A review of the demonstration and characterization of opiate receptors is described. The concept of subpopulations of receptors is discussed and evidence presented suggesting that analgesia due to opiates, enkephalins and acupuncture is mediated through a single subclass of receptor sites distinct from those mediating respiratory effects.
BeecherH.K.: Pain in the men wounded in battle. Ann. Surgery123; 96–105, 1946.
2.
MayerD. and LiebeskindJ.: Pain reduction by focal electrical stimulation of the brain: an anatomical and behavioral analysis. Brain. Res68; 73–93, 1974.
3.
HosobuchiYRosslerJ., BloomF. and GuillerminR.: Stimulation of human periaqueductal grey for pain relief increases immunoreactive β-endorphin in ventricular fluid. Science203; 279–281, 1971.
4.
HughesJ.T.: Isolation of an endogenous compound from brain with pharma-cological properties similar to morphine. Brain. Res88: 295–308, 1975.
5.
TereniusL. and WahlstromA.: Morphine-like ligand for opiate receptors human CSF. Life Sci. 16; 1765–1769, 1975.
6.
PasternakG.W.GoodmanR. and SnyderS.H.: An endogenous morphine-like factor in mammalian brain. Life Sci. 16; 1765–1769, 1975.
7.
HughesJ.SmithT.W.KosterlitzH.FathergillL.MorganB.A. and MorrisH.: Identification two related pentapeptides from the brain with potent opiate agonist activity. Nature258; 577–579, 1975.
8.
SimantovR. and SnyderS.H.: Morphine-like factors in mammalian brain: structure elucidation and interactions with opiate receptors. Proc. Nat. Acad. Sci. 73; 2515–2519, 1976.
9.
SimantovR.KuharM.PasternakG.W. and SnyderS.H. The regional distribution of the morphine-like factor enkephalin in monkey brain. Brain Research106: 189–197, 1976.
10.
BeaumontA. and HughesJ: Biology of Opioid Peptides. Ann. Rev. Pharmacol. Toxicol. 19; 245–267, 1979.
11.
JonesB.N. SternA.S.LewisR.V.KimuraS.SteinS.UndenfriendS. and ShivelyJ.: Structure of two adrenal polypeptides containing multiple enkephalin sequences. Arch. Biochem. Biophys. 204; 392–395, 1980.
12.
GorensteinC. and SnyderS.H.: Characterization of enkephalinases in Exogenous and endogenous opiate agonists and antagonists edWayW. L.(Pergamon Press, New York) pp. 345–348, 1980.
13.
SnyderS.A.: Opiate receptors in the brain. New Eng. J. Med. 296; 266, 1977.
14.
OmuraY.: Patho-physiology of acupuncture treatment: effects of acupuncture on cardiovascular and nervous systems, Acupuncture and Electro-Therapeutics Research, The International Journal1: 51–141. 1975.
15.
OmuraY.: Electro-acupuncture: its electro-physiological bases and criteria for effectiveness and safety, Part I, Acupuncture and Electro-Therapeutics Research, The International Journal. 1; 157-181, 1975.
16.
OmuraY.: Pathophysiology of acupuncture effects, ACTH and morphine-like substances, pain, phantom sensations (phantom pain, itch and coldness), brain micro-circulation, and memory, Acupuncture and Electro-Therapeutics Research, The Internation Journal. 2; 1–31, 1976.
17.
OmuraY.: Editorial: pain threshold measurement before and after acupuncture: controversial results of radiant heat method and electrical method, and the roles of ACTH-like substances and endorphins, Acupuncture and Electro-Therapeutics Research, The International Journal3: 1–21. 1978.
18.
OmuraY.: Editorial: Part II: Impressions of the history making acupuncture symposia held in Peking and travel experiences in the People's Republic of China, Acupuncture and Electro-Therapeutics Research, The International Journal5; 1–28, 1980.
19.
PertC.B., and SnyderS.H.: Opiate Receptor: Demonstration in nervous tissue. Science179; 1011–1014, 1973.
20.
TereniusL.: Characteristics of the receptor for narcotic analgesics in synaptic plasma membrane fraction from rat brain. Acta Pharmacol. Toxicol. 32; 377–384, 1973.
21.
SimonE.HillerJ. and EdelmanI.: Stereo specific binding of the potent narcotic analgesic 3H-etorphine to rat brain homogenate. Proc. Nat. Acad. Sci. 70; 1947–1949, 1973.
22.
ScatchardG.: The attractions of proteins for small molecules and ions. Ann. NY. Acad. Sci. 51; 660–672, 1949.
23.
PasternakG.W. and SnyderS.H.: Opiate receptor binding: effects of enzymatic treatments. Molec. Pharm.10; 183–194, 1975.
24.
PasternakG.W. and SnyderS.H.: Enzymatic treatment that discrimate between agonist and antagonist interactions. Molec. Pharmacol. 11; 735–744, 1975.
25.
CreeseI. and SnyderS.H.: Receptor binding and pharmacological activity of opiates in the guinea pig intestine. J. Pharmacol. Exp. Therap. 194; 205–219, 1975.
26.
PertC.B.SnowmanA. and SnyderS.H.: Localization of opiate receptor binding in synaptic membranes of rat brain. Brain Res. 70; 184–188, 1974.
27.
PertA. and YakshT.: Sites of morphine-induced analgesia in the primate brain: relation to pain pathways. Brain Res. 80; 135–140, 1974.
28.
JacquetY.F. and LajthaA.: Morphine action at central nervous system sites in rat: analgesia or hyperanalgesia depending on site and dose. Science182; 490–492, 1973.
29.
KuharM.J.PertC.B. and SnyderS.H.: Regional distribution of opiate receptor binding in monkey and human brain. Nature245; 447–450, 1973.
30.
PertC.B.PasternakG.W. and SynderS.H.: Opiate agonists and antagonists discriminated by receptor binding in brain. Science182; 1359–1361, 1973.
31.
PasternakG.W.SnowmanA. and SnyderS.H.: Selective enhancement of 3H-opiate agonist binding by divalent cations. Molec. Pharmacol. 11; 735–744, 1975.
32.
WilsonH.A.PasternakG.W. and SnyderS.H.: Differentiation of opiate agonist and antagonist binding by protein modifying reagents. Nature253; 448–450, 1975.
33.
LordJ.A.H.WaterfieldH.HughesJ. and KosterlitzH.: Endogenous opioid peptides: multiple agonists and receptors. Nature267; 495–500, 1977.
34.
ChangK.J. and CuatrecasasP.: Multiple opiate receptors: enkephalins and morphine bind to receptors of different specificity. J. Biol. Chern. 254; 2610–2618, 1979.
35.
ChangK.J.CooperB.R.HazumE. and CuatrecasasP.: Multiple opiate receptors: Different regional distribution in the brain and differential binding of opiates and opioid peptides. Molec. Pharmacol. 16; 91–104, 1979.
36.
PasternakG.W. and SnyderS.H.: Identification of novel high affinity opiate receptor binding in rat brain. Nature253; 563–565, 1975
37.
PasternakG.W. and HahnP.: Long-acting opiate agonists and antagonists: 14 hydroxydi hydromorphine hydrazones. J. Med. Chern. 23; 674–677, 1980.
38.
PasternakG.W.ChildersS.R. and SnyderS.H.: Opiate analgesia: evidence for mediation by a subpopulation of opiate receptors. Science208; 514–516, 1980.
39.
PasternakG.W.ChildersS.R. and SnyderS.H.: Naloxazone, a long acting opiate antagonist: effects in intact animals and on opiate receptor binding in vitro. J. Pharmacol. Exp. Therap. 214; 455–462, 1980.
40.
PasternakG.W.: Multiple opiate receptors: 3H-ethylketocyclazoci ne receptor binding and ketocyclazoci ne analgesia. Proc. Nat. Acad. Sci.77; 3691–3694, 1980.
41.
ZhangA.Z. and PasternakG.W.: Opiates and enkephalins: A common binding site mediates than analgesic actions in rats. Life Sci. (in press).
42.
PasternakG.W.BuattiM.C. and SpiegelK.: The binding and analgesic properties of a sigma opiate, SKF 10,047. J. Pharmacol. Exp. Therap. (in press).
43.
HazumE.ChangJ.CuatrecasasP. and PasternakG.W.: Naloxazone irreversibly inhibits the high affinity binding of 125I_D_ala2_ D-leu5-enkephalin. Life Sci. (in press).
44.
PasternakG.W.: Opiate, enkephalin and endorphin analgesia: their relationship to a single subpopulation of opiate receptors. Neurology (in press).
45.
WolozinB.L. and PasternakG.W.: A classification of multiple opiate and enkephalin binding sites in the central nervous system. Proc. Nat. Acad. Sci. USA. (in press).
46.
ZhangA.Z. and PasternakG.W.: Mu and delta opiate receptors: corre-lation with high and low affiniy opiate binding sites. Europ. J. Pharmacol67; 323–324, 1980.
47.
PasternakG.W.ZhangA.Z. and TecottL.: Developmental differences between high and low affinity opiate binding sites: their relationship to analgesia and respiratory depression. Life Sci. 27; 1185–1190, 1980.
48.
ZhangA.Z. and PasternakG.W.: Ontogeny of opioid pharmacology and receptors: high and low affinity sites differences. Europ. J. Pharmacol. (in press).
49.
BuattiM.C. and PasternakG.W.: Multiple opiate receptors: phylogenetic differences. Brain Res. (in press).
50.
ZhouG-ZXuS.F. and ZhangA.Z.: Effect on naloxazone or electro-acupuncture analgesia in rabbits. Acupuncture & Electro-Therapy Research, The International Journal5; 197–200, 1980.