanism."( Effects of procaine on the isolated dog coronary artery.
Imai, H; Imai, S; Nabata, H; Nakazawa, M, 1984
)
1.38
"Procaine penicillin is a commonly used antibiotic in equine medicine but its use is associated with a substantial incidence of adverse reactions. "( The role of procaine in adverse reactions to procaine penicillin in horses.
Chapman, CB; Courage, P; Huntington, PJ; Nielsen, IL; Sitaram, BR, 1992
)
2.11
"Procaine is a local anesthetic, also used in experimental gerontology and has been tested in cultivated human WI-38 fibroblasts. "( Effect of procaine on cultivated human WI-38 fibroblasts.
Houbion, A; Pigeolet, E; Raes, M; Remacle, J, 1988
)
2.12

Effects

Procaine has proven positive effects in carpal tunnel syndrome and chondromalacia patella. Procaine has high affinity to muscarinic M2 receptors in vivo in the rhesus monkey. It has been used to stimulate plant growth and it has been noted that it also promotes growth of microorganisms.

ExcerptReferenceRelevance
"If procaine has an antidepressant effect, there is some likelihood that this accounts for the reports of decreased complaints referable to the musculoskeletal, cardiovascular, endocrine sexual, gastrointestinal and respiratory systems."( The systemic use of procaine in the treatment of the elderly: a review.
Ostfeld, A; Smith, CM; Stotsky, BA, 1977
)
1.09
"Procaine has proven positive effects in carpal tunnel syndrome and chondromalacia patella."( Procaine and saline have similar effects on articular cartilage and synovium in rat knee.
Akca, B; Ankay Yilbas, A; Bahador Zirh, E; Buyukakkus, B; Saricaoglu, F; Uzumcugil, F; Zeybek, D, 2018
)
2.64
"Procaine has high affinity to muscarinic M2 receptors in vivo in the rhesus monkey."( A potential cholinergic mechanism of procaine's limbic activation.
Benson, BE; Carson, RE; Eckelman, WC; Herscovitch, P; Ketter, TA; Kiesewetter, DO; Post, RM, 2004
)
1.32
"1. Procaine has previously been shown to diminish the nephrotoxicity of cisplatin and the nephrotoxic effects of cisplatin and a new cisplatin complex (cis-diamminechloro-[2-(diethylamino) ethyl-4-aminobenzoate, N4]-chlorideplatinum (II) monohydrochloride monohydrate; DPR), that contains procaine hydrochloride were compared with rat renal cortical slices. "( Comparison of the toxicities of cisplatin and a new cisplatin-procaine complex to rat renal cortical slices.
Cafaggi, S; Esposito, M; Lindup, WE; Zhang, JG, 1996
)
1.16
"Procaine has been used to stimulate plant growth and it has been noted that it also promotes growth of microorganisms. "( Stimulatory effect of procaine on the growth of several microalgae and cyanobacteria.
Domen, H; Ezure, T; Ishida, M; Schmidt, W; Suzuki, T; Yamaguchi, T, 2000
)
2.06
"If procaine has an antidepressant effect, there is some likelihood that this accounts for the reports of decreased complaints referable to the musculoskeletal, cardiovascular, endocrine sexual, gastrointestinal and respiratory systems."( The systemic use of procaine in the treatment of the elderly: a review.
Ostfeld, A; Smith, CM; Stotsky, BA, 1977
)
1.09
"Procaine has been advocated in the treatment of malignant hyperpyrexia, whereas lignocaine has been shown to worsen the condition. "( An evaluation of procaine in the treatment of malignant hyperpyrexia.
Clarke, IM; Ellis, FR, 1975
)
2.04
"Procaine has different effects on various ionic conductive pathways through the frog skin. "( Evaluation of the stimulatory capacity of procaine on Na transport through frog skin.
Flonta, ML; Frangopol, PT; Nistor, M, 1991
)
1.99
"Procaine has opposite effects on the active transport of Na+ when applied on the mucosal side of the frog skin [where it produces a stimulation of the short-circuit current (Isc)] or when added on the serosal side (where it produces an inhibition of Isc). "( Procaine has opposite effects on passive Na and K permeabilities in frog skin.
Flonta, ML; Frangopol, PT; Galter, D; Mărgineanu, DG, 1987
)
3.16

Actions

Procaine could inhibit the proliferation of CNE-2Z cells. If procaine promotes premature AR of spermatozoa in vivo, it might be a factor for infertility in patients exposed to this local anesthetic.

ExcerptReferenceRelevance
"Procaine did produce overall longer sensory blockade (P = 0.0011) and motor blockade at the gastrocnemius (P = 0.0004) and quadriceps (P = 0.0146) muscles."( Spinal 2-chloroprocaine: a comparison with procaine in volunteers.
Gonter, AF; Kopacz, DJ, 2005
)
1.4
"If procaine promotes premature AR of spermatozoa in vivo, it might be a factor for infertility in patients exposed to this local anesthetic."( In guinea pig spermatozoa, the procaine-promoted synchronous acrosome reaction results in highly fertile cells exhibiting normal F-actin distribution.
Delgado-Buenrostro, NL; Mújica, A; Sánchez-Gutiérrez, M; Uribe, S; Zárate-Grande, M, 2006
)
1.13
"Procaine could inhibit the proliferation of CNE-2Z cells and the effects were in dose- and time-dependent manners. "( [Effects of procaine on human nasopharyngeal carcinoma cell strain CNE-2Z].
Luo, G; Xu, M; Zhang, Y; Zhou, H, 2007
)
2.16
"Procaine could inhibit cell growth and up-regulate the expression of RASSF1A mRNA, which may play an important role in CNE-2Z cells' proliferation inhibition induced by procaine."( [Effects of procaine on human nasopharyngeal carcinoma cell strain CNE-2Z].
Luo, G; Xu, M; Zhang, Y; Zhou, H, 2007
)
2.16
"Procaine lower than 10 mM was ineffective on [125I]-BH-CCK-8 binding, although procaine (10 mM) caused weak but significant inhibition of the binding."( Competitive inhibition by procaine of carbachol-induced stimulus-secretion coupling in rat pancreatic acini.
Busik, J; Habara, Y; Ikei, N; Kanno, T, 1993
)
1.31
"Procaine may increase the Ca inward current, acting on the intracellular Ca storage site and consequently accelerate the excitation-contraction coupling in frog ventricular muscle."( Effects of procaine on the ventricular muscle of bullfrog.
Hatae, J, 1979
)
1.37
"Procaine could inhibit the triggering as well as the induction of thermotolerance."( Development of thermotolerance in mouse fibroblast LM cells with modified membranes and after procaine treatment.
Konings, AW, 1985
)
1.21
"Procaine did not produce any marked change in the electrical constants of muscle fibres.3."( Changes in the time course of transmitter action produced by procaine.
Hirst, GD; Wood, DR, 1971
)
1.21

Treatment

Procaine treatment increased the glucagon and fluoride activation of the cyclase. The stimulation was concentration-dependent. Procaine-treated eggs can be penetrated by more than one spermatozoon.

ExcerptReferenceRelevance
"Procaine treatment during acquisition left the later retention of the initial learning (A+ vs B-) intact."( Using local anaesthetics to block neuronal activity and map specific learning tasks to the mushroom bodies of an insect brain.
Blunk, A; Devaud, JM; Giurfa, M; Grünewald, B; Podufall, J, 2007
)
1.06
"Procaine treatment increased the glucagon and fluoride activation of the cyclase and the stimulation was concentration-dependent; this compound seemed to act at the G/F unit level since changes in the glucagon binding were not observed and the basal activity was not modified."( The role of surface charge and hydrophobic interaction in the activation of rat liver adenylate cyclase.
Cerbon, J; Grajales, MO; Pliego, JA; Rubalcava, B, 1983
)
0.99
"Procaine pretreatment did not abolish the ability of MEL cells to complete the "latent period" and commit upon the removal of the block."( Procaine inhibits the erythroid differentiation of MEL cells by blocking commitment: possible involvement of calcium metabolism.
Housman, DE; Mitrani, AA; Tsiftsoglou, AS, 1981
)
2.43
"Procaine-treated eggs can be penetrated by more than one spermatozoon. "( Multipolar mitosis in procaine-treated polyspermic sea urchin eggs and in eggs fertilized with UV-irradiated spermatozoa with a computer model to simulate the positioning of centrosomes.
Czihak, G; Kojima, M; Linhart, J; Vogel, H, 1991
)
2.04
"Procaine treatment of wild-type cells resulted in the same phenotype through an envZ+-mediated mechanism."( Contrasting mechanisms of envZ control of mal and pho regulon genes in Escherichia coli.
Boos, W; Bukau, B; Case, CC; Granett, S; Villarejo, MR, 1986
)
0.99
"Procaine treatment induced the formation of large cytoplasmic blebs and cytoskeletal condensations but did not affect the surface coat."( Immediate effects of procaine and pentobarbital on placodal and non-placodal head ectoderm of the chick embryo in vitro.
Rowlett, KA; Wakely, J; Wasserberg, J, 1985
)
1.31
"Rats treated with procaine, even at 20%, showed no histologic abnormalities."( Spinal procaine is less neurotoxic than mepivacaine, prilocaine and bupivacaine in rats.
Hiruma, H; Hoka, S; Kawakami, T; Nara, Y; Takenami, T; Tsai, YH; Yagishita, S,
)
0.91
"Pre-treatment with procaine blocked both the contractures and the increased enzyme loss induced by these alkaloids."( Caffeine and quinine increase the release of sarcoplasmic enzymes from frog skeletal muscles.
Suarez-Kurtz, G, 1982
)
0.58
"Pretreatment with procaine did not prevent the onset of the condition and the administration of procaine when muscle rigidity was present failed to prevent a fatal outcome."( Further studies of porcine malignant hyperthermia.
Hall, LW; Trim, CM; Woolf, N, 1972
)
0.57

Toxicity

Toxic effects of procaine were, therefore, concluded to be due to the accumulation of the drug in the brain. To reduce its toxic side effects in patients, cisplatin has been bound with procaine in a cis platin-procaine complex (DPR)

ExcerptReferenceRelevance
" Toxic effects of procaine were, therefore, concluded to be due to the accumulation of the drug in the brain."( Effect of pretreatment with tricresylphosphates and phenobarbital on the metabolism and toxicity of procaine in rats.
Moroi, K; Satoh, T, 1977
)
0.81
"There have been reports of toxic reactions to ester-type local anesthetics in patients with genetic anomalies of plasma cholinesterase in so-called dibucaine-resistant homozygotes or heterozygotes."( Survey of local anesthetic toxicity in the families of patients with atypical plasma cholinesterase.
Eilderton, TE; Zsigmond, EK, 1975
)
0.25
"Although the toxic effect of local anaesthetics on the activity of cerebral cortex has been extensively studied, little is known about their toxic effect on brainstem."( Brainstem auditory evoked potentials during procaine toxicity in dogs.
Ding, ZN; Hirota, K; Kobayashi, T; Murakami, S; Yamamoto, K; Yoshita, Y, 1992
)
0.54
" Dose-response curves were constructed from the data obtained, and the CD50 and LD50 values for each local anesthetic alone and in combination with each of the vasoconstrictors were calculated by probit analysis."( Modification of local anesthetic toxicity by vasoconstrictors.
Dorris, RL; Taylor, SE,
)
0.13
"2% BS was not toxic to peripheral nerves."( Peripheral neurotoxicity of 2-chloroprocaine and bisulfite in the cat.
Ford, DJ; Raj, PP, 1987
)
0.55
" Shorter exposure times (3 hr) resulted in a marginal toxic effect (32%)."( Toxicity of chloroprocaine and sodium bisulfite on human neuroblastoma cells.
Lear, E; Seravalli, E, 1987
)
0.61
"A drug registry was established at Southern California College of Optometry (SCCO) to study use rates and incidence of adverse side effects of the nine pharmaceutical agents in the California optometry law."( Use of diagnostic pharmaceutical agents and incidence of adverse effects.
Applebaum, M; Jaanus, SD, 1983
)
0.27
" Prilocaine produced the predetermined toxic end-points (i."( Comparison of acute central nervous system and cardiovascular toxicity of 2-chloroprocaine and prilocaine in the rat.
Heavner, JE; Rosenberg, PH; Zou, J, 1993
)
0.51
" The changes of two characteristics of the neurite outgrowth, the mean radial length of neuritic processes growing out from the ganglia and the area of neurite outgrowth around the ganglion, were used as parameters to evaluate the toxic effect of both compounds."( Neurotoxic effect of cisplatin and the cisplatin-procaine complex DPR studied in organotypic cultures of chick embryonic dorsal root ganglia.
Cafaggi, S; Esposito, M; Mandys, V; Viale, M; Vrana, J, 1998
)
0.55
" To reduce its toxic side effects in patients, cisplatin has been bound with procaine in a cisplatin-procaine complex (DPR)."( Embryotoxicity of cisplatin and a cisplatin-procaine complex (DPR) studied in chick embryo.
Cafaggi, S; Esposito, M; Mandys, V; Peterka, M; Peterková, R; Viale, M, 2002
)
0.8
" ischiadicus as a first sign of toxic side effects indicated that low effect is combined with short paresis."( Local anaesthetic effects and toxicity of seven new diethanolamine and morpholine derivatives of fomocaine. Testing in rats compared with procaine and tetracaine.
Fleck, C; Karge, E; Listing, M; Loy, S; Oelschläger, H; Wennek-Klose, J, 2003
)
0.52
" Although lidocaine is more toxic than bupivacaine and ropivacaine, mepivacaine, which has a similar pharmacological effect to lidocaine, has the least-adverse effects on cone growth among clinically used local anesthetics."( Procaine and mepivacaine have less toxicity in vitro than other clinically used local anesthetics.
Kasaba, T; Onizuka, S; Takasaki, M, 2003
)
1.76
" Although lidocaine is more toxic than bupivacaine and ropivacaine, mepivacaine, which has a similar pharmacological effect to lidocaine, is the safest among clinically used local anesthetics."( Procaine and mepivacaine have less toxicity in vitro than other clinically used local anesthetics.
Kasaba, T; Onizuka, S; Takasaki, M, 2003
)
1.76
"These results confirm that HTK solution is safe and effective when used in LDLTx."( Safety and efficacy of living donor liver preservation with HTK solution.
Braun, F; Meyers, W; Moritz, M; Ringe, B; Soriano, H; Zeldin, G,
)
0.13
" Specular microscopy performed at 30 days postoperatively showed a significantly greater loss of endothelial cells with the use of VisThesia, suggesting that the 1% lidocaine concentration used in VisThesia may be toxic to corneal endothelial cells."( Safety and efficacy of two ocular anesthetic methods for phacoemulsification: topical anesthesia and viscoanesthesia (VisThesia).
Herasymyuk, O; Ouled-Moussa, R; Perone, JM; Popovici, A; Reynders, S,
)
0.13
" Required amputations, lesion areas, adverse events occurrence and clinical laboratory parameters (hemoglobin, blood cell counts, glycosilated hemoglobin, total proteins, creatinine, alanine transaminase and alkaline phosphatase) were determined during the treatment period."( Tolerability and safety of conventional therapy combination with DeMarco formula for infected ischemic diabetic foot.
Alvarez Duarte, H; Carretero, JH; Fors López, MM; García Mesa, M; Vilas, MM, 2010
)
0.36
"94%) adverse events (mainly cutaneous rash) were reported."( Tolerability and safety of conventional therapy combination with DeMarco formula for infected ischemic diabetic foot.
Alvarez Duarte, H; Carretero, JH; Fors López, MM; García Mesa, M; Vilas, MM, 2010
)
0.36
" Finally, 1000 μg/mL cefazolin showed no adverse effects on porcine kidney endothelial cells."( Antibiotic prophylaxis in (sub)normothermic organ preservation: in vitro efficacy and toxicity of cephalosporins.
Bruinsma, BG; de Boer, L; Heger, M; Post, IC; van Gulik, TM; van Rijssen, LB; Zaat, SA, 2013
)
0.39
" This may contribute to a further increase in the safe use of spinal anesthesia in the clinical setting."( Spinal anesthesia revisited: toxicity of new and old drugs and compounds.
Hampl, K; Steinfeldt, T; Wulf, H, 2014
)
0.4
" To this end we assessed the incidence of patients' preoperative anxiety, perioperative adverse events and patients' and surgeons' satisfaction."( [Simplified topical anesthesia protocol for ambulatory cataract surgery: safety and patient and surgeon satisfaction].
Angioi, K; Batta, B; Fuchs-Buder, T; Tréchot, F, 2014
)
0.4
" An anesthesiologist and nurse anesthetist were present in the area and could intervene in case of an adverse event."( [Simplified topical anesthesia protocol for ambulatory cataract surgery: safety and patient and surgeon satisfaction].
Angioi, K; Batta, B; Fuchs-Buder, T; Tréchot, F, 2014
)
0.4
" Twenty-three adverse events occurred of which 16 required interventions by the anaesthesiologist or surgeon: 5 supplemental local or regional anaesthesia, 6 iv-analgesia, 5 management of hypertension."( [Simplified topical anesthesia protocol for ambulatory cataract surgery: safety and patient and surgeon satisfaction].
Angioi, K; Batta, B; Fuchs-Buder, T; Tréchot, F, 2014
)
0.4
"Continuous pressure-controlled NEVKP is feasible and safe in good quality heart-beating donor kidney grafts."( Eight-Hour Continuous Normothermic Ex Vivo Kidney Perfusion Is a Safe Preservation Technique for Kidney Transplantation: A New Opportunity for the Storage, Assessment, and Repair of Kidney Grafts.
Bagli, DJ; Chun, YM; Echeverri, J; Foltys, DB; Ghanekar, A; Goldaracena, N; Grant, DR; John, R; Kaths, JM; Linares, I; Louis, KS; Mucsi, I; Robinson, LA; Selzner, M; Wiebe, A; Yip, PM, 2016
)
0.43
" Our results suggest that OBPC has a dose- and time-dependent cytotoxicity to HCEP cells by inducing cell cycle arrest and cell apoptosis via a death receptor-mediated mitochondria-dependent proapoptotic pathway, and this novel finding provides new insights into the acute cytotoxicity and its toxic mechanisms of OBPC on HCEP cells."( The cytotoxic effect of oxybuprocaine on human corneal epithelial cells by inducing cell cycle arrest and mitochondria-dependent apoptosis.
Fan, TJ; Fan, WY; Wang, DP; Wen, Q, 2017
)
0.75
" The Committee for the Study of Toxic Effects of Local Anesthetics found procaine, although a safer clinical alternative to cocaine, was capable of causing death when large doses were injected into tissues and advised that it should be used with caution."( Procaine and Local Anesthetic Toxicity: A Collaboration Between the Clinical and Basic Sciences.
Jacob, JS; Kovac, AL,
)
1.81

Pharmacokinetics

The short in vitro half-life of chloroprocaine (11-21 seconds) has been cited to support the safety of this approach. The in vivo half- life after intraperitoneal administration was estimated to be 5.5 seconds.

ExcerptReferenceRelevance
"A multicompartment pharmacokinetic model is presented to describe procaine distribution in humans during and following intravenous infusion."( Pharmacokinetic model for procaine in humans during and following intravenous infusion.
Ferrari, A; Hunt, DH; Seifen, AB; Smith, RH; Thompson, DS, 1979
)
0.8
" Using a two-compartment pharmacokinetic model, disposition kinetics were studied."( Pharmacokinetics of intravenous procaine infusion in humans.
Chapman, J; Ferrari, AA; Seifen, AB; Seifen, EE; Thompson, DS,
)
0.41
"3 mg/Kg) plasma levels peaked at about 400 ng/ml and then declined with a half-life of about 75 minutes."( A review of the pharmacology, pharmacokinetics and behavioral effects of procaine in thoroughbred horses.
Blake, JW; Tobin, T, 1976
)
0.49
" The short in vitro half-life of chloroprocaine (11-21 seconds) has been cited to support the safety of this approach."( Pharmacokinetics and Tolerability of Intraperitoneal Chloroprocaine After Fetal Extraction in Women Undergoing Cesarean Delivery.
Bleyle, LA; Brookfield, K; Koop, D; Togioka, BM; Treggiari, MM; Yanez, ND; Zarnegarnia, Y, 2022
)
1.23
" The primary objective was to define the pharmacokinetic profile of intraperitoneal chloroprocaine, including in vivo half-life."( Pharmacokinetics and Tolerability of Intraperitoneal Chloroprocaine After Fetal Extraction in Women Undergoing Cesarean Delivery.
Bleyle, LA; Brookfield, K; Koop, D; Togioka, BM; Treggiari, MM; Yanez, ND; Zarnegarnia, Y, 2022
)
1.19
"The in vivo half-life of intraperitoneal chloroprocaine (5."( Pharmacokinetics and Tolerability of Intraperitoneal Chloroprocaine After Fetal Extraction in Women Undergoing Cesarean Delivery.
Bleyle, LA; Brookfield, K; Koop, D; Togioka, BM; Treggiari, MM; Yanez, ND; Zarnegarnia, Y, 2022
)
1.22

Compound-Compound Interactions

ExcerptReferenceRelevance
"Tetrodotoxin (TTX), alone and in combination with various vasoconstrictors and local anesthetics, was evaluated for its ability to produce peripheral nerve blocks in the rat and central neural blocks in the cat and dog."( The local anesthetic activity of tetrodotoxin alone and in combination with vasoconstrictors and local anesthetics.
Adams, HJ; Blair, MR; Takman, BH,
)
0.13
"The effect of a collagenous preparation Colocyl and its combination with proteolytic enzymes on the healing of soft tissue purulent wounds were studied in 239 patients."( [Treatment of suppurative wounds of soft tissues with colocyl and its combination with proteolytic enzymes].
Aboiants, RK; Berchenko, GN; Berchenko, VV; Kharitonov, IuK, 1986
)
0.27
"The work deals with the results of SPV in combination with prolonged drug blockade of the celiac plexus in 78 patients with duodenal ulcers."( [Selective proximal vagotomy in combination with prolonged drug blockade of the celiac plexus in the treatment of patients with duodenal ulcers].
Chilikidi, KIu; Gervaziev, VB; Lubianskiĭ, VG, 1993
)
0.29
" 1), a new cisplatin-derived compound, in combination with five conventional anticancer drugs: the antimetabolites 5-fluorouracil (5FU) and methotrexate (MTX), the alkylating agent mitomycin C (MMC), the antimicrotubule agent taxol (TAX) and the intercalating agent of the antracycline group doxorubicin (DOX), against murine P388 leukemic cells."( Effect of the cisplatin-procaine complex DPR in combination with several anticancer agents on murine P388 leukemic cells in vitro and in vivo.
Cafaggi, S; Esposito, M; Mariggiò, MA; Parodi, A; Pastrone, I; Viale, M,
)
0.44
" The purpose of this study was to evaluate clinical efficacy of the TWBC in combination with B-HTK for myocardial protection."( [Efficacy of terminal warm blood cardioplegia in combination with Bretschneider-HTK solution for myocardial protection].
Endoh, M; Hachida, M; Ishitoya, H; Kitamura, M; Koyanagi, H; Morishita, A, 1999
)
0.3
"These data show that COP combined with a mHTK solution represents a potential alternative to complement currently used cold storage techniques for prolonged preservation periods."( Coronary oxygen persufflation combined with HTK cardioplegia prolongs the preservation time in heart transplantation.
Bardakcioglu, O; de Vivie, ER; Fischer, JH; Jeschkeit, S; Kuhn-Régnier, F; Sobottke, R; Switkowski, R, 2000
)
0.31
"To assess safety of topical anesthesia for transpupillary silicone oil removal in combination with cataract surgery."( Topical anesthesia for transpupillary silicone oil removal combined with cataract surgery.
Hugger, P; Jonas, JB; Sauder, G, 2005
)
0.33
"The clinical interventional study included 37 consecutive patients having transpupillary silicone oil removal combined with cataract surgery."( Topical anesthesia for transpupillary silicone oil removal combined with cataract surgery.
Hugger, P; Jonas, JB; Sauder, G, 2005
)
0.33

Bioavailability

ExcerptReferenceRelevance
" absorption rate is nearly a third of that of lidocaine or tetracaine."( Comparative subcutaneous absorption of local anesthetics: lidocaine, procaine and tetracaine.
Lustig, A; Menczel, E; Paran, I; Yacobi, A, 1977
)
0.49
" For instance, hydrolysis of a compound by plasma enzymes can significantly alter the bioavailability of the active compound."( Determination of the stability of drugs in plasma.
Hartman, DA, 2003
)
0.32
"The knowledge on human serum albumin (HSA) binding is of utmost importance as it affects pharmacokinetic behavior and bioavailability of drugs."( Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
Bajusz, D; Balogh, GT; Dargó, G; Müller, J; Simon, K, 2020
)
0.56

Dosage Studied

The dose-response curve of procaine or lignocaine (lidocaine) added to the St. Jude’s drug cocktail was compared to that of 2-chloroprocaine. The results indicate that a pregnant patient may be dosed in the lateral supine position without adversely affecting the caudad or cephalad spread of plain or pH-adjusted 2% 2- chlorine.

ExcerptRelevanceReference
" In contrast other solutions, such as the Bretschneider solution, which have extremes of electrolyre concentration, are associated with a complex dose-response relationship."( Protection of the ischemic myocardium. Volume-duration relationships and the efficacy of myocardial infusates.
Braimbridge, MV; Hearse, DJ; Jynge, P, 1978
)
0.26
" The dose-response relationship revealed that procaine inhibited the resting membrane conductance almost completely in a one-to-one manner with the dissociation constant of about 1 mM."( The effect of procaine on the passive electrical properties of guinea-pig ventricular muscle.
Hashimoto, K; Ochi, R, 1978
)
0.88
" Analyes of dose-response relation in suppressing peak transient and steady-state conductances show that trichloroethylene interacts with receptor on a one-to-one stoichiometric basis."( Mode of action of trichloroethylene on squid axon membranes.
Kitz, RJ; Narahashi, T; Roberts, JD; Shrivastav, BB, 1976
)
0.26
" High frequency and long duration of block can be attained if sufficiently high concentrations of TTX are used, although latency is long and high dosage may produce systemic toxicity."( The local anesthetic activity of tetrodotoxin alone and in combination with vasoconstrictors and local anesthetics.
Adams, HJ; Blair, MR; Takman, BH,
)
0.13
" For example, intermittent application of a particular dosage results in lower blood levels, and allowing sufficient time between doses reduces the amount necessary to obtain the desired anesthesia."( Local anesthesia in otolaryngology. A re-evaluation.
Schenck, NL,
)
0.13
" This dosage was doubled to 10 ml per injection during the second six weeks."( Effects of a procaine preparation (Gerovital H3) in hospitalized geriatric patients: a double-blind study.
Grossman, J; Hotz, M; Kling, R; Plutchik, R; Rubin, L; Siegel, B; Zwerling, I, 1975
)
0.62
" The beginning dosage of medication should be lower than for younger patients, and elderly patients must be monitored carefully for side effects."( Depression in elderly patients.
Fann, WE; Wheless, JC, 1975
)
0.25
" Dose-response curves determined in nonpregnant ewes indicate that significant decreases in blood flow may occur at arterial blood concentrations encountered clinically."( Effects of local anesthetic agents on the uterine vasculatures and myometrium.
Anderson, SG; Greiss, FC; Still, JG, 1976
)
0.26
"A simple and rapid spectrophotometric procedure has been developed for the determination of four local anaesthetics containing a free primary amine moiety and of procainamide hydrochloride as the drug substances and in dosage forms."( Use of 7,7,8,8-tetracyanoquinodimethane for spectrophotometric determination of certain local anaesthetics and procainamide hydrochloride.
Hassan, HY; Hussein, SA; Mohamed, AM; Mohamed, HA, 1991
)
0.28
" The dose-response curves for left atrial and pulmonary artery injection of 1-PBG were shifted successively to the right by intravenous infusion of the 5-HT3 antagonist MDL72222 (0."( Characteristics of cardiovascular reflexes originating from 5-HT3 receptors in the heart and lungs of unanaesthetized rabbits.
Evans, RG; Ludbrook, J; Michalicek, J, 1990
)
0.28
" Our observations thus support the conclusions of other workers who used mixtures of two local anesthetics to show that the dose-response behavior does not fit single-site behavior, but requires at least two distinct sites."( Isochannels and blocking modes of voltage-dependent sodium channels.
Guo, X; Heiny, J; Moczydlowski, E; Uehara, A, 1986
)
0.27
" Analysis of cumulative dose-response curves showed that the two local anesthetics antagonized methoxamine and inhibited the field-stimulation response."( Effects of lidocaine and procaine on canine nasal blood vessels.
Jackson, RT; Wang, HW,
)
0.43
" There was no significant difference between groups in median duration of subsequent bupivacaine analgesia (60 min in each group) or mean (+/- SD) dosage of bupivacaine during the first stage of labor (64 +/- 43 versus 72 +/- 57 mg)."( The influence of pH-adjusted 2-chloroprocaine on the quality and duration of subsequent epidural bupivacaine analgesia during labor: a randomized, double-blind study.
Bates, JN; Chestnut, DH; Choi, WW; Geiger, M, 1989
)
0.55
" Our results indicate that a pregnant patient may be dosed in the lateral supine position without adversely affecting the caudad or cephalad spread of plain or pH-adjusted 2% 2-chloroprocaine, which is clinically important because the incidence of aortocaval compression is increased in the supine position when compared with the lateral supine position."( The effect of pH-adjusted 2-chloroprocaine on the onset of epidural analgesia in pregnant patients in the lying and sitting position during the first stage of labor.
Ackerman, WE; Denson, DD; Juneja, MM; Kaczorowski, DM; Nicholson, CJ; Sarracino, SM; Schipper, J, 1989
)
0.75
" Dose-response curves were constructed from the data obtained, and the CD50 and LD50 values for each local anesthetic alone and in combination with each of the vasoconstrictors were calculated by probit analysis."( Modification of local anesthetic toxicity by vasoconstrictors.
Dorris, RL; Taylor, SE,
)
0.13
" Cardiotoxicity associated with bupivacaine is related not to the concentration employed but to the total dosage administered as a rapid intravenous injection."( Is there a need for chloroprocaine 3% and bupivacaine 0.75%?
Covino, BG, 1988
)
0.58
" 1) H2O2 dissolved in different concentrations produced arterial contractions similar to those by equimolar Oxy-Hb, showing similar dose-response curves."( [On the mechanism underlying spasmogenic actions of oxy-hemoglobin on the cerebral artery, analyzed from the inhibitory effects of nicardipine, procaine and indomethacin].
Doi, M, 1988
)
0.48
" We retrospectively reviewed all our consultations for evaluation of local anesthetic allergy from 1965 to 1985 to assess the safety and efficacy of skin testing and provocative test dosing with a variety of local anesthetic agents."( Provocative challenge with local anesthetics in patients with a prior history of reaction.
Chandler, MJ; Grammer, LC; Patterson, R, 1987
)
0.27
"5 kg) at an average dosage of 30 mg (1."( Spinal fluid concentrations of mepivacaine in horses and procaine in cows after thoracolumbar subarachnoid analgesia.
Ibrahim, AI; Muir, WW; Skarda, RT, 1985
)
0.51
" The dose-response and time-action parameters of the cardiac antiarrhythmic protection afforded by the prototype drugs and their acryloyl derivatives against chloroform-hypoxia-induced cardiac arrhythmias in unanesthetized mice and epinephrine-induced arrhythmias in alpha-chloralose anesthetized cats were determined."( Prolongation of procaine's and procainamide's actions by binding to acryloyl polymers.
Baker, T; Erker, EF; Okamoto, M; Riker, WF; Udenfriend, S, 1985
)
0.62
" Procaine administered in a dosage (5 x 10(-3) W/V)which would suppress the contracture due to caffeine (10 mM), did not modify the tension developed during the hyperpolarization."( Muscle contraction during hyperpolarizing currents in the crab.
García, H; Uchitel, OD, 1974
)
1.16
" Log dose-response curves to oxotremorine and acetylcholine were similar and both drugs were competitively antagonized by atropine."( Investigation of the mechanism of action of oxotremorine on the guinea-pig isolated ileum preparation.
Cox, B; Hecker, SE, 1971
)
0.25
" The effect of d-TC and local anaesthetics on the dose-response relationship between ionophoretically applied L-glutamate and synaptic current suggested that both acted as non-competitive inhibitors."( Voltage-dependent drug blockade of L-glutamate activated channels of the crayfish.
Dekin, MS; Edwards, C, 1983
)
0.27
" Urine samples were collected from the dogs twice daily before dosing, during the dosing period, and for 4 days after final dose administration."( Procaine in the urine of racing Greyhounds: possible sources.
Dorvil, MG; Duer, WC; Gancarz, T; Hill, DW; Rosen, P; Sundlof, SF, 1983
)
1.71
" Protoveratrine A increased the uptake of 22Na+ into the slices with a similar dose-response curve to that found for gamma-aminobutyrate release."( The role of Ca2+ in the protoveratrine-induced release of gamma-aminobutyrate from rat brain slices.
Minchin, MC, 1980
)
0.26
"The dose-response curve of procaine or lignocaine (lidocaine) added to the St."( Protection of the myocardium during ischemic arrest. Dose-response curves for procaine and lignocaine in cardioplegic solutions.
Braimbridge, MV; Hearse, DJ; O'Brien, K, 1981
)
0.79
" In all cases, chloroprocaine was chosen because of preexisting or associated conditions that might increase the risk of bupivacaine toxicity, such as hepatic resection, repeated dosing in a neonate, or the need for higher concentrations of local anesthetic to achieve adequate surgical conditions."( Chloroprocaine for epidural anesthesia in infants and children.
O'Dell, N; Tobias, JD, 1995
)
1.09
" For concentrations of eugenol in the upper range of the dose-response curve (10 mM), the contracture was independent of the Ca++ concentration in the medium."( Effects of eugenol on excitation-contraction coupling in skeletal muscle.
Coelho-de-Souza, AN; Figueiredo, IM; Leal-Cardoso, JH; Souza, IT,
)
0.13
" Dose-response curves for net fluid secretion (stimulated-basal (30 min)-1) activated by 5,50 and 500 ng ml-1 STa were obtained for jejuna and ilea from fed, starved and chronically undernourished rats."( Fluid hypersecretion induced by enterotoxin STa in nutritionally deprived rats: jejunal and ileal dynamics in vivo.
Levin, RJ; Nzegwu, HC, 1994
)
0.29
" A tetracaine dose-response curve for HVA-ICa indicated an apparent dissociation constant of 79."( Local anesthetics depress the calcium current of rat sensory neurons in culture.
Muteki, T; Sugiyama, K, 1994
)
0.29
" Dose-response curves were plotted for each drug."( Duration of spinal anaesthesia is determined by the partition coefficient of local anaesthetic.
Benita, S; Golomb, E; Grant, GJ; Langerman, L, 1994
)
0.29
" Correlates of neural activation in the neocortex displayed an inverse dose-response curve to that found in the hippocampus; the time-to-peak effect was shorter (6-43 min) and the maximal change was reduced."( Imaging of hippocampal and neocortical neural activity following intravenous cocaine administration in freely behaving cats.
Harper, RM; Poe, GR; Rector, DM, 1993
)
0.29
" The effect of two cardioplegic solution was evaluated by postoperative cardiac function (CI, %SF), released enzymes (CPK), histology and dosage of catecholamine."( [Efficacy of myocardial preservation using HTK solution in continuous 120 min cross-clamping method--a comparative study with GIK method].
Bonkohara, Y; Hachida, M; Imamaki, M; Katsumata, T; Koyanagi, H; Nemoto, S; Nonoyama, M; Saitou, S; Satou, M; Toyama, A, 1993
)
0.29
" The optimized methods show good linearity, precision (RSD < 2%) and accuracy (bias < 2% for dosage forms)."( Validation of high-performance liquid chromatographic methods on two silica base-deactivated reversed phases for the determination of chloroprocaine and bupivacaine.
Brun, F; Veuthey, JL, 1996
)
0.5
"3 mM), at approximately twice the equimolar dosage of cocaine, produced apneustic breathing that was indistinguishable from that produced by cocaine."( Cardiorespiratory effects of cocaine and procaine at the ventral brainstem.
Dehkordi, O; Dennis, GC; Millis, RM; Trouth, CO, 1996
)
0.56
" Particular attention was focused on the aspects of dose-response relationship, temperature sensitivity, and ischemic tolerance."( Effect of the potassium-channel opener nicorandil as an adjunct to cardioplegia on myocardial preservation in isolated rabbit hearts.
Sunamori, M; Wang, Y; Yoshida, T, 1996
)
0.29
" In addition, the slope factor (steepness) of the dose-response relation was lowered 4-fold."( Norepinephrine-mediated calcium signaling is altered in vascular smooth muscle of diabetic rat.
Bielefeld, DR; Cohen, RM; Ferguson, DG; Lorenz, JN; Pun, RY; Tam, ES, 1997
)
0.3
" Oxethazaine shifted the carbachol dose-response curves to the right with suppression of maximal response."( Effect of procaine and oxethazaine on muscarinic receptors of parietal cells.
Kimura, N; Miwa, T; Miyazawa, M; Muramatsu, S; Suzuki, T; Tani, N; Watanabe, Y, 1997
)
0.7
" Dose-response studies revealed procaine hydrochloride pretreated 3 min before KCN, at doses of 18."( Effect of procaine hydrochloride on cyanide intoxication and its effect on neuronal calcium in mice.
Jiang, S; Liu, Z; Zhuang, X, 1998
)
0.99
" Dose-response curves were made for each of the additives (n> or =4 for each dose)."( Improving the preservation of isolated rat skeletal muscles stored for 16 hours at 4 degrees C.
Bär, DP; de Smet, M; de With, MC; Kon, M; Kroese, AB; van der Heijden, EP; Werker, PM, 2000
)
0.31
" We compared spinal versus systemic dose-response to L-NAME, and examined effects of intrathecal arginine on tachyphylaxis."( Evidence that spinal segmental nitric oxide mediates tachyphylaxis to peripheral local anesthetic nerve block.
Berde, CB; DiCanzio, J; Sholas, MG; Wang, C; Wilder, RT; Zurakowski, D, 2001
)
0.31
" The comparison of the information content of a number of methods--skin testing, dosed provocation, leukocyte alteration test and chemiluminescence--for revealing increased sensitivity to novocain in 30 persons with adverse reactions to this preparation registered in their medical history."( [Investigation on the mechanisms of leukocyte alteration in patients with intolerance to some drugs (with novocaine as a model)].
Gervazieva, VB; Kuznetsova, NM; Stepanova, EV; Sveranovskaia, VV,
)
0.13
" Subjective responses increased in a dose-response manner."( Dose-response measures of rCBF and subjective changes following procaine in healthy female volunteers.
Adinoff, B; Alexander, D; Best, SE; Devous, MD; Kelly Payne, J; Williams, M, 2002
)
0.55
" The assays were shown to be suitable for measuring epinephrine-prilocaine and epinephrine-procaine combinations in their respective injection dosage forms."( Stability-indicating HPLC assays for the determination of prilocaine and procaine drug combinations.
Stewart, JT; Storms, ML, 2002
)
0.77
" Log dose-response curves were plotted for quinidine, papaverine, procaine, dibenamine and procaine amide."( A comparison of tests for antifibrillatory action.
SZEKERES, L; WILLIAMS, EM, 1961
)
0.48
" We examined the safety, dose-response characteristics, and effects of epinephrine with spinal 2-CP."( Spinal 2-chloroprocaine: a dose-ranging study and the effect of added epinephrine.
Kopacz, DJ; McDonald, SB; Smith, KN, 2004
)
0.68
" The average dosage of, respectively, procaine benzylpenicillin (I."( Pharmacological and toxicological aspects of combination of beta-lactam and aminoglycoside antibiotic, prednisolone and procaine hydrochloride on the example of Vetramycin.
Kania, BF; Kania, K, 2003
)
0.8
" One aspect of this study will investigate the possibility of reducing the dosage of zidovudine required if it is used in combination with Anticort."( Procaine oral stabilised--Samaritan pharmaceuticals: SP-01, SP001.
, 2004
)
1.77
" In our study we compared myocardial protection in isolated coronary bypass with a short period of ischemia using low dosage HTK and cold crystalloid cardioplegia."( Low-dose histidine-tryptophan-ketoglutarate solution for myocardial protection.
Akay, T; Arslan, A; Aslamaci, S; Gultekin, B; Ozkan, S; Sezgin, A; Tasdelen, A; Uguz, E, 2005
)
0.33
"We evaluated the dose-response relationship of 2-chloroprocaine for lower limb outpatient procedure in 45 ASA physical status I-II outpatients undergoing elective lower limb surgery under spinal anesthesia, with 30 mg (group Chlor-30, n = 15), 40 mg (group Chlor-40, n = 15), or 50 mg (group Chlor-50, n = 15) of 1% preservative free 2-chloroprocaine."( Intrathecal 2-chloroprocaine for lower limb outpatient surgery: a prospective, randomized, double-blind, clinical evaluation.
Benassi, C; Berti, M; Casati, A; Danelli, G; Fanelli, A; Fanelli, G; Fioro, A; Petronella, G, 2006
)
0.9
" Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process."( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential.
Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A,
)
0.13
" After rats were injected intrathecally with proxymetacaine, oxybuprocaine, bupivacaine, and lidocane, dose-response curves were constructed."( Intrathecal oxybuprocaine and proxymetacaine produced potent and long-lasting spinal anesthesia in rats.
Chen, YC; Chen, YW; Chu, CC; Hung, CH; Wang, JJ, 2009
)
0.93
" Moreover, for continuous perfusion preservation the dosage of the lipophilic chelator LK 614 should probably be lower than for static cold storage."( Use of a new modified HTK solution for machine preservation of marginal liver grafts.
Hirner, A; Minor, T; Rauen, U; Stegemann, J, 2010
)
0.36
"To compare a surgically adjusted dose of strabismus surgery using topical anesthesia in cooperative patients with dosage guidelines adapted to the surgeon's personal technique using sub-Tenon's anesthesia."( Surgery for esotropia under topical anesthesia.
Ogallar, C; Rodríguez, JM; Tejedor, J, 2010
)
0.36
" The last one was reported on the 15th day of treatment and DMF dosing was discontinued by patient's request."( Tolerability and safety of conventional therapy combination with DeMarco formula for infected ischemic diabetic foot.
Alvarez Duarte, H; Carretero, JH; Fors López, MM; García Mesa, M; Vilas, MM, 2010
)
0.36
"The solid-state properties of pharmaceutical salts, which are dependent on the counterion used to form the salt, are critical for successful development of a stable dosage form."( Analysis of relationships between solid-state properties, counterion, and developability of pharmaceutical salts.
Guerrieri, P; Li, T; Rumondor, AC; Taylor, LS, 2010
)
0.36
" Forty rats were treated with procain-HCl intravenously at a dosage of 2 mg/kg body weight/h either at or 1 h after induction of pancreatitis."( Effect of procainhydrochloride on phospholipase A2 catalytic activity in sodium taurocholate-induced acute experimental pancreatitis in rats.
Kahl, S; Malfertheiner, P; Mayer, J; Nevalainen, TJ; Peuravuori, H; Pross, M; Schuette, K; Schulz, HU, 2010
)
0.36
" During preservation, in the periods of zero, 12, 18 and 24 hours, were conducted evaluating the degree of mucosal injury and dosage of malondialdehyde acid (MDA)."( Effects of ischemic preconditioning associated to different preservation solutions in protecting the intestinal graft.
Abrahão, Mde S; Gonzalez, AM; Montero, EF; Neves, Jde S; Salzedas Netto, AA, 2011
)
0.37
" The dosage of 5 mg ketamine/kg body mass was rarely sufficient to obtain surgical tolerance in group INJE."( [Comparison of three different anesthesia procedures in calves with respect to possible pain-associated reactions].
Hefti, A; Metzner, M; Sauter-Louis, C; Schlemmer, I,
)
0.13
" Duration of epidural infusion did not influence dosing requirement, suggesting the absence of drug tachyphylaxis."( Evaluation of prolonged epidural chloroprocaine for postoperative analgesia in infants.
Bielsky, AR; Murphy, ME; Reiter, PD; Ross, EL, 2015
)
0.69
" The aim of this trial was to determine the optimal dosage of chloroprocaine for this indication."( Chloroprocaine 10 mg/ml for low-dose spinal anaesthesia in perianal surgery - a randomised dose finding study.
Bussen, D; Gebhardt, V; Mueller-Hansen, L; Schmittner, MD; Schwarz, A; Weiss, C, 2017
)
1.17
" Dosing regimens are presented and the applications of 2-chloroprocaine in this population are discussed."( Chloroprocaine for epidural anesthesia in infants and children.
Tobias, JD; Veneziano, G, 2017
)
1.18
" These results provide approaches to apply longer acting LA with a higher analgesic potency in an appropriate dosage and with an appropriate method of application."( [Pain and distress response of suckling piglets to injection and castration under local anaesthesia with procaine and licocaine - Part 2: Defence behaviour, catecholamines, coordination of movements].
Harlizius, J; Hofmann, K; Numberger, J; Otten, W; Rauh, A; Ritzmann, M; Scholz, T; Schulze-Horsel, T; Weiß, C; Zöls, S, 2019
)
0.73
" Current results cannot be extrapolated to repeated dosing or prolonged infusion."( Evaluation of neurotoxicity and long-term function and behavior following intrathecal 1 % 2-chloroprocaine in juvenile rats.
Eddinger, K; Grafe, MR; Malkmus, S; Powell, SB; Roberts, AJ; Shubayev, VI; Steinauer, J; Walker, SM; Yaksh, TL, 2022
)
0.94
" Therefore, our study suggests that intraperitoneal chloroprocaine, in a dosage ≤1200 mg, administered after fetal extraction, is well tolerated during cesarean delivery."( Pharmacokinetics and Tolerability of Intraperitoneal Chloroprocaine After Fetal Extraction in Women Undergoing Cesarean Delivery.
Bleyle, LA; Brookfield, K; Koop, D; Togioka, BM; Treggiari, MM; Yanez, ND; Zarnegarnia, Y, 2022
)
1.21
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
local anaestheticAny member of a group of drugs that reversibly inhibit the propagation of signals along nerves. Wide variations in potency, stability, toxicity, water-solubility and duration of action determine the route used for administration, e.g. topical, intravenous, epidural or spinal block.
central nervous system depressantA loosely defined group of drugs that tend to reduce the activity of the central nervous system.
peripheral nervous system drugA drug that acts principally at one or more sites within the peripheral neuroeffector systems, the autonomic system, and motor nerve-skeletal system.
drug allergenAny drug which causes the onset of an allergic reaction.
[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 (3)

ClassDescription
benzoate esterEsters of benzoic acid or substituted benzoic acids.
substituted aniline
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
[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]

Pathways (1)

PathwayProteinsCompounds
Procaine Action Pathway3111

Protein Targets (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency0.39810.100020.879379.4328AID588453
thyroid stimulating hormone receptorHomo sapiens (human)Potency39.81070.001318.074339.8107AID926; AID938
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency23.77810.035520.977089.1251AID504332
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency24.90530.00207.533739.8107AID891
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.81070.251215.843239.8107AID504327
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency15.95410.00106.000935.4813AID943; AID944
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1449628
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (22)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (151)

Assay IDTitleYearJournalArticle
AID1878517Anesthetic activity in mouse assessed as loss of righting efflux administered as single injection via caudal vein2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID350219Lipophilicity, log K at pH 2 by by hydrophilic interaction chromatography using 95% acetonitrile as mobile phase2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1878532Toxicity in iv dosed rat assessed as convulsion administered continuously2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID655939Positive chronotropic activity in guinea pig spontaneously beating right atria assessed as decrease in atrial rate at 10'-4 M relative to control2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Synthesis and toxicopharmacological evaluation of m-hydroxymexiletine, the first metabolite of mexiletine more potent than the parent compound on voltage-gated sodium channels.
AID655940Negative inotropic activity in guinea pig left atria assessed as decrease of 1 Hz current-induced developed tension2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Synthesis and toxicopharmacological evaluation of m-hydroxymexiletine, the first metabolite of mexiletine more potent than the parent compound on voltage-gated sodium channels.
AID19262Aqueous solubility2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
Prediction of drug solubility from Monte Carlo simulations.
AID527493Octanol-water partition coefficient, log P of the compound after partitioning between 0.1 M NaOH and 1-octanol by deuterium-free NMR method2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
A practical deuterium-free NMR method for the rapid determination of 1-octanol/water partition coefficients of pharmaceutical agents.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1529187Binding affinity to human serum albumin assessed as change in dissociation constant pKa2 of compound in aqueous medium to presence of human serum albumin by UV-pH titration based spectrophotometric analysis2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID1878547Cardiotoxicity in iv dosed rat assessed as morphological change in heart administered continuously2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID1529183Protein binding in immobilized human serum albumin after 15 mins by HPLC analysis2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID527494Octanol-water partition coefficient, log P of the compound2010Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22
A practical deuterium-free NMR method for the rapid determination of 1-octanol/water partition coefficients of pharmaceutical agents.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1878527Toxicity in mouse assessed as adverse effect at 1.5 times ED50, iv2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID91481Binding constant against human serum albumin (HSA)2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Cheminformatic models to predict binding affinities to human serum albumin.
AID1576817Half-life in human plasma at 250 uM incubated for 24 hrs and measured up to 24 hrs by LC-MS analysis2019Journal of medicinal chemistry, 08-22, Volume: 62, Issue:16
Cyclization of RGD Peptides by Suzuki-Miyaura Cross-Coupling.
AID23271Partition coefficient (logD7.4)1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Structure-activity relationships of antineoplastic agents in multidrug resistance.
AID71803Tonic inhibition of compound action potential by 50% was determined in the absence of avidin in desheathed frog sciatic nerves1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Limited nerve impulse blockade by "leashed" local anesthetics.
AID1135965Inhibition of beta1-adrenergic receptor in guinea pig auricle assessed as reversal of isoproterenol-induced effect1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
Adrenoceptor blocking agents. 2. 2-(alpha-Hydroxyarylmethyl)-3,3-dimethylaziridines, a new class of selective beta2-adrenoceptor antagonists.
AID45741Collateral sensitivity of CHRC5 cells to local anesthetics/steroids as log of ratio of molar concentration of drug inducing 50% growth inhibition in CHO AUXB1 cells to that of CHRC5 cells1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Structure-activity relationships of antineoplastic agents in multidrug resistance.
AID205267Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID1878544Cardiotoxicity in iv dosed rat assessed as change in LDH level administered continuously2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID450269Displacement of [3H]-BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Ligand-based design and synthesis of novel sodium channel blockers from a combined phenytoin-lidocaine pharmacophore.
AID384955Intrinsic aqueous solubility at pH 10 by shake-flask method2008Journal of medicinal chemistry, May-22, Volume: 51, Issue:10
Molecular characteristics for solid-state limited solubility.
AID1878539Hepatotoxicity in iv dosed rat assessed as change in ALT level administered continuously2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID1878543Cardiotoxicity in iv dosed rat assessed as change in alpha-HBDH level administered continuously2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1711033Metabolic stability in rat plasma assessed as parent compound remaining at 10 uM measured after 2 hrs2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
In vitro synergistic anticancer activity of the combination of T-type calcium channel blocker and chemotherapeutic agent in A549 cells.
AID1849442Stability in mouse plasma assessed as half life and measured after 120 mins by LC-MS/MS analysis
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID237685Lipophilicity determined as logarithm of the partition coefficient in the alkane/water system2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Calculating virtual log P in the alkane/water system (log P(N)(alk)) and its derived parameters deltalog P(N)(oct-alk) and log D(pH)(alk).
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID655942Vasorelaxant activity in potassium depolarized guinea pig aortic strip assessed as inhibition of calcium-induced contraction at 10'-4 M2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Synthesis and toxicopharmacological evaluation of m-hydroxymexiletine, the first metabolite of mexiletine more potent than the parent compound on voltage-gated sodium channels.
AID395328Lipophilicity, log P of the compound2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID1878521Anesthetic activity in mouse assessed as reduction in recovery time of righting reflex at 1.5 times ED50, iv2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID1823668Stability in human plasma assessed as parent compound remaining at 10 uM measured after 120 mins by LC-MS analysis2021Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
Discovery of New Imidazo[2,1-
AID350218Octanol-water partition coefficient, log PC of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID350220Lipophilicity, log K at pH 2 by by hydrophilic interaction chromatography using 100% water as mobile phase2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1878542Cardiotoxicity in iv dosed rat assessed as change in CK-MB level administered continuously2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1878529Toxicity in iv dosed rat administered continuously2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID1878534Toxicity in iv dosed rat assessed as cyanosis administered continuously2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID1878516Lipophilicity, log D of the compound2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID319288Induction of chromosomal satellite repeats demethylation in human HL60 cells at 0.5 mM after 72 hrs2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Constrained analogues of procaine as novel small molecule inhibitors of DNA methyltransferase-1.
AID1849440Stability in human plasma assessed as half life and measured after 120 mins by LC-MS/MS analysis
AID1849439Stability in mouse plasma assessed as compound remaining and measured after 120 mins by LC-MS/MS analysis
AID1823667Stability in human plasma assessed as parent compound remaining at 10 uM measured after 30 mins by LC-MS analysis2021Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
Discovery of New Imidazo[2,1-
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1529184Protein binding in immobilized human serum albumin by HPLC analysis2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID781325pKa (acid-base dissociation constant) as determined by Liao ref: J Chem Info Model 20092014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1135973Antiarrhythmic activity against guinea pig auricle1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
Adrenoceptor blocking agents. 2. 2-(alpha-Hydroxyarylmethyl)-3,3-dimethylaziridines, a new class of selective beta2-adrenoceptor antagonists.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1348629Metabolic stability in human plasma at 5 uM after 120 mins by UPLC-MS/MS analysis2018European journal of medicinal chemistry, Jan-01, Volume: 143A fluorine scan of a tubulin polymerization inhibitor isocombretastatin A-4: Design, synthesis, molecular modelling, and biological evaluation.
AID1135963Reversal of isoproterenol-induced increase in mean arterial blood pressure in cat assessed as depressor phase at 2.5 mg/kg, iv1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
Adrenoceptor blocking agents. 2. 2-(alpha-Hydroxyarylmethyl)-3,3-dimethylaziridines, a new class of selective beta2-adrenoceptor antagonists.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1878541Nephrotoxicity in iv dosed rat assessed as change in urea level administered continuously2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID1878530Therapeutic index, ratio of LD50 for toxicity in iv dosed rat to ED50 for anesthetic activity in iv dosed rat2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID631009Inhibition of human recombinant DNMT1 expressed in Sf9 cells assessed as remaining activity at 2 mM after 3 hrs by scintillation counting in presence of [3H]S-adenosyl methionine2011Journal of medicinal chemistry, Nov-10, Volume: 54, Issue:21
Synthesis and biochemical evaluation of δ(2)-isoxazoline derivatives as DNA methyltransferase 1 inhibitors.
AID1878528Anesthetic activity in iv dosed rat assessed as loss of righting efflux administered continuously2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID1529178Dissociation constant, pKa1 of compound in aqueous medium by UV-pH titration based spectrophotometric analysis2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID1135964Inhibition of beta2-adrenergic receptor in guinea pig tracheal chain assessed as reversal of isoproterenol-induced effect after 15 mins1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
Adrenoceptor blocking agents. 2. 2-(alpha-Hydroxyarylmethyl)-3,3-dimethylaziridines, a new class of selective beta2-adrenoceptor antagonists.
AID1061889Displacement of [3H]BTX-B from neuronal voltage-gated sodium channel in rat cerebral cortex synaptoneurosomes after 60 mins by scintillation counting2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
A highly predictive 3D-QSAR model for binding to the voltage-gated sodium channel: design of potent new ligands.
AID1823669Stability in rat plasma assessed as parent compound remaining at 10 uM measured after 30 mins by LC-MS analysis2021Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
Discovery of New Imidazo[2,1-
AID1878519Therapeutic index, ratio of LD50 for toxicity in mouse to ED50 for anesthetic activity in mouse2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID1878548Toxicity in iv dosed rat assessed as body weight loss administered continuously as infusion for 2 weeks2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1135962Reversal of epinephrine-induced increase in mean arterial blood pressure in cat at 2.5 mg/kg, iv1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
Adrenoceptor blocking agents. 2. 2-(alpha-Hydroxyarylmethyl)-3,3-dimethylaziridines, a new class of selective beta2-adrenoceptor antagonists.
AID312895Partition coefficient, log P of the compound2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
High-throughput log P determination by ultraperformance liquid chromatography: a convenient tool for medicinal chemists.
AID1878540Nephrotoxicity in iv dosed rat assessed as change in creatinine level administered continuously2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1878518Toxicity in mouse administered as single injection via caudal vein2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1517043Stability in human plasma assessed as remaining compound at 10 uM incubated for 120 mins by LC-MS analysis
AID1529182Protein binding in plasma (unknown origin)2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID1135972Anesthetic effect in guinea pig at 0.1 % by intradermal wheal method1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
Adrenoceptor blocking agents. 2. 2-(alpha-Hydroxyarylmethyl)-3,3-dimethylaziridines, a new class of selective beta2-adrenoceptor antagonists.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1878546Nephrotoxicity in iv dosed rat assessed as morphological change in kidney administered continuously2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1232353Metabolic stability in mouse plasma assessed as compound remaining incubated for 60 mins (Rvb = 100%)2015Journal of medicinal chemistry, Jul-23, Volume: 58, Issue:14
Identifying Medication Targets for Psychostimulant Addiction: Unraveling the Dopamine D3 Receptor Hypothesis.
AID1878545Hepatotoxicity in iv dosed rat assessed as morphological change in liver administered continuously2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID1878538Hepatotoxicity in iv dosed rat assessed as change in AST level administered continuously2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1878531Toxicity in iv dosed rat assessed as muscle fibrillation administered continuously2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID1849437Stability in human plasma assessed as compound remaining and measured after 120 mins by LC-MS/MS analysis
AID319287Inhibition of human recombinant DNMT1 expressed in Sf9 cells2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Constrained analogues of procaine as novel small molecule inhibitors of DNA methyltransferase-1.
AID350216Dissociation constant, pKa of the compound2009Journal of medicinal chemistry, May-28, Volume: 52, Issue:10
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
AID1878535Toxicity in iv dosed rat assessed as irregular respiratory rhythm administered continuously2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID781326pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1776039Stability of compound in human plasma assessed as half life at 20 uM incubated for 3 hrs by LC-MS (SIM) assay2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Deconstructing Noncovalent Kelch-like ECH-Associated Protein 1 (Keap1) Inhibitors into Fragments to Reconstruct New Potent Compounds.
AID1459073Metabolic stability in human plasma assessed as compound remaining at 100 uM after 4 hrs incubation by LC-MS/MS analysis2017European journal of medicinal chemistry, Jan-05, Volume: 125New potent biaryl sulfate-based hepatitis C virus inhibitors.
AID655934Negative inotropic activity in guinea pig left atria assessed as decrease of 1 Hz current-induced developed tension at 5 x 10'-7 M relative to control2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Synthesis and toxicopharmacological evaluation of m-hydroxymexiletine, the first metabolite of mexiletine more potent than the parent compound on voltage-gated sodium channels.
AID603957Octanol-water partition coefficient, log P of the compound2008European journal of medicinal chemistry, Apr, Volume: 43, Issue:4
QSPR modeling of octanol/water partition coefficient for vitamins by optimal descriptors calculated with SMILES.
AID1529185Protein binding in human serum albumin after 4.5 hrs by LC-MS based rapid equilibrium dialysis method2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID1135978Reversal of isoproterenol-induced increase in mean arterial blood pressure in cat assessed as pressor phase at 2.5 mg/kg, iv1978Journal of medicinal chemistry, Jan, Volume: 21, Issue:1
Adrenoceptor blocking agents. 2. 2-(alpha-Hydroxyarylmethyl)-3,3-dimethylaziridines, a new class of selective beta2-adrenoceptor antagonists.
AID1517045Stability in rat plasma assessed as remaining compound at 10 uM incubated for 120 mins by LC-MS analysis
AID1529181Binding affinity to human serum albumin assessed as dissociation constant pKa2 at 1:1 ratio by UV-pH titration based spectrophotometric analysis (Rvb = 11.56 No_unit)2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID450273Lipophilicity, log P of the compound2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Ligand-based design and synthesis of novel sodium channel blockers from a combined phenytoin-lidocaine pharmacophore.
AID395325Lipophilicity, log P by microemulsion electrokinetic chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID1823670Stability in rat plasma assessed as parent compound remaining at 10 uM measured after 120 mins by LC-MS analysis2021Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10
Discovery of New Imidazo[2,1-
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1517044Stability in rat plasma assessed as remaining compound at 10 uM incubated for 30 mins by LC-MS analysis
AID540235Phospholipidosis-negative literature compound
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID409954Inhibition of mouse brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1529186Binding affinity to human serum albumin assessed as change in dissociation constant pKa1 of compound in aqueous medium to presence of human serum albumin by UV-pH titration based spectrophotometric analysis2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID312896Partition coefficient, log P by UPLC method2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
High-throughput log P determination by ultraperformance liquid chromatography: a convenient tool for medicinal chemists.
AID1517041Stability in human plasma assessed as remaining compound at 10 uM incubated for 30 mins by LC-MS analysis
AID1878533Toxicity in iv dosed rat assessed as muscular rigidity administered continuously2022Bioorganic & medicinal chemistry letters, 03-15, Volume: 60Design, synthesis and biological evaluation of novel procaine derivatives for intravenous anesthesia.
AID1529179Dissociation constant, pKa2 of compound in aqueous medium by UV-pH titration based spectrophotometric analysis2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID1529180Binding affinity to human serum albumin assessed as dissociation constant pKa1 at 1:1 ratio by UV-pH titration based spectrophotometric analysis (Rvb = 3.87 No_unit)2020Journal of medicinal chemistry, 02-27, Volume: 63, Issue:4
Human Serum Albumin Binding in a Vial: A Novel UV-pH Titration Method To Assist Drug Design.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID515780Intrinsic solubility of the compound in water2010Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
QSAR-based solubility model for drug-like compounds.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1711030Metabolic stability in human plasma assessed as parent compound remaining at 10 uM measured after 2 hrs2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
In vitro synergistic anticancer activity of the combination of T-type calcium channel blocker and chemotherapeutic agent in A549 cells.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508628Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8,596)

TimeframeStudies, This Drug (%)All Drugs %
pre-19906875 (79.98)18.7374
1990's756 (8.79)18.2507
2000's477 (5.55)29.6817
2010's376 (4.37)24.3611
2020's112 (1.30)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 67.22

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 Index67.22 (24.57)
Research Supply Index9.23 (2.92)
Research Growth Index4.27 (4.65)
Search Engine Demand Index134.90 (26.88)
Search Engine Supply Index2.19 (0.95)

This Compound (67.22)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials323 (3.26%)5.53%
Reviews193 (1.95%)6.00%
Case Studies263 (2.66%)4.05%
Observational12 (0.12%)0.25%
Other9,106 (92.01%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (13)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Prospective Randomized Study to Compare Clinical Outcomes in Patients With Osteomyelitis Treated With Intravenous Antibiotics Versus Intravenous Antibiotics With an Early Switch to Oral Antibiotics [NCT02099240]Early Phase 111 participants (Actual)Interventional2014-03-06Terminated(stopped due to Not enough patient enrollment and lack of staffing)
Low Epidural Anesthesia With Chloroprocaine Versus Lidocaine: a Prospective, Randomized, Double-blinded Multi-centre Clinical Trial in China [NCT02287870]Phase 4120 participants (Actual)Interventional2008-01-31Completed
Intrathecal 60mg Prilocaine, Hyperbaric 40mg 9-chloroprocaine and 10.5mg Bupivacaine Each With Added Sufentanil (2µg) for Elective Ambulatory Umbilical and Unilateral Inguinal Herniorrhaphy [NCT02813382]101 participants (Actual)Observational2015-08-31Completed
Chloroprocaine Lavage to Improve Outcomes Related to Operative Cesarean Delivery [NCT03760718]Early Phase 115 participants (Anticipated)Interventional2019-09-30Active, not recruiting
Simplified Antibiotic Regimens for the Management of Sepsis in Young Infants in First-level Facilities: Randomized Controlled Trial [NCT01027429]Phase 32,543 participants (Actual)Interventional2009-12-31Completed
Randomized Controlled Trial of Intramuscular Ceftriaxone Versus Procaine Penicillin Versus Cotrimoxazole and Gentamicin for Management of Serious Bacterial Infections in Young Infants in Community Settings [NCT00189384]Phase 3426 participants Interventional2003-11-30Active, not recruiting
Efficacy and Safety of FORRAD® for the Management of Radiation-induced Mucositis in Patients With Nasopharyngeal Carcinoma Receiving IMRT: A Single-center, Randomized Controlled Trial [NCT02735317]Phase 290 participants (Anticipated)Interventional2016-04-30Not yet recruiting
Determination of the Minimum Local Anesthetic Dose (MLAD) of Spinal Chloroprocaine for Inguinal Herniorrhaphy in Ambulatory Surgery [NCT03805503]Phase 412 participants (Actual)Interventional2015-09-16Completed
Clinical and Radiographic Evaluation of Pulpotomy Technique for Preserving Vitality of Traumatized Anterior Permanent Immature Teeth: A Randomized Clinical Trial [NCT03838068]Phase 2/Phase 333 participants (Actual)Interventional2017-01-18Completed
The Maternal CLIMB Trial: Chloroprocaine to Reduce the Impact of Motor Block on Patient Recovery After Short Obstetric Surgery [NCT03967288]Phase 427 participants (Actual)Interventional2019-10-24Suspended(stopped due to Four patients required conversion to GETA (2 in each study arm))
Decision Support for Intraoperative Low Blood Pressure [NCT02726620]22,435 participants (Actual)Interventional2017-01-05Completed
Evaluation of the Comparative Analgesic Value of Adductor Canal Block Versus Femoral Block Following Total Knee Arthroplasty [NCT03395990]16 participants (Actual)Interventional2016-03-27Completed
Randomized, Multi-center, Double-blind, Two-armed, Parallel Active Groups, Prospective Trial, to Evaluate, in Pediatric Population, the Efficacy and Safety of Chloroprocaine 1% and 2% for Peripheral Nerve Block. [NCT03918798]Phase 2174 participants (Anticipated)Interventional2019-02-14Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT02726620 (43) [back to overview]30-day Mortality
NCT02726620 (43) [back to overview]Average Use of Cardiovascular Drugs: Ephedrine
NCT02726620 (43) [back to overview]Average Use of Cardiovascular Drugs: Epinephrine
NCT02726620 (43) [back to overview]Average Use of Cardiovascular Drugs: Glycopyrrolate
NCT02726620 (43) [back to overview]Average Use of Cardiovascular Drugs: Norepinephrine
NCT02726620 (43) [back to overview]Average Use of Cardiovascular Drugs: Phenylephrine
NCT02726620 (43) [back to overview]Depth and Duration of Intraoperative Hypotension - Threshold MAP 50 mmHg
NCT02726620 (43) [back to overview]Depth and Duration of Intraoperative Hypotension - Threshold MAP 55 mmHg
NCT02726620 (43) [back to overview]Depth and Duration of Intraoperative Hypotension - Threshold MAP 60 mmHg
NCT02726620 (43) [back to overview]Depth and Duration of Intraoperative Hypotension - Threshold MAP 65 mmHg
NCT02726620 (43) [back to overview]Depth and Duration of Intraoperative Hypotension - Threshold MAP 70 mmHg
NCT02726620 (43) [back to overview]Depth and Duration of Intraoperative Hypotension - Threshold MAP 75 mmHg
NCT02726620 (43) [back to overview]Estimated Intraoperative Blood Loss
NCT02726620 (43) [back to overview]In-hospital Mortality
NCT02726620 (43) [back to overview]Incidence of a MAP < 50 mmHg
NCT02726620 (43) [back to overview]Incidence of a MAP < 50 mmHg for > 10 Minutes
NCT02726620 (43) [back to overview]Incidence of a MAP < 50 mmHg for > 20 Minutes
NCT02726620 (43) [back to overview]Incidence of a MAP < 55 mmHg
NCT02726620 (43) [back to overview]Incidence of a MAP < 55 mmHg for > 10 Minutes
NCT02726620 (43) [back to overview]Incidence of a MAP < 55 mmHg for > 20 Minutes
NCT02726620 (43) [back to overview]Incidence of a MAP < 60 mmHg
NCT02726620 (43) [back to overview]Incidence of a MAP < 60 mmHg for > 10 Minutes
NCT02726620 (43) [back to overview]Incidence of a MAP < 60 mmHg for > 20 Minutes
NCT02726620 (43) [back to overview]Intraoperative Administration of Intravenous Fluids
NCT02726620 (43) [back to overview]Intravenous Anesthetic Drug Use During Intraoperative Hypotension: MAP < 50 mmHg
NCT02726620 (43) [back to overview]Intravenous Anesthetic Drug Use During Intraoperative Hypotension: MAP < 55 mmHg
NCT02726620 (43) [back to overview]Intravenous Anesthetic Drug Use During Intraoperative Hypotension: MAP < 60 mmHg
NCT02726620 (43) [back to overview]Intravenous Anesthetic Drug Use During Intraoperative Hypotension: MAP < 65 mmHg
NCT02726620 (43) [back to overview]Postoperative Rise in Creatinine Levels
NCT02726620 (43) [back to overview]Time to Discharge Readiness at the Postanesthesia Care Unit (PACU)
NCT02726620 (43) [back to overview]Timing of Cardiovascular Drugs for MAP < 50 mmHg
NCT02726620 (43) [back to overview]Timing of Cardiovascular Drugs for MAP < 55 mmHg
NCT02726620 (43) [back to overview]Timing of Cardiovascular Drugs for MAP < 60 mmHg
NCT02726620 (43) [back to overview]Timing of Cardiovascular Drugs for MAP < 65 mmHg
NCT02726620 (43) [back to overview]Usage Frequency of Cardiovascular Drugs: Ephedrine
NCT02726620 (43) [back to overview]Usage Frequency of Cardiovascular Drugs: Ephinephrine
NCT02726620 (43) [back to overview]Usage Frequency of Cardiovascular Drugs: Glycopyrrolate
NCT02726620 (43) [back to overview]Usage Frequency of Cardiovascular Drugs: Norepinephrine
NCT02726620 (43) [back to overview]Usage Frequency of Cardiovascular Drugs: Phenylephrine
NCT02726620 (43) [back to overview]Inhaled Anesthetic Drug Use During Intraoperative Hypotension: MAP < 50 mmHg
NCT02726620 (43) [back to overview]Inhaled Anesthetic Drug Use During Intraoperative Hypotension: MAP < 55 mmHg
NCT02726620 (43) [back to overview]Inhaled Anesthetic Drug Use During Intraoperative Hypotension: MAP < 60 mmHg
NCT02726620 (43) [back to overview]Inhaled Anesthetic Drug Use During Intraoperative Hypotension: MAP < 65 mmHg
NCT03395990 (1) [back to overview]Pain Intensity as Measured by 11-point Verbal Numeric Rating Scale (NRS-11) for Pain.

30-day Mortality

Vanderbilt University Medical Center: combination of in-hospital mortality and 'alive-index' (which checks for visits to the hospital in the electronic healthcare record as indication of being alive at 30 days) (NCT02726620)
Timeframe: 30 days after surgery

InterventionParticipants (Count of Participants)
Usual Care Group511
Hypotension Decision Support143

[back to top]

Average Use of Cardiovascular Drugs: Ephedrine

Cardiovascular drugs as defined under interventions. Average use for each drug will be calculated. Cardiovascular drugs that were given in <1% of cases are not reported, as the average dosages would be meaningless. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionmg (Median)
Usual Care Group20
Hypotension Decision Support15

[back to top]

Average Use of Cardiovascular Drugs: Epinephrine

Cardiovascular drugs as defined under interventions. Average use for each drug will be calculated. Cardiovascular drugs that were given in <1% of cases are not reported, as the average dosage would be meaningless. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionmg (Median)
Usual Care Group1.00
Hypotension Decision Support0.70

[back to top]

Average Use of Cardiovascular Drugs: Glycopyrrolate

Cardiovascular drugs as defined under interventions. Average use for each drug will be calculated. Cardiovascular drugs that were given in <1% of cases are not reported, as the average dosage would be meaningless. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionmg (Median)
Usual Care Group0.40
Hypotension Decision Support0.40

[back to top]

Average Use of Cardiovascular Drugs: Norepinephrine

Cardiovascular drugs as defined under interventions. Average use for each drug will be calculated. Cardiovascular drugs that were given in <1% of cases are not reported, as the average dosage would be meaningless. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionmg (Median)
Usual Care Group0.62
Hypotension Decision Support0.70

[back to top]

Average Use of Cardiovascular Drugs: Phenylephrine

Cardiovascular drugs as defined under interventions. Average use for each drug will be calculated. Cardiovascular drugs that were given in <1% of cases are not reported, as the average dosage would be meaningless. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionmg (Median)
Usual Care Group0.90
Hypotension Decision Support1.30

[back to top]

Depth and Duration of Intraoperative Hypotension - Threshold MAP 50 mmHg

Depth and duration of intraoperative hypotension will be modeled by calculating areas under the threshold for mean arterial pressures (MAPs). Thresholds will vary from 75 mmHg to 50 mmHg in 5 mmHg decrements. Together these variables represent the depth and duration of intraoperative hypotension. To optimize goodness of fit of these variables, the decremental steps may be increased to 10 mmHg and more restrictive lowest and highest thresholds may be chosen for the statistical analysis. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionmmHg*minute (Median)
Usual Care Group19
Hypotension Decision Support19

[back to top]

Depth and Duration of Intraoperative Hypotension - Threshold MAP 55 mmHg

Depth and duration of intraoperative hypotension will be modeled by calculating areas under the threshold for mean arterial pressures (MAPs). Thresholds will vary from 75 mmHg to 50 mmHg in 5 mmHg decrements. Together these variables represent the depth and duration of intraoperative hypotension. To optimize goodness of fit of these variables, the decremental steps may be increased to 10 mmHg and more restrictive lowest and highest thresholds may be chosen for the statistical analysis. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionmmHg*minute (Median)
Usual Care Group23
Hypotension Decision Support23

[back to top]

Depth and Duration of Intraoperative Hypotension - Threshold MAP 60 mmHg

Depth and duration of intraoperative hypotension will be modeled by calculating areas under the threshold for mean arterial pressures (MAPs). Thresholds will vary from 75 mmHg to 50 mmHg in 5 mmHg decrements. Together these variables represent the depth and duration of intraoperative hypotension. To optimize goodness of fit of these variables, the decremental steps may be increased to 10 mmHg and more restrictive lowest and highest thresholds may be chosen for the statistical analysis. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionmmHg*minute (Median)
Usual Care Group57
Hypotension Decision Support52

[back to top]

Depth and Duration of Intraoperative Hypotension - Threshold MAP 65 mmHg

Depth and duration of intraoperative hypotension will be modeled by calculating areas under the threshold for mean arterial pressures (MAPs). Thresholds will vary from 75 mmHg to 50 mmHg in 5 mmHg decrements. Together these variables represent the depth and duration of intraoperative hypotension. To optimize goodness of fit of these variables, the decremental steps may be increased to 10 mmHg and more restrictive lowest and highest thresholds may be chosen for the statistical analysis. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionmmHg*minute (Median)
Usual Care Group96
Hypotension Decision Support86

[back to top]

Depth and Duration of Intraoperative Hypotension - Threshold MAP 70 mmHg

Depth and duration of intraoperative hypotension will be modeled by calculating areas under the threshold for mean arterial pressures (MAPs). Thresholds will vary from 75 mmHg to 50 mmHg in 5 mmHg decrements. Together these variables represent the depth and duration of intraoperative hypotension. To optimize goodness of fit of these variables, the decremental steps may be increased to 10 mmHg and more restrictive lowest and highest thresholds may be chosen for the statistical analysis. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionmmHg*minute (Median)
Usual Care Group273
Hypotension Decision Support235

[back to top]

Depth and Duration of Intraoperative Hypotension - Threshold MAP 75 mmHg

Depth and duration of intraoperative hypotension will be modeled by calculating areas under the threshold for mean arterial pressures (MAPs). Thresholds will vary from 75 mmHg to 50 mmHg in 5 mmHg decrements. Together these variables represent the depth and duration of intraoperative hypotension. To optimize goodness of fit of these variables, the decremental steps may be increased to 10 mmHg and more restrictive lowest and highest thresholds may be chosen for the statistical analysis. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionmmHg*minute (Median)
Usual Care Group485
Hypotension Decision Support417

[back to top]

Estimated Intraoperative Blood Loss

The estimated blood loss in mL during the surgical procedure (NCT02726620)
Timeframe: During the surgical procedure: an expected average of 2 hours

InterventionmL (Median)
Usual Care Group100
Hypotension Decision Support75

[back to top]

In-hospital Mortality

Hospital mortality rate during a single hospital admission after the surgery (NCT02726620)
Timeframe: All postoperative days during a single hospital admission, expected median of 5 days

InterventionParticipants (Count of Participants)
Usual Care Group487
Hypotension Decision Support137

[back to top]

Incidence of a MAP < 50 mmHg

Incidence of a mean arterial pressure (MAP) < 50 mmHg during anesthesia for 1 minute or more. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group7781
Hypotension Decision Support2196

[back to top]

Incidence of a MAP < 50 mmHg for > 10 Minutes

Incidence of a mean arterial pressure (MAP) < 50 mmHg for a cumulative duration of all hypotensive episodes of more than 10 minutes during the anesthetic phase of the procedure. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group1159
Hypotension Decision Support326

[back to top]

Incidence of a MAP < 50 mmHg for > 20 Minutes

Incidence of a mean arterial pressure (MAP) < 50 mmHg for a cumulative duration of all hypotensive episodes of more than 20 minutes during the anesthetic phase of the procedure. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group304
Hypotension Decision Support85

[back to top]

Incidence of a MAP < 55 mmHg

Incidence of a mean arterial pressure (MAP) < 55 mmHg during anesthesia for 1 minute or more. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group10991
Hypotension Decision Support3045

[back to top]

Incidence of a MAP < 55 mmHg for > 10 Minutes

Incidence of a mean arterial pressure (MAP) < 55 mmHg for a cumulative duration of all hypotensive episodes of more than 10 minutes during the anesthetic phase of the procedure. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group3181
Hypotension Decision Support759

[back to top]

Incidence of a MAP < 55 mmHg for > 20 Minutes

Incidence of a mean arterial pressure (MAP) < 55 mmHg for a cumulative duration of all hypotensive episodes of more than 20 minutes during the anesthetic phase of the procedure. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group1223
Hypotension Decision Support284

[back to top]

Incidence of a MAP < 60 mmHg

Incidence of a mean arterial pressure (MAP) < 60 mmHg during anesthesia for 1 minute or more. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group13779
Hypotension Decision Support3798

[back to top]

Incidence of a MAP < 60 mmHg for > 10 Minutes

Incidence of a mean arterial pressure (MAP) < 60 mmHg for a cumulative duration of all hypotensive episodes of more than 10 minutes during the anesthetic phase of the procedure. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group6989
Hypotension Decision Support1723

[back to top]

Incidence of a MAP < 60 mmHg for > 20 Minutes

Incidence of a mean arterial pressure (MAP) < 60 mmHg for a cumulative duration of all hypotensive episodes of more than 20 minutes during the anesthetic phase of the procedure. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group3632
Hypotension Decision Support792

[back to top]

Intraoperative Administration of Intravenous Fluids

Total amount (mL) of intravenous fluids (as defined under interventions) administered during the surgical procedure. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionmL (Median)
Usual Care Group1500.00
Hypotension Decision Support1400.00

[back to top]

Intravenous Anesthetic Drug Use During Intraoperative Hypotension: MAP < 50 mmHg

Average concentrations of propofol infusion rates during MAP < 50 mmHg episodes (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionmcg/kg/min (propofol) (Median)
Usual Care Group65.00
Hypotension Decision Support50.00

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Intravenous Anesthetic Drug Use During Intraoperative Hypotension: MAP < 55 mmHg

Average concentrations of propofol infusion rates during MAP < 55 mmHg episodes (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionmcg/kg/min (propofol) (Median)
Usual Care Group63.95
Hypotension Decision Support50.00

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Intravenous Anesthetic Drug Use During Intraoperative Hypotension: MAP < 60 mmHg

Average concentrations of propofol infusion rates during MAP < 60 mmHg episodes (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionmcg/kg/min (propofol) (Median)
Usual Care Group61.07
Hypotension Decision Support50.00

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Intravenous Anesthetic Drug Use During Intraoperative Hypotension: MAP < 65 mmHg

Average concentrations of propofol infusion rates during MAP < 65 mmHg episodes (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionmcg/kg/min (propofol) (Median)
Usual Care Group60.10
Hypotension Decision Support48.59

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Postoperative Rise in Creatinine Levels

Absolute values for serum creatinine before and after surgery will be compared. When multiple postoperative creatinine measurements are made, the maximum difference is reported. (NCT02726620)
Timeframe: Within 7 days after surgery

Interventionmg/dL (Median)
Usual Care Group0.00
Hypotension Decision Support0.00

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Time to Discharge Readiness at the Postanesthesia Care Unit (PACU)

The time from arriving at the postanesthesia care unit (PACU) until the time the patient is considered ready for discharge (in minutes). (NCT02726620)
Timeframe: A specific time frame on the day of surgery: from the start of admission to the PACU to discharge from the PACU, an expected average of 4 hours

Interventionminutes (Median)
Usual Care Group67
Hypotension Decision Support60

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Timing of Cardiovascular Drugs for MAP < 50 mmHg

Cardiovascular drugs as defined under interventions. Time of first administration of cardiovascular drug relative to the time at which the mean arterial pressure (MAP) drops below 50 mmHg. Per patient the average time to first administration of all hypotensive episodes was calculated. That average time is used as the outcome variable. A negative value indicates that administration occurred before the drop in MAP. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionminutes (Median)
Usual Care Group1
Hypotension Decision Support0

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Timing of Cardiovascular Drugs for MAP < 55 mmHg

Cardiovascular drugs as defined under interventions. Time of first administration of cardiovascular drug relative to the time at which the mean arterial pressure (MAP) drops below 55 mmHg. Per patient the average time to first administration of all hypotensive episodes was calculated. That average time is used as the outcome variable. A negative value indicates that administration occurred before the drop in MAP. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionminutes (Median)
Usual Care Group1
Hypotension Decision Support0.5

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Timing of Cardiovascular Drugs for MAP < 60 mmHg

Cardiovascular drugs as defined under interventions. Time of first administration of cardiovascular drug relative to the time at which the mean arterial pressure (MAP) drops below 60 mmHg. Per patient the average time to first administration of all hypotensive episodes was calculated. That average time is used as the outcome variable. A negative value indicates that administration occurred before the drop in MAP. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionminutes (Median)
Usual Care Group0.8
Hypotension Decision Support1.5

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Timing of Cardiovascular Drugs for MAP < 65 mmHg

Cardiovascular drugs as defined under interventions. Time of first administration of cardiovascular drug relative to the time at which the mean arterial pressure (MAP) drops below 60 mmHg. Per patient the average time to first administration of all hypotensive episodes was calculated. That average time is used as the outcome variable. A negative value indicates that administration occurred before the drop in MAP. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

Interventionminutes (Median)
Usual Care Group2
Hypotension Decision Support1.14

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Usage Frequency of Cardiovascular Drugs: Ephedrine

Cardiovascular drugs as defined under interventions. Frequency of patients receiving the drug. Cardiovascular drugs that were given in <1% of cases are not reported. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group9310
Hypotension Decision Support2718

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Usage Frequency of Cardiovascular Drugs: Ephinephrine

Cardiovascular drugs as defined under interventions. Frequency of patients receiving the drug. Cardiovascular drugs that were given in <1% of cases are not reported. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group1215
Hypotension Decision Support409

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Usage Frequency of Cardiovascular Drugs: Glycopyrrolate

Cardiovascular drugs as defined under interventions. Frequency of patients receiving the drug. Cardiovascular drugs that were given in <1% of cases are not reported. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group11093
Hypotension Decision Support1257

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Usage Frequency of Cardiovascular Drugs: Norepinephrine

Cardiovascular drugs as defined under interventions. Frequency of patients receiving the drug. Cardiovascular drugs that were given in <1% of cases are not reported. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group762
Hypotension Decision Support233

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Usage Frequency of Cardiovascular Drugs: Phenylephrine

Cardiovascular drugs as defined under interventions. Frequency of patients receiving the drug. Cardiovascular drugs that were given in <1% of cases are not reported. (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

InterventionParticipants (Count of Participants)
Usual Care Group12211
Hypotension Decision Support3685

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Inhaled Anesthetic Drug Use During Intraoperative Hypotension: MAP < 50 mmHg

Average concentrations of inhalational anesthesia during MAP < 50 mmHg episodes (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

,
InterventionEndTidal% (other) (Median)
Sevoflurane (EndTidal %)Isoflurane (EndTidal %)Desflurane (EndTidal %)
Hypotension Decision Support1.230.654.70
Usual Care Group1.320.654.28

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Inhaled Anesthetic Drug Use During Intraoperative Hypotension: MAP < 55 mmHg

Average concentrations of inhalational anesthesia during MAP < 55 mmHg episodes (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

,
InterventionEndTidal% (other) (Median)
Sevoflurane (EndTidal %)Isoflurane (EndTidal %)Desflurane (EndTidal %)
Hypotension Decision Support1.250.674.65
Usual Care Group1.340.684.60

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Inhaled Anesthetic Drug Use During Intraoperative Hypotension: MAP < 60 mmHg

Average concentrations of inhalational anesthesia during MAP < 60 mmHg episodes (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

,
InterventionEndTidal% (other) (Median)
Sevoflurane (EndTidal %)Isoflurane (EndTidal %)Desflurane (EndTidal %)
Hypotension Decision Support1.250.672.33
Usual Care Group1.350.684.36

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Inhaled Anesthetic Drug Use During Intraoperative Hypotension: MAP < 65 mmHg

Average concentrations of inhalational anesthesia during MAP < 65 mmHg episodes (NCT02726620)
Timeframe: During the anesthetic phase of the surgical procedure: an expected average of 2.5 hours

,
InterventionEndTidal% (other) (Median)
Sevoflurane (EndTidal %)Isoflurane (EndTidal %)Desflurane (EndTidal %)
Hypotension Decision Support1.270.682.31
Usual Care Group1.350.684.10

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Pain Intensity as Measured by 11-point Verbal Numeric Rating Scale (NRS-11) for Pain.

Pain intensity prior to intervention and at 5 minute intervals after intervention. The 11-point Numeric Rating Scale quantifies a subject's pain experience from 0/10 (no pain) to 10/10 (worst pain imaginable). (NCT03395990)
Timeframe: Baseline, up to 30 minutes.

,
Interventionunits on a scale (Median)
Pre-block5 minutes post-block10 minutes post-block15 minutes post-block20 minutes post-block25 minutes post-block30 minutes post-block
Chloroprocaine7.04.04.03.23.03.02.0
Saline6.06.06.56.56.05.55.5

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