Page last updated: 2024-11-12

azd-3043

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

Description

AZD-3043: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	10286834
CHEMBL ID	3354350
SCHEMBL ID	1882795
MeSH ID	M0575382

Synonyms (21)

Synonym
SCHEMBL1882795
thrx-918661
(4-((n,n-diethylcarbamoyl)methoxy)-3-ethoxyphenyl)acetic acid propyl ester
azd 3043 [who-dd]
benzeneacetic acid, 4-(2-(diethylamino)-2-oxoethoxy)-3-ethoxy-, propyl ester
372ab76lql ,
579494-66-9
azd 3043
azd-3043
thrx 918661
azd3043
unii-372ab76lql
benzeneacetic acid, 4-[2-(diethylamino)-2-oxoethoxy]-3-ethoxy-, propyl ester
CHEMBL3354350
DB12576
Q27256612
propyl 2-[4-[2-(diethylamino)-2-oxoethoxy]-3-ethoxyphenyl]acetate
DTXSID601339521
4-[2-(diethylamino)-2-oxoethoxy]-3-ethoxybenzeneacetic acid, propyl ester
AKOS040750666
[4-[(n,n-diethylcarbamoyl)methoxy]-3-ethoxyphenyl]acetic acid propyl ester

Research Excerpts

Toxicity

Excerpt	Reference	Relevance
" Assessments included adverse events, vital signs, blood gases, laboratory values, clinical signs of sedation/anesthesia, and bispectral index score."	( A Bolus and Bolus Followed by Infusion Study of AZD3043, an Investigational Intravenous Drug for Sedation and Anesthesia: Safety and Pharmacodynamics in Healthy Male and Female Volunteers. Ahlén, K; Barassin, S; Björnsson, MA; Kalman, S; Kanes, SJ; Koch, P; Norberg, Å, 2015)	0.42
" Adverse events occurring in >1 subject were headache (n = 15; 21%), nausea (n = 7; 10%), vomiting (n = 3; 4%), and fatigue (n = 2; 3%)."	( A Bolus and Bolus Followed by Infusion Study of AZD3043, an Investigational Intravenous Drug for Sedation and Anesthesia: Safety and Pharmacodynamics in Healthy Male and Female Volunteers. Ahlén, K; Barassin, S; Björnsson, MA; Kalman, S; Kanes, SJ; Koch, P; Norberg, Å, 2015)	0.42
" Assessments included adverse events, vital signs, blood gases, laboratory values, clinical signs of sedation/anesthesia, and bispectral index."	( First Human Study of the Investigational Sedative and Anesthetic Drug AZD3043: A Dose-Escalation Trial to Assess the Safety, Pharmacokinetics, and Efficacy of a 30-Minute Infusion in Healthy Male Volunteers. Ahlén, K; Barassin, S; Björnsson, MA; Kalman, S; Kanes, SJ; Koch, P; Norberg, Å, 2015)	0.42
" Adverse events occurring in >1 subject were headache (n = 4), erythema (n = 3), chest discomfort (n = 2), nausea (n = 2), and dyspnea (n = 2)."	( First Human Study of the Investigational Sedative and Anesthetic Drug AZD3043: A Dose-Escalation Trial to Assess the Safety, Pharmacokinetics, and Efficacy of a 30-Minute Infusion in Healthy Male Volunteers. Ahlén, K; Barassin, S; Björnsson, MA; Kalman, S; Kanes, SJ; Koch, P; Norberg, Å, 2015)	0.42

Pharmacokinetics

Excerpt	Reference	Relevance
" We describe a population pharmacokinetic (PK) model of arterial and venous concentrations of AZD3043 and the pharmacodynamic effects on bispectral index (BIS) in healthy volunteers."	( A Recirculatory Model for Pharmacokinetics and the Effects on Bispectral Index After Intravenous Infusion of the Sedative and Anesthetic AZD3043 in Healthy Volunteers. Björnsson, MA; Kalman, S; Norberg, Å; Simonsson, USH, 2015)	0.42
"001), leading to an increased half-life with increasing dose."	( A Recirculatory Model for Pharmacokinetics and the Effects on Bispectral Index After Intravenous Infusion of the Sedative and Anesthetic AZD3043 in Healthy Volunteers. Björnsson, MA; Kalman, S; Norberg, Å; Simonsson, USH, 2015)	0.42

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

Bioassays (29)

Assay ID	Title	Year	Journal	Article
AID1877625	Anesthetic activity in mouse assessed as onset time	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1877638	Anesthetic activity in rabbit assessed as time duration of loss of righting reflex	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1877622	Anesthetic activity in mouse assessed as concentration required to induce hypnotic effect	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1174559	Therapeutic index, ratio of LC50 for Sprague-Dawley rat by rotarod test to HD50 for hypnotic activity in iv dosed Sprague-Dawley rat	2015	European journal of medicinal chemistry, Jan-07, Volume: 89	Phenyl acetate derivatives, fluorine-substituted on the phenyl group, as rapid recovery hypnotic agents with reflex depression.
AID1877630	Therapeutic index, ratio of LD50 for toxicity in rat to HD50 for anesthetic activity in rat	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1877629	Toxicity in rat assessed as lethal dose	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1174562	Induction of hypnotic activity in iv dosed Sprague-Dawley rat assessed as reflex depression 10 secs following injection	2015	European journal of medicinal chemistry, Jan-07, Volume: 89	Phenyl acetate derivatives, fluorine-substituted on the phenyl group, as rapid recovery hypnotic agents with reflex depression.
AID1877633	Therapeutic index, ratio of LD50 for toxicity in rabbit to HD50 for anesthetic activity in rabbit	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1174563	Induction of hypnotic activity in iv dosed Sprague-Dawley rat assessed as reflex depression 20 secs following injection	2015	European journal of medicinal chemistry, Jan-07, Volume: 89	Phenyl acetate derivatives, fluorine-substituted on the phenyl group, as rapid recovery hypnotic agents with reflex depression.
AID1877636	Anesthetic activity in rat assessed as time to walk at 2 times of HD50 concentration	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1877637	Anesthetic activity in rabbit assessed as onset time	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1174557	Induction of hypnotic activity in iv dosed Sprague-Dawley rat assessed as loss of righting reflex	2015	European journal of medicinal chemistry, Jan-07, Volume: 89	Phenyl acetate derivatives, fluorine-substituted on the phenyl group, as rapid recovery hypnotic agents with reflex depression.
AID1877632	Toxicity in rabbit assessed as lethal dose	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1877640	Inhibition of GABAA receptor (unknown origin) at 50 uM by radioligand receptor binding assay relative to control	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1877627	Anesthetic activity in mouse assessed as time to walk at 2 times of HD50 concentration	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1174570	Displacement of [3H]MK801 from NMDA receptor in Sprague-Dawley rat cerebral cortex membrane at 50 umol by liquid scintillation counting	2015	European journal of medicinal chemistry, Jan-07, Volume: 89	Phenyl acetate derivatives, fluorine-substituted on the phenyl group, as rapid recovery hypnotic agents with reflex depression.
AID1877639	Anesthetic activity in rabbit assessed as time to walk at 2 times of HD50 concentration	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1174560	Induction of hypnotic activity in iv dosed Sprague-Dawley rat assessed as time duration of loss of righting reflex	2015	European journal of medicinal chemistry, Jan-07, Volume: 89	Phenyl acetate derivatives, fluorine-substituted on the phenyl group, as rapid recovery hypnotic agents with reflex depression.
AID1174568	Octanol-buffer partition coefficient, log P of the compound by HPLC	2015	European journal of medicinal chemistry, Jan-07, Volume: 89	Phenyl acetate derivatives, fluorine-substituted on the phenyl group, as rapid recovery hypnotic agents with reflex depression.
AID1877626	Anesthetic activity in mouse assessed as time duration of loss of righting reflex	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1877621	Lipophilicity, logP of the compound	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1877631	Anesthetic activity in rabbit assessed as concentration required to induce hypnotic effect	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1174569	Displacement of [3H]EBOB from GABAA receptor in Sprague-Dawley rat frontoparietal cortex membrane at 50 umol by liquid scintillation counting	2015	European journal of medicinal chemistry, Jan-07, Volume: 89	Phenyl acetate derivatives, fluorine-substituted on the phenyl group, as rapid recovery hypnotic agents with reflex depression.
AID1877623	Toxicity in mouse assessed as lethal dose	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1877624	Therapeutic index, ratio of LD50 for toxicity in mouse to HD50 for anesthetic activity in mouse	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1877634	Anesthetic activity in rat assessed as onset time	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1877635	Anesthetic activity in rat assessed as time duration of loss of righting reflex	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
AID1174558	Toxicity in Sprague-Dawley rat assessed as motor coordination by rotarod test	2015	European journal of medicinal chemistry, Jan-07, Volume: 89	Phenyl acetate derivatives, fluorine-substituted on the phenyl group, as rapid recovery hypnotic agents with reflex depression.
AID1877628	Anesthetic activity in rat assessed as concentration required to induce hypnotic effect	2022	Bioorganic & medicinal chemistry letters, 02-01, Volume: 57	Design, synthesis, and evaluation of phenylpiperazine-phenylacetate derivatives as rapid recovery hypnotic agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	8 (88.89)	24.3611
2020's	1 (11.11)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	3 (33.33%)	5.53%
Reviews	1 (11.11%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	5 (55.56%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
propofol Propofol: An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS.. propofol : A phenol resulting from the formal substitution of the hydrogen at the 2 position of 1,3-diisopropylbenzene by a hydroxy group.	7.52	2	phenols	anticonvulsant; antiemetic; intravenous anaesthetic; radical scavenger; sedative
propanidid Propanidid: An intravenous anesthetic that has been used for rapid induction of anesthesia and for maintenance of anesthesia of short duration. (From Martindale, The Extra Pharmacopoeia, 30th ed, p918)	2.59	2	methoxybenzenes
etomidate Etomidate: Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic.. etomidate : The ethyl ester of 1-[(1R)-1-phenylethyl]-1H-imidazole-5-carboxylic acid. It is an intravenous general anaesthetic with no analgesic activity.	3.18	1	ethyl ester; imidazoles	intravenous anaesthetic; sedative
remimazolam remimazolam: sedative; structure in first source	3.18	1

Condition	Relationship Strength	Studies	Trials
Bilateral Headache [description not available]	5.38	2	2
Headache The symptom of PAIN in the cranial region. It may be an isolated benign occurrence or manifestation of a wide variety of HEADACHE DISORDERS.	5.38	2	2
Nausea An unpleasant sensation in the stomach usually accompanied by the urge to vomit. Common causes are early pregnancy, sea and motion sickness, emotional stress, intense pain, food poisoning, and various enteroviruses.	4.41	1	1
Erythema Redness of the skin produced by congestion of the capillaries. This condition may result from a variety of disease processes.	3.5	1	1
Anesthesia A state characterized by loss of feeling or sensation. This depression of nerve function is usually the result of pharmacologic action and is induced to allow performance of surgery or other painful procedures.	2.11	1	0
Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.	2.07	1	0

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