Lindane
Identification
- Summary
Lindane is an ectoparasiticide and ovicide used in the treatment of Pediculosis humanis capitis (head lice) and Phthirus pubis (crab lice).
- Generic Name
- Lindane
- DrugBank Accession Number
- DB00431
- Background
An organochlorine insecticide that has been used as a pediculicide and a scabicide. Lindane has been banned in California, United Kingdom, Australia, and many western countries due to concerns about neurotoxicity and adverse effects on the environment. In Canada, Lindane is not recommmended as a first-line therapy due to reports of resistance, neurotoxicity, and bone marrow suppression, but has been approved by the FDA as a second-line therapy for topical treatment of pediculosis capitis (head lice), pediculosis pubis (pubic lice), or scabies in patients greater than two years of age who cannot tolerate or have failed first-line treatment. Lindane is still allowed for pharmaceutical use until 2015.
- Type
- Small Molecule
- Groups
- Approved, Withdrawn
- Structure
- Weight
- Average: 290.83
Monoisotopic: 287.860066434 - Chemical Formula
- C6H6Cl6
- Synonyms
- (1r,2c,3t,4c,5c,6t)-1,2,3,4,5,6-hexachlorocyclohexane
- (1α,2α,3β,4α,5α,6β)-1,2,3,4,5,6-hexachlorocyclohexane
- 1,2,3,4,5,6-hexachlorocyclohexane
- Benzene hexachloride
- gamma-1,2,3,4,5,6-hexachlorocyclohexane
- gamma-benzene hexachloride
- gamma-BHC
- gamma-HCH
- gamma-Hexachlorocyclohexane
- gamma-Lindane
- Gammallin
- Gammaxene
- Lindan
- Lindane
- Lindano
- Lindanum
- γ-hexachlorocyclohexane
- γ-Hexachlorzyklohexan
- γ-lindane
Pharmacology
- Indication
For the treatment of patients infested with Sarcoptes scabiei or pediculosis capitis who have either failed to respond to adequate doses, or are intolerant of other approved therapies.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Lice ••• ••• ••••• Treatment of Pediculosis capitis •••••••••••• ••••••• Treatment of Scabies ••• ••• ••••• Treatment of Scabies •••••••••••• •••••• Treatment of Crab lice •••••••••••• ••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Scabies is a common, highly pruritic infestation of the skin caused by Sarcoptes scabiei (lice). It is a very contagious condition with specific lesions, such as burrows, and nonspecific lesions, such as papules, vesicles and excoriations. The typical areas of the body it affects are finger webs, scalp (hair), wrists, axillary folds, abdomen, buttocks, inframammary folds and genitalia (males). It is characterized by intense night-time itching. Scabies is spread through close personal contact (relatives, sexual partners, schoolchildren, chronically ill patients and crowded communities). Scabies infestations and the corresponding symptoms can be eliminated by killing the scabies with topical insecticides or scabicides. Lindane is a scabicide that is essentially an organochloride insecticide.
- Mechanism of action
Lindane is an organochloride insecticide that has similar neurotoxic protperties to DDT. It exerts its parasiticidal action by being directly absorbed through the parasite's exoskeleton (primarily lice, or scabies) and their ova. The gamma-aminobutyric acid (GABA(1)) receptor/chloride ionophore complex is the primary site of action for lindane, and other insecticides such as endosulfan, and fipronil. Blockage of the GABA-gated chloride channel reduces neuronal inhibition, which leads to hyperexcitation of the central nervous system. This results in paralysis, convulsions, and death. Lindane has very low ovicidal activity.
Target Actions Organism AGamma-aminobutyric acid receptor subunit beta-1 antagonistHumans UGlycine receptor subunit alpha-1 antagonistHumans UGlycine receptor subunit alpha-2 antagonistHumans UGlycine receptor subunit alpha-3 antagonistHumans UGlycine receptor subunit beta antagonistHumans UGamma-aminobutyric acid receptor subunit beta-3 Not Available Humans UGamma-aminobutyric acid receptor subunit rho-1 Not Available Humans UProgesterone receptor Not Available Humans UEstrogen receptor alpha Not Available Humans UNuclear receptor subfamily 1 group I member 2 Not Available Humans - Absorption
Lindane is absorbed significantly through the skin. A mean peak blood concentration of 28 nanograms per mL occurred in infants and children 6 hours after total body application of lindane lotion for scabies.
- Volume of distribution
Not Available
- Protein binding
91%
- Metabolism
Primarily hepatic through dechlorination leading to 2-chlorophenol, 0-chlorophenol, chlorocyclohexane, chlorocyclohexanol.
- Route of elimination
Not Available
- Half-life
18 hours
- Clearance
Not Available
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Lindane is a moderately toxic compound via oral exposure, with a reported oral LD50 of 88 to 190 mg/kg in rats. Gamma-HCH (which constitutes 99% of lindane) is generally considered to be the most acutely toxic of the isomers following single administration. It is moderately toxic via the dermal route as well, with reported dermal LD50 values of 500 to 1000 mg/kg in rats, 300 mg/kg in mice, 400 mg/kg in guinea pigs, and 300 mg/kg in rabbits. Acute exposure to lindane may lead to central nervous system stimulation (usually developing within 1 hour), mental/motor impairment, excitation, clonic (intermittent) and tonic (continuous) convulsion. Other adverse reactions include central nervous system toxicity, as well as skin and gastrointestinal changes.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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 Integrate drug-drug
interactions in your softwareBupropion The risk or severity of seizure can be increased when Bupropion is combined with Lindane. Dalfampridine The risk or severity of seizure can be increased when Lindane is combined with Dalfampridine. Hydroxychloroquine The risk or severity of seizure can be increased when Hydroxychloroquine is combined with Lindane. - Food Interactions
- Avoid excessive or chronic alcohol consumption.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- International/Other Brands
- Gamene / Kwell / Scabene
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Lindane Lotion 10 mg/1mL Topical Olta Pharmaceuticals Corporation 2009-03-17 Not applicable US Lindane Shampoo 10 mg/1mL Topical Olta Pharmaceuticals Corporation 2009-03-17 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Lindane Shampoo 10 mg/1mL Topical Physicians Total Care, Inc. 1981-12-07 2009-12-31 US Lindane Shampoo 10 mg/1mL Topical Versa Pharm Incorporated 2011-11-21 Not applicable US Lindane Shampoo, suspension 10 mg/1mL Topical Morton Grove Pharmaceuticals, Inc. 1984-09-18 Not applicable US Lindane Lotion 10 mg/1mL Topical Physicians Total Care, Inc. 1981-12-17 2009-12-31 US Lindane Lotion 10 mg/1mL Topical Morton Grove Pharmaceuticals, Inc. 1984-08-16 2016-06-02 US - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Dom-lindane Lotion - 1% Liquid 1 % Topical Dominion Pharmacal 1995-12-31 2004-08-16 Canada Gamma Benzene Hexachloride Lotion USP 1% w/v (LICSCAB Lotion) Lotion Cutaneous UNIMED SDN BHD 2020-09-08 Not applicable Malaysia Hexit Lotion Lotion 1 % Topical Odan Laboratories Ltd 2003-07-15 2012-12-31 Canada Hexit Shampoo 1.0% Shampoo 1 % Topical Odan Laboratories Ltd 1989-12-31 2012-12-31 Canada Kwellada Lotion 1% Lotion 1 % Topical Reed & Carnrick, Division Of Block Drug Company (Canada) Ltd. 1958-12-31 1997-07-22 Canada
Categories
- ATC Codes
- P03AB02 — Lindane
- Drug Categories
- Agents that reduce seizure threshold
- Agrochemicals
- Antiparasitic Products, Insecticides and Repellents
- Chlorine Containing Products
- Compounds used in a research, industrial, or household setting
- Ectoparasiticides, Incl. Scabicides
- Ectoparasiticides, Incl. Scabicides, Insecticides and Repellents
- Hydrocarbons, Chlorinated
- Hydrocarbons, Halogenated
- Insecticides
- Pesticides
- Toxic Actions
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as cyclohexyl halides. These are organohalogen compounds containing a monocyclic cyclohexane moiety that is substituted at one or more positions by an halogen atom.
- Kingdom
- Organic compounds
- Super Class
- Organohalogen compounds
- Class
- Alkyl halides
- Sub Class
- Cyclohexyl halides
- Direct Parent
- Cyclohexyl halides
- Alternative Parents
- Organochlorides / Hydrocarbon derivatives / Alkyl chlorides
- Substituents
- Aliphatic homomonocyclic compound / Alkyl chloride / Cyclohexyl halide / Hydrocarbon derivative / Organochloride
- Molecular Framework
- Aliphatic homomonocyclic compounds
- External Descriptors
- cyclodiene organochlorine insecticide, hexachlorocyclohexane (CHEBI:32888) / Organochlorine insecticides (C07075)
- Affected organisms
- Scabies (Sarcoptes scabei) and other insects
Chemical Identifiers
- UNII
- 59NEE7PCAB
- CAS number
- 58-89-9
- InChI Key
- JLYXXMFPNIAWKQ-GNIYUCBRSA-N
- InChI
- InChI=1S/C6H6Cl6/c7-1-2(8)4(10)6(12)5(11)3(1)9/h1-6H/t1-,2-,3-,4+,5+,6+
- IUPAC Name
- (1R,2S,3r,4R,5S,6r)-1,2,3,4,5,6-hexachlorocyclohexane
- SMILES
- Cl[C@H]1[C@H](Cl)[C@@H](Cl)[C@@H](Cl)[C@H](Cl)[C@H]1Cl
References
- General References
- External Links
- Human Metabolome Database
- HMDB0014575
- KEGG Drug
- D00360
- KEGG Compound
- C07075
- PubChem Compound
- 727
- PubChem Substance
- 46508542
- ChemSpider
- 10481896
- BindingDB
- 50410525
- 1388
- ChEBI
- 32888
- ChEMBL
- CHEMBL15891
- Therapeutic Targets Database
- DAP001036
- PharmGKB
- PA164754914
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Lindane
- MSDS
- Download (54.1 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 2 Completed Treatment Head Lice Infestation 1
Pharmacoeconomics
- Manufacturers
- Reed and carnrick pharmaceuticals div block drug co inc
- Sola barnes hind
- Olta pharmaceuticals corp
- Wockhardt eu operations (swiss) ag
- Stiefel laboratories inc
- Packagers
- AL and S LLC
- Alliant Pharmaceuticals Inc.
- Apotheca Inc.
- Century Pharmaceuticals Inc.
- Dept Health Central Pharmacy
- Dispensing Solutions
- Major Pharmaceuticals
- Pharmedix
- Physicians Total Care Inc.
- Qualitest
- United Research Laboratories Inc.
- Wockhardt Ltd.
- Dosage Forms
Form Route Strength Liquid Topical 1 % Lotion Topical 1 g Lotion Cutaneous Shampoo Topical 1 % Solution Cutaneous Lotion Topical 10 mg/1mL Shampoo Topical 10 mg/1mL Shampoo, suspension Topical 10 mg/1mL Lotion Topical 1 % Lotion Topical - Prices
Unit description Cost Unit Lindane 1% Lotion 60ml Bottle 142.33USD bottle Lindane 1% Shampoo 60ml Bottle 142.33USD bottle Lindane 1% lotion 5.16USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 112.5 °C PhysProp boiling point (°C) 323.4 °C PhysProp water solubility 7.3 mg/L (at 25 °C) RICHARDSON,LT & MILLER,DM (1960) logP 3.72 HANSCH,C ET AL. (1995) - Predicted Properties
Property Value Source Water Solubility 0.00547 mg/mL ALOGPS logP 3.94 ALOGPS logP 4.35 Chemaxon logS -4.7 ALOGPS Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 0 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 0 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 54.08 m3·mol-1 Chemaxon Polarizability 23.08 Å3 Chemaxon Number of Rings 1 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9918 Blood Brain Barrier + 0.9862 Caco-2 permeable + 0.8369 P-glycoprotein substrate Non-substrate 0.8826 P-glycoprotein inhibitor I Non-inhibitor 0.9733 P-glycoprotein inhibitor II Non-inhibitor 0.9944 Renal organic cation transporter Non-inhibitor 0.8593 CYP450 2C9 substrate Non-substrate 0.8522 CYP450 2D6 substrate Non-substrate 0.7758 CYP450 3A4 substrate Non-substrate 0.7335 CYP450 1A2 substrate Inhibitor 0.6037 CYP450 2C9 inhibitor Non-inhibitor 0.7892 CYP450 2D6 inhibitor Non-inhibitor 0.9592 CYP450 2C19 inhibitor Non-inhibitor 0.5936 CYP450 3A4 inhibitor Non-inhibitor 0.9007 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7408 Ames test Non AMES toxic 0.9754 Carcinogenicity Carcinogens 0.5058 Biodegradation Not ready biodegradable 0.9271 Rat acute toxicity 2.0905 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9077 hERG inhibition (predictor II) Non-inhibitor 0.9617
Spectra
- Mass Spec (NIST)
- Download (11.7 KB)
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 115.9076283 predictedDarkChem Lite v0.1.0 [M-H]- 115.8518283 predictedDarkChem Lite v0.1.0 [M-H]- 135.17506 predictedDeepCCS 1.0 (2019) [M+H]+ 137.4221 predictedDeepCCS 1.0 (2019) [M+Na]+ 143.34596 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- 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
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
- Cole LM, Roush RT, Casida JE: Drosophila GABA-gated chloride channel: modified [3H]EBOB binding site associated with Ala-->Ser or Gly mutants of Rdl subunit. Life Sci. 1995;56(10):757-65. [Article]
- Sauviat MP, Pages N: [Cardiotoxicity of lindane, a gamma isomer of hexachlorocyclohexane]. J Soc Biol. 2002;196(4):339-48. [Article]
- Anand M, Agrawal AK, Rehmani BN, Gupta GS, Rana MD, Seth PK: Role of GABA receptor complex in low dose lindane (HCH) induced neurotoxicity: neurobehavioural, neurochemical and electrophysiological studies. Drug Chem Toxicol. 1998 Feb;21(1):35-46. [Article]
- Joy RM, Walby WF, Stark LG, Albertson TE: Lindane blocks GABAA-mediated inhibition and modulates pyramidal cell excitability in the rat hippocampal slice. Neurotoxicology. 1995 Summer;16(2):217-28. [Article]
- Bloomquist JR: Chloride channels as tools for developing selective insecticides. Arch Insect Biochem Physiol. 2003 Dec;54(4):145-56. [Article]
- Narahashi T: Neuronal ion channels as the target sites of insecticides. Pharmacol Toxicol. 1996 Jul;79(1):1-14. [Article]
- Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
- Vale C, Fonfria E, Bujons J, Messeguer A, Rodriguez-Farre E, Sunol C: The organochlorine pesticides gamma-hexachlorocyclohexane (lindane), alpha-endosulfan and dieldrin differentially interact with GABA(A) and glycine-gated chloride channels in primary cultures of cerebellar granule cells. Neuroscience. 2003;117(2):397-403. [Article]
- Heusinkveld HJ, Thomas GO, Lamot I, van den Berg M, Kroese AB, Westerink RH: Dual actions of lindane (gamma-hexachlorocyclohexane) on calcium homeostasis and exocytosis in rat PC12 cells. Toxicol Appl Pharmacol. 2010 Oct 1;248(1):12-9. doi: 10.1016/j.taap.2010.06.013. Epub 2010 Jun 21. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Transmitter-gated ion channel activity
- Specific Function
- The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing).
- Gene Name
- GLRA1
- Uniprot ID
- P23415
- Uniprot Name
- Glycine receptor subunit alpha-1
- Molecular Weight
- 52623.35 Da
References
- Vale C, Fonfria E, Bujons J, Messeguer A, Rodriguez-Farre E, Sunol C: The organochlorine pesticides gamma-hexachlorocyclohexane (lindane), alpha-endosulfan and dieldrin differentially interact with GABA(A) and glycine-gated chloride channels in primary cultures of cerebellar granule cells. Neuroscience. 2003;117(2):397-403. [Article]
- Heusinkveld HJ, Thomas GO, Lamot I, van den Berg M, Kroese AB, Westerink RH: Dual actions of lindane (gamma-hexachlorocyclohexane) on calcium homeostasis and exocytosis in rat PC12 cells. Toxicol Appl Pharmacol. 2010 Oct 1;248(1):12-9. doi: 10.1016/j.taap.2010.06.013. Epub 2010 Jun 21. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Transmitter-gated ion channel activity
- Specific Function
- The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing).
- Gene Name
- GLRA2
- Uniprot ID
- P23416
- Uniprot Name
- Glycine receptor subunit alpha-2
- Molecular Weight
- 52001.585 Da
References
- Vale C, Fonfria E, Bujons J, Messeguer A, Rodriguez-Farre E, Sunol C: The organochlorine pesticides gamma-hexachlorocyclohexane (lindane), alpha-endosulfan and dieldrin differentially interact with GABA(A) and glycine-gated chloride channels in primary cultures of cerebellar granule cells. Neuroscience. 2003;117(2):397-403. [Article]
- Heusinkveld HJ, Thomas GO, Lamot I, van den Berg M, Kroese AB, Westerink RH: Dual actions of lindane (gamma-hexachlorocyclohexane) on calcium homeostasis and exocytosis in rat PC12 cells. Toxicol Appl Pharmacol. 2010 Oct 1;248(1):12-9. doi: 10.1016/j.taap.2010.06.013. Epub 2010 Jun 21. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Transmitter-gated ion channel activity
- Specific Function
- The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing).
- Gene Name
- GLRA3
- Uniprot ID
- O75311
- Uniprot Name
- Glycine receptor subunit alpha-3
- Molecular Weight
- 53799.775 Da
References
- Vale C, Fonfria E, Bujons J, Messeguer A, Rodriguez-Farre E, Sunol C: The organochlorine pesticides gamma-hexachlorocyclohexane (lindane), alpha-endosulfan and dieldrin differentially interact with GABA(A) and glycine-gated chloride channels in primary cultures of cerebellar granule cells. Neuroscience. 2003;117(2):397-403. [Article]
- Heusinkveld HJ, Thomas GO, Lamot I, van den Berg M, Kroese AB, Westerink RH: Dual actions of lindane (gamma-hexachlorocyclohexane) on calcium homeostasis and exocytosis in rat PC12 cells. Toxicol Appl Pharmacol. 2010 Oct 1;248(1):12-9. doi: 10.1016/j.taap.2010.06.013. Epub 2010 Jun 21. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Glycine binding
- Specific Function
- The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing).
- Gene Name
- GLRB
- Uniprot ID
- P48167
- Uniprot Name
- Glycine receptor subunit beta
- Molecular Weight
- 56121.62 Da
References
- Vale C, Fonfria E, Bujons J, Messeguer A, Rodriguez-Farre E, Sunol C: The organochlorine pesticides gamma-hexachlorocyclohexane (lindane), alpha-endosulfan and dieldrin differentially interact with GABA(A) and glycine-gated chloride channels in primary cultures of cerebellar granule cells. Neuroscience. 2003;117(2):397-403. [Article]
- Heusinkveld HJ, Thomas GO, Lamot I, van den Berg M, Kroese AB, Westerink RH: Dual actions of lindane (gamma-hexachlorocyclohexane) on calcium homeostasis and exocytosis in rat PC12 cells. Toxicol Appl Pharmacol. 2010 Oct 1;248(1):12-9. doi: 10.1016/j.taap.2010.06.013. Epub 2010 Jun 21. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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
- Ratra GS, Casida JE: GABA receptor subunit composition relative to insecticide potency and selectivity. Toxicol Lett. 2001 Jul 6;122(3):215-22. [Article]
- Chen L, Durkin KA, Casida JE: Structural model for gamma-aminobutyric acid receptor noncompetitive antagonist binding: widely diverse structures fit the same site. Proc Natl Acad Sci U S A. 2006 Mar 28;103(13):5185-90. Epub 2006 Mar 10. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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
- Ratra GS, Erkkila BE, Weiss DS, Casida JE: Unique insecticide specificity of human homomeric rho 1 GABA(C) receptor. Toxicol Lett. 2002 Mar 24;129(1-2):47-53. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Zinc ion binding
- Specific Function
- The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Progesterone receptor ...
- Gene Name
- PGR
- Uniprot ID
- P06401
- Uniprot Name
- Progesterone receptor
- Molecular Weight
- 98979.96 Da
References
- Scippo ML, Argiris C, Van De Weerdt C, Muller M, Willemsen P, Martial J, Maghuin-Rogister G: Recombinant human estrogen, androgen and progesterone receptors for detection of potential endocrine disruptors. Anal Bioanal Chem. 2004 Feb;378(3):664-9. Epub 2003 Oct 25. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Zinc ion binding
- Specific Function
- Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissu...
- Gene Name
- ESR1
- Uniprot ID
- P03372
- Uniprot Name
- Estrogen receptor
- Molecular Weight
- 66215.45 Da
References
- Scippo ML, Argiris C, Van De Weerdt C, Muller M, Willemsen P, Martial J, Maghuin-Rogister G: Recombinant human estrogen, androgen and progesterone receptors for detection of potential endocrine disruptors. Anal Bioanal Chem. 2004 Feb;378(3):664-9. Epub 2003 Oct 25. [Article]
- Okubo T, Yokoyama Y, Kano K, Soya Y, Kano I: Estimation of estrogenic and antiestrogenic activities of selected pesticides by MCF-7 cell proliferation assay. Arch Environ Contam Toxicol. 2004 May;46(4):445-53. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- General Function
- Zinc ion binding
- Specific Function
- Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism an...
- Gene Name
- NR1I2
- Uniprot ID
- O75469
- Uniprot Name
- Nuclear receptor subfamily 1 group I member 2
- Molecular Weight
- 49761.245 Da
References
- Kretschmer XC, Baldwin WS: CAR and PXR: xenosensors of endocrine disrupters? Chem Biol Interact. 2005 Aug 15;155(3):111-28. [Article]
Drug created at June 13, 2005 13:24 / Updated at November 03, 2023 23:42