Fludiazepam is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It is a scheduled drug in the U.S., but is approved for use in Japan.

Structure

Similar Structures

Synonyms

7-chloro-5-(o-Fluorophenyl)-1,3-dihydro-1-methyl-2H-1,4-benzodiazepin-2-one
Fludiazepam
Fludiazepamum

External IDs

ID 540 / Ro 5-3438

International/Other Brands

Erispan (Sumitomo)

Categories

UNII

7F64A2K16Z

CAS number

3900-31-0

Weight

Average: 302.731
Monoisotopic: 302.062218928

Chemical Formula

C₁₆H₁₂ClFN₂O

InChI Key

ROYOYTLGDLIGBX-UHFFFAOYSA-N

InChI

InChI=1S/C16H12ClFN2O/c1-20-14-7-6-10(17)8-12(14)16(19-9-15(20)21)11-4-2-3-5-13(11)18/h2-8H,9H2,1H3

IUPAC Name

7-chloro-5-(2-fluorophenyl)-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one

SMILES

CN1C2=C(C=C(Cl)C=C2)C(=NCC1=O)C1=CC=CC=C1F

Pharmacology

Indication

Used for the short-term treatment of anxiety disorders.

Pharmacodynamics

Fludiazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Fludiazepam accumulates primarily in the cortex and thalamus.

Mechanism of action

Fludiazepam has similar action to diazepam, but binds with four times more affinity to benzodiazepine receptors than diazepam.

Target	Actions	Organism
AGamma-aminobutyric acid receptor subunit alpha-1	potentiator	Humans
AGamma-aminobutyric acid receptor subunit alpha-2	potentiator	Humans
AGamma-aminobutyric acid receptor subunit alpha-3	potentiator	Humans
AGamma-aminobutyric acid receptor subunit alpha-5	potentiator	Humans
AGamma-aminobutyric acid receptor subunit gamma-1	potentiator	Humans
AGamma-aminobutyric acid receptor subunit gamma-2	potentiator	Humans
AGamma-aminobutyric acid receptor subunit gamma-3	potentiator	Humans
AGamma-aminobutyric acid receptor subunit beta-1	potentiator	Humans
AGamma-aminobutyric acid receptor subunit beta-2	potentiator	Humans
AGamma-aminobutyric acid receptor subunit beta-3	potentiator	Humans
AGamma-aminobutyric acid receptor subunit delta	potentiator	Humans
AGamma-aminobutyric acid receptor subunit epsilon	potentiator	Humans
AGamma-aminobutyric acid receptor subunit pi	potentiator	Humans
AGamma-aminobutyric acid receptor subunit rho-1	potentiator	Humans
AGamma-aminobutyric acid receptor subunit rho-2	potentiator	Humans
AGamma-aminobutyric acid receptor subunit rho-3	potentiator	Humans

Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Hepatic.

Route of elimination

Not Available

Half life

Not Available

Clearance

Not Available

Toxicity

Symptoms of overdose include drowsiness, weakness, nausea, dizziness, abdominal pain, cerebral oedema and renal tubular necrosis, hyperglycaemia and hypoglycaemia, liver damage, encephalopathy, coma and death.

Affected organisms

Humans and other mammals

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Not Available

Interactions

Drug Interactions

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

Drug	Interaction
Unlock Additional Data
2,5-Dimethoxy-4-ethylthioamphetamine	The risk or severity of adverse effects can be increased when Fludiazepam is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3-isobutyl-1-methyl-7H-xanthine	The therapeutic efficacy of Fludiazepam can be decreased when used in combination with 3-isobutyl-1-methyl-7H-xanthine.
4-Bromo-2,5-dimethoxyamphetamine	The risk or severity of adverse effects can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Fludiazepam.
4-Methoxyamphetamine	The risk or severity of adverse effects can be increased when 4-Methoxyamphetamine is combined with Fludiazepam.
5-methoxy-N,N-dimethyltryptamine	The risk or severity of adverse effects can be increased when Fludiazepam is combined with 5-methoxy-N,N-dimethyltryptamine.
6-O-benzylguanine	The therapeutic efficacy of Fludiazepam can be decreased when used in combination with 6-O-benzylguanine.
7-Deazaguanine	The therapeutic efficacy of Fludiazepam can be decreased when used in combination with 7-Deazaguanine.
7-Nitroindazole	The risk or severity of adverse effects can be increased when Fludiazepam is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline	The risk or severity of adverse effects can be increased when Fludiazepam is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
7,9-Dimethylguanine	The therapeutic efficacy of Fludiazepam can be decreased when used in combination with 7,9-Dimethylguanine.

Additional Data Available

Extended Description

Extended description of the mechanism of action and particular properties of each drug interaction.

Learn more

Severity

A severity rating for each drug interaction, from minor to major.

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Evidence Level

A rating for the strength of the evidence supporting each drug interaction.

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Action

An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions

Avoid alcohol.
Avoid grapefruit products.
Limit caffeine intake.

References

Synthesis Reference

Yamamato, H., Inaba, S.,Okamoto, T., Hirohashi, T., Ishizumi, K., Yamamoto, M., Maruyama, l., Mori, K. and Kobayashi, T.; U.S. Patents 3,723,461; March 27, 1973; 3,828,027; August 6, 1974 and 3,925,364; December 9, 1975; all assigned to Sumitomo Chemical Co., Ltd.

General References

Ishiwata K, Yanai K, Ido T, Miura-Kanno Y, Kawashima K: Synthesis and biodistribution of [11C]fludiazepam for imaging benzodiazepine receptors. Int J Rad Appl Instrum B. 1988;15(4):365-71. [PubMed:2855634]
Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046]

External Links

Human Metabolome Database: HMDB0015513
KEGG Drug: D01354
PubChem Compound: 3369
PubChem Substance: 46507563
ChemSpider: 3252
ChEBI: 31618
ChEMBL: CHEMBL13291
Therapeutic Targets Database: DAP000934
PharmGKB: PA164745609
Wikipedia: Fludiazepam

ATC Codes

N05BA17 — Fludiazepam

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Completed	Treatment	Menière's Disease / Vertigo	1

Pharmacoeconomics

Manufacturers: Not Available
Packagers: Not Available
Dosage forms: Not Available
Prices: Not Available
Patents: Not Available

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	218.5-219	Yamamato, H., Inaba, S.,Okamoto, T., Hirohashi, T., Ishizumi, K., Yamamoto, M., Maruyama, l., Mori, K. and Kobayashi, T.; U.S. Patents 3,723,461; March 27, 1973; 3,828,027; August 6, 1974 and 3,925,364; December 9, 1975; all assigned to Sumitomo Chemical Co., Ltd.
logP	2.75	HANSCH,C ET AL. (1995)

Predicted Properties

Property	Value	Source
Water Solubility	0.0144 mg/mL	ALOGPS
logP	2.83	ALOGPS
logP	3.22	ChemAxon
logS	-4.3	ALOGPS
pKa (Strongest Basic)	1.89	ChemAxon
Physiological Charge	0	ChemAxon
Hydrogen Acceptor Count	2	ChemAxon
Hydrogen Donor Count	0	ChemAxon
Polar Surface Area	32.67 Å²	ChemAxon
Rotatable Bond Count	1	ChemAxon
Refractivity	80.03 m³·mol^-1	ChemAxon
Polarizability	29.45 Å³	ChemAxon
Number of Rings	3	ChemAxon
Bioavailability	1	ChemAxon
Rule of Five	Yes	ChemAxon
Ghose Filter	Yes	ChemAxon
Veber's Rule	Yes	ChemAxon
MDDR-like Rule	No	ChemAxon

Predicted ADMET features

Property	Value	Probability
Human Intestinal Absorption	+	1.0
Blood Brain Barrier	+	0.9946
Caco-2 permeable	+	0.8567
P-glycoprotein substrate	Substrate	0.6618
P-glycoprotein inhibitor I	Inhibitor	0.5293
P-glycoprotein inhibitor II	Non-inhibitor	0.8532
Renal organic cation transporter	Inhibitor	0.592
CYP450 2C9 substrate	Non-substrate	0.6724
CYP450 2D6 substrate	Non-substrate	0.9087
CYP450 3A4 substrate	Substrate	0.8081
CYP450 1A2 substrate	Inhibitor	0.7925
CYP450 2C9 inhibitor	Non-inhibitor	0.5446
CYP450 2D6 inhibitor	Non-inhibitor	0.8884
CYP450 2C19 inhibitor	Inhibitor	0.5598
CYP450 3A4 inhibitor	Inhibitor	0.5153
CYP450 inhibitory promiscuity	High CYP Inhibitory Promiscuity	0.5827
Ames test	Non AMES toxic	0.8792
Carcinogenicity	Non-carcinogens	0.817
Biodegradation	Not ready biodegradable	1.0
Rat acute toxicity	2.2719 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.9953
hERG inhibition (predictor II)	Non-inhibitor	0.8236

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	Not Available
Mass Spectrum (Electron Ionization)	MS	splash10-0uk9-2794000000-6f1a3e2e0783b2069f2f
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	Not Available

Taxonomy

Description: This compound belongs to the class of organic compounds known as 1,4-benzodiazepines. These are organic compounds containing a benzene ring fused to a 1,4-azepine.
Kingdom: Organic compounds
Super Class: Organoheterocyclic compounds
Class: Benzodiazepines
Sub Class: 1,4-benzodiazepines
Direct Parent: 1,4-benzodiazepines
Alternative Parents: Alpha amino acids and derivatives / Fluorobenzenes / Aryl fluorides / Aryl chlorides / Tertiary carboxylic acid amides / Lactams / Ketimines / Propargyl-type 1,3-dipolar organic compounds / Azacyclic compounds / Organopnictogen compounds
show 5 more
Substituents: 1,4-benzodiazepine / Alpha-amino acid or derivatives / Fluorobenzene / Halobenzene / Aryl chloride / Aryl fluoride / Aryl halide / Monocyclic benzene moiety / Benzenoid / Tertiary carboxylic acid amide
show 20 more
Molecular Framework: Aromatic heteropolycyclic compounds
External Descriptors: organofluorine compound, organochlorine compound, 1,4-benzodiazepinone (CHEBI:31618)

Targets

Details1. Gamma-aminobutyric acid receptor subunit alpha-1

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Potentiator

General Function: Inhibitory extracellular ligand-gated ion channel activity
Specific Function: Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name: GABRA1
Uniprot ID: P14867
Uniprot Name: Gamma-aminobutyric acid receptor subunit alpha-1
Molecular Weight: 51801.395 Da

References

Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046]

Details2. Gamma-aminobutyric acid receptor subunit alpha-2

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Potentiator

General Function: Inhibitory extracellular ligand-gated ion channel activity
Specific Function: GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name: GABRA2
Uniprot ID: P47869
Uniprot Name: Gamma-aminobutyric acid receptor subunit alpha-2
Molecular Weight: 51325.85 Da

References

Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046]

Details3. Gamma-aminobutyric acid receptor subunit alpha-3

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Potentiator

General Function: Inhibitory extracellular ligand-gated ion channel activity
Specific Function: GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name: GABRA3
Uniprot ID: P34903
Uniprot Name: Gamma-aminobutyric acid receptor subunit alpha-3
Molecular Weight: 55164.055 Da

References

Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046]

Details4. Gamma-aminobutyric acid receptor subunit alpha-5

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Potentiator

General Function: Transporter activity
Specific Function: GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name: GABRA5
Uniprot ID: P31644
Uniprot Name: Gamma-aminobutyric acid receptor subunit alpha-5
Molecular Weight: 52145.645 Da

References

Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046]

Details5. Gamma-aminobutyric acid receptor subunit gamma-1

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Potentiator

General Function: Inhibitory extracellular ligand-gated ion channel activity
Specific Function: GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name: GABRG1
Uniprot ID: Q8N1C3
Uniprot Name: Gamma-aminobutyric acid receptor subunit gamma-1
Molecular Weight: 53594.49 Da

References

Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046]

Details6. Gamma-aminobutyric acid receptor subunit gamma-2

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Potentiator

General Function: Inhibitory extracellular ligand-gated ion channel activity
Specific Function: Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name: GABRG2
Uniprot ID: P18507
Uniprot Name: Gamma-aminobutyric acid receptor subunit gamma-2
Molecular Weight: 54161.78 Da

References

Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046]

Details7. Gamma-aminobutyric acid receptor subunit gamma-3

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Potentiator

General Function: Inhibitory extracellular ligand-gated ion channel activity
Specific Function: GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name: GABRG3
Uniprot ID: Q99928
Uniprot Name: Gamma-aminobutyric acid receptor subunit gamma-3
Molecular Weight: 54288.16 Da

References

Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046]

Details8. Gamma-aminobutyric acid receptor subunit beta-1

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Potentiator

General Function: Ligand-gated ion channel activity
Specific Function: Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name: GABRB1
Uniprot ID: P18505
Uniprot Name: Gamma-aminobutyric acid receptor subunit beta-1
Molecular Weight: 54234.085 Da

References

Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046]

Details9. Gamma-aminobutyric acid receptor subunit beta-2

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Potentiator

General Function: Inhibitory extracellular ligand-gated ion channel activity
Specific Function: Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name: GABRB2
Uniprot ID: P47870
Uniprot Name: Gamma-aminobutyric acid receptor subunit beta-2
Molecular Weight: 59149.895 Da

References

Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046]

Details10. Gamma-aminobutyric acid receptor subunit beta-3

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Potentiator

General Function: Gaba-gated chloride ion channel activity
Specific Function: Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Gene Name: GABRB3
Uniprot ID: P28472
Uniprot Name: Gamma-aminobutyric acid receptor subunit beta-3
Molecular Weight: 54115.04 Da

References

Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046]

Details11. Gamma-aminobutyric acid receptor subunit delta

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Potentiator

General Function: Gaba-a receptor activity
Specific Function: GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name: GABRD
Uniprot ID: O14764
Uniprot Name: Gamma-aminobutyric acid receptor subunit delta
Molecular Weight: 50707.835 Da

References

Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046]

Details12. Gamma-aminobutyric acid receptor subunit epsilon

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Potentiator

General Function: Inhibitory extracellular ligand-gated ion channel activity
Specific Function: GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name: GABRE
Uniprot ID: P78334
Uniprot Name: Gamma-aminobutyric acid receptor subunit epsilon
Molecular Weight: 57971.175 Da

References

Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046]

Details13. Gamma-aminobutyric acid receptor subunit pi

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Potentiator

General Function: Gaba-a receptor activity
Specific Function: GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. In the ute...
Gene Name: GABRP
Uniprot ID: O00591
Uniprot Name: Gamma-aminobutyric acid receptor subunit pi
Molecular Weight: 50639.735 Da

References

Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046]

Details14. Gamma-aminobutyric acid receptor subunit rho-1

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Potentiator

General Function: Gaba-a receptor activity
Specific Function: GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Rho-1 GABA...
Gene Name: GABRR1
Uniprot ID: P24046
Uniprot Name: Gamma-aminobutyric acid receptor subunit rho-1
Molecular Weight: 55882.91 Da

References

Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046]

Details15. Gamma-aminobutyric acid receptor subunit rho-2

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Potentiator

General Function: Gaba-a receptor activity
Specific Function: GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Rho-2 GABA...
Gene Name: GABRR2
Uniprot ID: P28476
Uniprot Name: Gamma-aminobutyric acid receptor subunit rho-2
Molecular Weight: 54150.41 Da

References

Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046]

Details16. Gamma-aminobutyric acid receptor subunit rho-3

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Potentiator

General Function: Gaba-a receptor activity
Specific Function: GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name: GABRR3
Uniprot ID: A8MPY1
Uniprot Name: Gamma-aminobutyric acid receptor subunit rho-3
Molecular Weight: 54271.1 Da

References

Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046]

Drug created on July 31, 2007 07:10 / Updated on February 12, 2020 17:56

Fludiazepam

Identification

Structure for Fludiazepam (DB01567)

Pharmacology

Interactions

References

Clinical Trials

Pharmacoeconomics

Properties

Spectra

Taxonomy

Targets

References

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