Table 11

P2 receptors in the central nervous system

Region of neurone isolation/recordingAgonistAntagonist/inhibitorReceptorEffectDesensitizationReference
Cerebellum2MeSATP > ADP > ATP > ADO ≫ α,β-meATP > AMP > UTPGDPβSP2YK+channel Ikeuchi and Nishizaki, 1996a
Inferior colliculus2MeSATP > ADP > ATP > AMP > α,β-meATPGDPβSP2YK+channel Ikeuchi and Nishizaki, 1995b
Superior colliculus2MeSATP > ADP > ADO > ATP ≫ AMP (UTP, α,β-meATP inactive)P2YK+channel Ikeuchi et al., 1995b
Dorsal motor nucleus of vagusATP (α,β-meATP inactive)Suramin, RB2 GDPβS-insensitiveP2XRapid inward currentNo Nabekura et al., 1995
HippocampusATPSuraminSlow inward currents12-a No Inoue et al., 1992
Hippocampus2MeSATP > ATP > ADP > α,β-meATPSuraminInward currents Balachandran and Bennett, 1996
HippocampusADP ≥ 2MeSATP > ATP > ADO ≫ AMP (UTP, α,β-meATP inactive)GDPβSP2YK+ channel, ↑ [Ca2+]i Ikeuchiet al., 1996a,b
HippocampusATP = ADP ≫ AMP > α,β-meATP↑[Ca2+]i via PKCP2Y↑ [Ca2+]i Mironov, 1994
Hypoglossal nucleusATPSuramin, PPADSP2Excitation of hypoglossal nerve Funk et al., 1997
ATP inactiveNo inward currents Nabekura et al., 1995
HypothalamusATP, ATPγS > α,β-meATP (ADP inactive)SuraminP2XRapid ↑ [Ca2+]i Slow (>100 s) Chen et al., 1994a
Locus ceruleusATP, α,β-meATPP2X↑ Firing, depolarizationNo Harms et al., 1992
Locus ceruleusα,β-meATP, 2MeSATPSuramin, α,β-meATPP2X↑ Firing, depolarizationNo Tschöpl et al., 1992
Locus ceruleus2MeSATP > ATP = ADP > α,β-meATP↑ Conductance; depolarizationSlow Shen and North, 1993
Locus ceruleusα,β-meATPSuramin, PPADSP2XRapid depolarizationNo Nieber et al., 1997
Suramin, PPADSP2XBlock of synaptic potentials
Medial habenulaATP, α,β-meATPSuraminP2XInward currentsYes Edwardset al., 1992
Suramin, α,β-meATPP2XBlock of synaptic potentials(>100 ms)
Medial vestibular nucleusα,β-meATPSuramin, PPADSP2X↑ FiringNo Chessell et al., 1997
ADPβSPPADS (not suramin)P2Y↑ FiringSlow
Medulla2MeSATP > ADP > ATP ≥GDPβSP2YK+channel Ikeuchi et al., 1995a
α,β-meATP ≥ AMP > UTP
Mesencephalic nucleusATP inactiveIneffective at evoking inward currents Shen and North, 1993
Mesencephalic nucleusATP, ATPγS, α,β-meATPSuraminP2XInward currentsSlow Khakhet al., 1997
Nucleus tractus solitariusATPInward currentsNo Ueno et al., 1992; Nabekura et al., 1995
Parabrachial nucleusATP inactiveNo inward currents Shen and North, 1993
Rostral ventrolateralATP, α,β-meATPSuraminP2X↑ FiringNo Sun et al., 1992
 medullaNo, Yes12-b Ralevic et al., 1996
Striatum2MeSATP > ATP ≥ α,β-meATPSuramin, RB2, PTXP2YDopamine release Zhang et al., 1995
StriatumATP ≫ 2MeSATP ≥ ADP > ADO > AMPK+channel Ikeuchi and Nishizaki, 1995a
Substantia nigraATPInward currents at 1 in 12 neurones Nabekuraet al., 1995
Supraoptic vasopressin neuronesATP = α,β-meATPSuraminP2X↑ FiringNo12-c Dayet al., 1993
SuraminP2Block of excitation to vagus nerve stimulation
Supraoptic magnocellular neurosecretory cells (hypothalamic)α,β-meATP > ATP > UTP > 2MeSATP > βγ-meATPPPADSP2XDepolarization, ↑ input conductanceNo Hiruma and Bourque, 1995
Tuberomammillary nucleusATP ≥ 2MeSATP ≫ α,β-meATP ≥ ADPP2XRapid inward cation currentNo Furukawa et al., 1994
Dorsal horn of spinalATPP2XInward currentsYes Jahr and Jessel, 1983
 cordATP↑ Excitability Fyffe and Perl, 1984
ATP, ATPγSSuraminP2XRapid inward currentsPartial Li and Perl, 1995
Spinal cord neurones2MeSATP ≥ ATP ≥ ADP ≫ ADP (AMP, UTP, α,β-meATP inactive)GDPβSP2YK+currents Ikeuchi and Nishizaki, 1996b
  • 12-a A rapid inward current is also observed, but is blocked by a non-NMDA receptor antagonist.

  • 12-b Desensitization observed in a subpopulation of α,β-meATP-sensitive neurones.

  • 12-c Reproducible responses to ATP on rapid application at <1 min intervals.

  • GDPβS, guanosine-5′-O-(2-thiodiphosphate); G protein inhibitor; PTX, pertussis toxin; RB2, reactive blue 2.