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Details for receptor: CB1

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EndoNet ID: ENR00825

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Synonyms

  • CB1
  • CNR1 isoform 1
  • cannabinoid receptor 1
  • CB-R
  • CANN6
  • CB1R
  • Long

General information

  • Potential therapeutic uses of cannabinoid receptoragonistsinclude themanagement of multiple sclerosis/spinal cord injury, pain, inflammatory disorders, glaucoma, bronchial asthma, vasodilation that accompanies advanced cirrhosis, and cancer. [1]
  • The evoked release of a range of excitatory and inhibitory transmitters from neurons in several brain areas or from certain peripheral neurons can be inhibited by the activation of presynaptic CB1 receptors. [1]
  • Leptin-regulated endocannabinoids are involved in maintaining food intake. [2]
  • CB receptor signalling mechanisms are diverse and dependent on the system studied. [3]
  • Four fatty acid derivatives identified to be arachidonylethanolamide (AEA), 2-arachidonylglycerol (2-AG), 2-arachidonylglycerol ether (noladin ether) and virodhamine have been isolated from both nervous and peripheral tissues. Both AEA and 2-AG have been shown to mimic the pharmacological and behavioural effects of Delta(9)-THC on CB1. [4]
  • CB receptors appear to be intrinsically active and possibly coupled to more than one type of G protein. [3]

Links to other resources

UniProt P21554
Ensembl ENST00000428600

Subunit information

Isoform 1

Sequence 
MKSILDGLA DTTFRTITT DLLYVGSND 
IQYEDIKGD MASKLGYFP QKFPLTSFR 
GSPFQEKMT AGDNPQLVP ADQVNITEF 
YNKSLSSFK ENEENIQCG ENFMDIECF 
MVLNPSQQL AIAVLSLTL GTFTVLENL 
LVLCVILHS RSLRCRPSY HFIGSLAVA 
DLLGSVIFV YSFIDFHVF HRKDSRNVF 
LFKLGGVTA SFTASVGSL FLTAIDRYI 
SIHRPLAYK RIVTRPKAV VAFCLMWTI 
AIVIAVLPL LGWNCEKLQ SVCSDIFPH 
IDETYLMFW IGVTSVLLL FIVYAYMYI 
LWKAHSHAV RMIQRGTQK SIIIHTSED 
GKVQVTRPD QARMDIRLA KTLVLILVV 
LIICWGPLL AIMVYDVFG KMNKLIKTV 
FAFCSMLCL LNSTVNPII YALRSKDLR 
HAFRSMFPS CEGTAQPLD NSMGDSDCL 
HKHANNAAS VHRAAESCI KSTVKIAKV 
TMSVSTDTS AEAL

Binding hormones

  • anandamide (20:4, n-6)
    • Anandamide behaves as a partial cannabinoid receptor agonist with marginally greater CB1 than CB2 affinity but much less CB2 than CB1 efficacy. [1]
  • Virodhamine
    • An endocannabinoid with partial agonist/antagonist activity at the CB1 receptor and agonist activity at the CB2 receptor.
  • 2-Arachidonyl glycerol ether
    • Noladin ether has significantly higher affinity for CB1 than CB2 receptors. [1]
  • 2-Arachidonoylglycerol

Anatomical structures with this receptor

  • cerebellum

    Influences

    • negative GABA
    • negative glutamate

  • hippocampus

    Influences

    • negative GABA

  • peripheral_nerve_system_element

  • heart

    Induced phenotypes

    • atrial muscle contraction
      • Binding of cannabinoids to CB1 receptors decrease contraction in atrial myocardium. [5]

  • lung

  • urinary_bladder

    Induced phenotypes

    • urination
      • Binding to CB1 regulates the voiding of the bladder and prevents incontinence. [6]

  • adrenal_gland

    Influences

    • negative CGRP1
      • Stimulation of the CB1 receptor results in the inhibition of a range of excitatory and inhibitory neurotransmitters, like acetylcholine, noradrenaline, dopamine, 5-hydroxytryptamine, D-aspartate and cholecystokinin. [1]
    • negative acetylcholine
      • Stimulation of the CB1 receptor results in the inhibition of a range of excitatory and inhibitory neurotransmitters, like acetylcholine, noradrenaline, dopamine, 5-hydroxytryptamine, D-aspartate and cholecystokinin. [1]
    • negative cholecystokinin
      • Activation of presynaptic CB1 receptor leads to the inhibition of neurotransmitter release, e.g. cholecystokinin [1]

  • spinal_cord

  • cerebral_cortex

    Influences

    • negative serotonin
      • Stimulation of the CB1 receptor results in the inhibition of a range of excitatory and inhibitory neurotransmitters, like acetylcholine, noradrenaline, dopamine, 5-hydroxytryptamine, D-aspartate and cholecystokinin. [1]

  • reticular_part_of_substantia_nigra

    Influences

    • negative GABA

  • pallidum

  • basket_cell

    Influences

    • negative GABA
Reference