Tmic
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Record Information
Version2.0
Creation Date2009-07-03 22:18:55 UTC
Update Date2014-12-24 20:25:35 UTC
Accession NumberT3D2487
Identification
Common NameApamin (Apis mellifera)
ClassProtein
DescriptionApamin is a component of bee venom and was originally isolated in the Western honey bee (Apis mellifera). It is a polypeptide neurotoxin that acts by blocking SK channels in the central nervous system. Apamin can have therapeutic applications, as the SK channels have been proposed as targets for the treatment of ataxia, epilepsy, memory disorders, and possibly schizophrenia and Parkinson's disease. (3)
Compound Type
  • Amide
  • Amine
  • Animal Toxin
  • Insect Toxin
  • Natural Compound
  • Organic Compound
  • Protein
Protein StructureT3d2487
Synonyms
Synonym
Apamin
Apamin (apis mellifera)
Chemical FormulaNot Available
Average Molecular Mass5223.305 g/mol
CAS Registry Number24345-16-2
SequenceNot Available
Chemical Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available
Biological Properties
StatusDetected and Not Quantified
OriginExogenous
Cellular Locations
  • Extracellular
Biofluid LocationsNot Available
Tissue LocationsNot Available
PathwaysNot Available
ApplicationsNot Available
Biological RolesNot Available
Chemical RolesNot Available
Physical Properties
StateLiquid
AppearanceClear solution.
Experimental Properties
PropertyValue
Melting PointNot Available
Boiling PointNot Available
Solubility>10 mg/mL
LogPNot Available
Predicted PropertiesNot Available
Spectra
SpectraNot Available
Toxicity Profile
Route of ExposureInjection (sting/bite) (4)
Mechanism of ToxicityApamin binds to the SK channels (small conductance Ca2+-activated K+ channels) in the brain and spinal cord and inhibits them, likely by acting as a pore blocker. Inhibition of SK channels by apamin increases the neuronal excitability and lowers the threshold for generating an action potential. (3)
MetabolismFree toxin may be removed by opsonization via the reticuloendothelial system (primarily the liver and kidneys) or it may be degraded through cellular internalization via the lysosomes. Lysosomes are membrane-enclosed organelles that contain an array of digestive enzymes, including several proteases.
Toxicity ValuesLD50: 6.00 mg/kg (Intravenous, Mouse) (1)
Lethal DoseNot Available
Carcinogenicity (IARC Classification)No indication of carcinogenicity to humans (not listed by IARC).
Uses/SourcesApamin is a the main component of the venom of the Western honey bee (Apis mellifera). Apamin can have therapeutic applications, as the SK channels have been proposed as targets for the treatment of ataxia, epilepsy, memory disorders, and possibly schizophrenia and Parkinson's disease. (3)
Minimum Risk LevelNot Available
Health EffectsApamin poisoning may cause development of optic neuritis and atrophy. Serious cases may lead to atrial fibrillation, cerebral infarction, acute myocardial infarction, Fisher's syndrome, Guillain-Barre syndrome, claw hand caused by Ulnar nerve entrapment, and haemorrhaging in the lungs. (3)
SymptomsApamin poisoning is characterized by burning or stinging pain, swelling, and redness at the site of the bee sting, and may be followed by swelling of the tongue and throat, difficulty breathing, and shock. (3)
TreatmentPatients poisoned with bee venom can be treated with anti-inflammatory medication, antihistamines and oral prednisolone. (3)
Normal Concentrations
Not Available
Abnormal Concentrations
Not Available
DrugBank IDNot Available
HMDB IDNot Available
PubChem Compound ID16129677
ChEMBL IDNot Available
ChemSpider ID17286484
KEGG IDNot Available
UniProt IDP01500
OMIM ID
ChEBI IDNot Available
BioCyc IDNot Available
CTD IDNot Available
Stitch IDApamin
PDB IDNot Available
ACToR IDNot Available
Wikipedia LinkNot Available
References
Synthesis ReferenceNot Available
MSDST3D2487.pdf
General References
  1. Rothman RB: Does phentermine inhibit monoamine oxidase? Lancet. 1999 Apr 17;353(9161):1362-3. [10218558 ]
  2. Habermehl G (1981). Venomous animals and their toxins. Berlin: Springer-Verlag,
  3. Wikipedia. Apamin. Last Updated 31 March 2009. [Link]
  4. Wikipedia. Insect toxins. Last Updated 19 February 2009. [Link]
Gene Regulation
Up-Regulated GenesNot Available
Down-Regulated GenesNot Available

Targets

General Function:
Small conductance calcium-activated potassium channel activity
Specific Function:
Forms a voltage-independent potassium channel activated by intracellular calcium. Activation is followed by membrane hyperpolarization. Thought to regulate neuronal excitability by contributing to the slow component of synaptic afterhyperpolarization. The channel is blocked by apamin (By similarity).
Gene Name:
KCNN1
Uniprot ID:
Q92952
Molecular Weight:
59986.87 Da
References
  1. Wikipedia. Apamin. Last Updated 31 March 2009. [Link]
General Function:
Small conductance calcium-activated potassium channel activity
Specific Function:
Forms a voltage-independent potassium channel activated by intracellular calcium. Activation is followed by membrane hyperpolarization. Thought to regulate neuronal excitability by contributing to the slow component of synaptic afterhyperpolarization. The channel is blocked by apamin.
Gene Name:
KCNN2
Uniprot ID:
Q9H2S1
Molecular Weight:
63759.03 Da
References
  1. Wikipedia. Apamin. Last Updated 31 March 2009. [Link]
General Function:
Small conductance calcium-activated potassium channel activity
Specific Function:
Forms a voltage-independent potassium channel activated by intracellular calcium. Activation is followed by membrane hyperpolarization. Thought to regulate neuronal excitability by contributing to the slow component of synaptic afterhyperpolarization. The channel is blocked by apamin.
Gene Name:
KCNN3
Uniprot ID:
Q9UGI6
Molecular Weight:
82025.305 Da
References
  1. Wikipedia. Apamin. Last Updated 31 March 2009. [Link]