Page last updated: 2024-11-12

a 85783.0

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

Description

A 85783.0: a platelet activating factor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	9957997
CHEMBL ID	98318
MeSH ID	M0246119

Synonyms (21)

Synonym
CHEMBL98318 ,
bdbm50035397
6-(4-fluoro-phenyl)-3-((r)-3-pyridin-3-yl-1h-pyrrolo[1,2-c]thiazole-7-carbonyl)-indole-1-carboxylic acid dimethylamide
161395-33-1
(r)-6-(4-fluorophenyl)-n,n-dimethyl-3-[3-(3-pyridinyl)-1h,3h-pyrrolo[1,2-c]thiazol-7-yl]carbonyl-1h-indole-1-carboxamide
a-85783
unii-ocs3j46f47
a 85783.0
a-85783.0
DTXSID20433311
6-(4-fluorophenyl)-n,n-dimethyl-3-[(3r)-3-pyridin-3-yl-1,3-dihydropyrrolo[1,2-c][1,3]thiazole-7-carbonyl]indole-1-carboxamide
(r)-6-(4-fluorophenyl)-n,n-dimethyl-3-(3-(3-pyridinyl)-1h,3h-pyrrolo(1,2-c)thiazol-7-yl)carbonyl-1h-indole-1-carboxamide
1h-indole-1-carboxamide, 6-(4-fluorophenyl)-n,n-dimethyl-3-(((3r)-3-(3-pyridinyl)-1h,3h-pyrrolo(1,2-c)thiazol-7-yl)carbonyl)-
OCS3J46F47 ,
J-009822
(r)-6-(4-fluorophenyl)-3-[3-(3-pyridyl)-1h,3h-pyrrolo[1,2-c]thiazol-7-oyl]indole-1 carboxylic acid dimethylamide
1h-indole-1-carboxamide, 6-(4-fluorophenyl)-n,n-dimethyl-3-[[(3r)-3-(3-pyridinyl)-1h,3h-pyrrolo[1,2-c]thiazol-7-yl]carbonyl]-
CS-0113256
PD163522
HY-133200
(r)-6-(4-fluorophenyl)-n,n-dimethyl-3-(3-(pyridin-3-yl)-1h,3h-pyrrolo[1,2-c]thiazole-7-carbonyl)-1h-indole-1-carboxamide

Research Excerpts

Dosage Studied

Excerpt	Relevance	Reference
"Peripheral blood taken over 12 h after dosing was used for ex vivo beta-TG release and, in the case of the 70 mg dose, measurement of plasma drug concentration."	( Ex vivo inhibition of beta-thromboglobulin release following administration to man of ABT-299, a novel prodrug of a potent platelet activating factor antagonist. Albert, DH; Carter, GW; Kleinert, HD; Magoc, TJ; Menacherry, SD; Morgan, DW; Reyes, AE; Summers, JB; Sun, E, 1997)	0.3

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (5)

Assay ID	Title	Year	Journal	Article
AID177706	In vivo potency for inhibition of LPS-induced hypotension in rat by intra arterial (i.a.) administration	1994	Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26	N-(acyloxyalkyl)pyridinium salts as soluble prodrugs of a potent platelet activating factor antagonist.
AID165479	Competitive binding with [3H]PAF to rabbit platelet membranes	1994	Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26	N-(acyloxyalkyl)pyridinium salts as soluble prodrugs of a potent platelet activating factor antagonist.
AID177705	In vivo potency for complete inhibition of LPS-induced intestinal damage in rat by intravenous administration	1994	Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26	N-(acyloxyalkyl)pyridinium salts as soluble prodrugs of a potent platelet activating factor antagonist.
AID165635	Inhibitory activity was determined in PAF-induced serotonin release from rabbit platelets	1994	Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26	N-(acyloxyalkyl)pyridinium salts as soluble prodrugs of a potent platelet activating factor antagonist.
AID177707	In vivo potency for inhibition of PAF-induced cutaneous vascular permeability in rat by intravenous administration	1994	Journal of medicinal chemistry, Dec-23, Volume: 37, Issue:26	N-(acyloxyalkyl)pyridinium salts as soluble prodrugs of a potent platelet activating factor antagonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	5 (83.33)	18.2507
2000's	1 (16.67)	29.6817
2010's	0 (0.00)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.10

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 weak demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	12.10 (24.57)
Research Supply Index	2.08 (2.92)
Research Growth Index	4.18 (4.65)
Search Engine Demand Index	0.00 (26.88)
Search Engine Supply Index	0.00 (0.95)

This Compound (12.10)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	1 (16.67%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	5 (83.33%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
thiazoles [no description available]	4.48	5	1	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
d-alpha tocopherol Vitamin E: A generic descriptor for all TOCOPHEROLS and TOCOTRIENOLS that exhibit ALPHA-TOCOPHEROL activity. By virtue of the phenolic hydrogen on the 2H-1-benzopyran-6-ol nucleus, these compounds exhibit varying degree of antioxidant activity, depending on the site and number of methyl groups and the type of ISOPRENOIDS.. tocopherol : A collective name for a group of closely related lipids that contain a chroman-6-ol nucleus substituted at position 2 by a methyl group and by a saturated hydrocarbon chain consisting of three isoprenoid units. They are designated as alpha-, beta-, gamma-, and delta-tocopherol depending on the number and position of additional methyl substituents on the aromatic ring. Tocopherols occur in vegetable oils and vegetable oil products, almost exclusively with R,R,R configuration. Tocotrienols differ from tocopherols only in having three double bonds in the hydrocarbon chain.. vitamin E : Any member of a group of fat-soluble chromanols that exhibit biological activity against vitamin E deficiency. The vitamers in this class consists of a chroman-6-ol core which is substituted at position 2 by a methyl group and (also at position 2) either a saturated or a triply-unsaturated hydrocarbon chain consisting of three isoprenoid units. The major function of vitamin E is to act as a natural antioxidant by scavenging free radicals and molecular oxygen.. (R,R,R)-alpha-tocopherol : An alpha-tocopherol that has R,R,R configuration. The naturally occurring stereoisomer of alpha-tocopherol, it is found particularly in sunflower and olive oils.	2	1	0	alpha-tocopherol	algal metabolite; antiatherogenic agent; anticoagulant; antioxidant; antiviral agent; EC 2.7.11.13 (protein kinase C) inhibitor; immunomodulator; micronutrient; nutraceutical; plant metabolite
ng-nitroarginine methyl ester NG-Nitroarginine Methyl Ester: A non-selective inhibitor of nitric oxide synthase. It has been used experimentally to induce hypertension.	2.03	1	0	alpha-amino acid ester; L-arginine derivative; methyl ester; N-nitro compound	EC 1.14.13.39 (nitric oxide synthase) inhibitor
web 2086 WEB 2086: structure given in first source; PAF antagonist	2	1	0	organonitrogen heterocyclic compound; organosulfur heterocyclic compound
triazoles Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.	2	1	0	1,2,3-triazole
1-hexadecyl-2-acetyl-glycero-3-phosphocholine Platelet Activating Factor: A phospholipid derivative formed by PLATELETS; BASOPHILS; NEUTROPHILS; MONOCYTES; and MACROPHAGES. It is a potent platelet aggregating agent and inducer of systemic anaphylactic symptoms, including HYPOTENSION; THROMBOCYTOPENIA; NEUTROPENIA; and BRONCHOCONSTRICTION.. 2-O-acetyl-1-O-hexadecyl-sn-glycero-3-phosphocholine : A 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine betaine which has hexadecyl as the alkyl group. PAF is a potent phospholipid activator and mediator of many leukocyte functions, including platelet aggregation, inflammation, and anaphylaxis.	4.3	4	1	2-acetyl-1-alkyl-sn-glycero-3-phosphocholine	antihypertensive agent; beta-adrenergic antagonist; bronchoconstrictor agent; hematologic agent; vasodilator agent
abt 299 ABT 299: converted in vivo to A-85783.0; a platelet activating factor antagonist; structure in first source	4.06	3	1

Condition	Relationship Strength	Studies
Middle Ear Effusion [description not available]	2.03	1
Otitis Media with Effusion Inflammation of the middle ear with a clear pale yellow-colored transudate.	2.03	1
Anasarca [description not available]	1.98	1
Blood Pressure, Low [description not available]	1.98	1
Endotoxin Shock [description not available]	1.98	1
Edema Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.	1.98	1
Hypotension Abnormally low BLOOD PRESSURE that can result in inadequate blood flow to the brain and other vital organs. Common symptom is DIZZINESS but greater negative impacts on the body occur when there is prolonged depravation of oxygen and nutrients.	1.98	1
Shock, Septic Sepsis associated with HYPOTENSION or hypoperfusion despite adequate fluid resuscitation. Perfusion abnormalities may include but are not limited to LACTIC ACIDOSIS; OLIGURIA; or acute alteration in mental status.	1.98	1
Innate Inflammatory Response [description not available]	1.99	1
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	1.99	1

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