[11C]-GR89696, a potent kappa opiate receptor radioligand; in vivo binding of the R and S enantiomers

Nuclear Medicine and Biology

Volumn 29, Issue 1, 2002, Pages 47-53

  Ravert, Hayden T ^a   Scheffel, Ursula ^a   Mathews, William B ^a   Musachio, John L ^a   Dannals, Robert F ^a  

^a DEPARTMENT OF PATHOLOGY   (United States)

Author keywords

C 11; GR103545; GR89696; Kappa opioid receptors; PET

Indexed keywords

3,4 DICHLORO N METHYL N [2 (1 PYRROLIDINYL)CYCLOHEXYL]BENZENEACETAMIDE; 4 [(3,4 DICHLOROPHENYL)ACETYL] 3 (1 PYRROLIDINYLMETHYL) 1 PIPERAZINECARBOXYLIC ACID METHYL ESTER; 4 [(3,4 DICHLOROPHENYL)ACETYL] 3 (1 PYRROLIDINYLMETHYL) 1 PIPERAZINECARBOXYLIC ACID METHYL ESTER C 11; C 1977; CARBON 11; CYPRODIME; ESTER DERIVATIVE; FORMIC ACID DERIVATIVE; FUMARIC ACID DERIVATIVE; KAPPA OPIATE RECEPTOR; MESYLIC ACID; N METHYL N [7 (1 PYRROLIDINYL) 1 OXASPIRO[4.5]DEC 8 YL]BENZENEACETAMIDE; NALTRINDOLE; RADIOLIGAND; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BRAIN REGION; CEREBELLUM; CHIRALITY; CONTROLLED STUDY; DRUG BINDING; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; ENANTIOMER; HYPOTHALAMUS; ISOTOPE LABELING; MALE; MOUSE; NONHUMAN; OLFACTORY BULB; PRECURSOR;

ADRENERGIC ALPHA-AGONISTS; ANIMALS; BRAIN; MICE; MORPHINANS; NALTREXONE; NARCOTIC ANTAGONISTS; PIPERAZINES; PYRROLIDINES; RECEPTORS, OPIOID, KAPPA; STEREOISOMERISM; TISSUE DISTRIBUTION;

EID: 0036151266     PISSN: 09698051     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0969-8051(01)00285-2     Document Type: Article

References (19)

1. GR89696 is a kappa-2 opioid receptor agonist and a kappa-1 opioid receptor antagonist in the guinea pig hippocampus
2. Synthesis and in vitro characterization of fluorinated U-50488 analogs for PET studies of kappa opioid receptors
3. Opiate receptor avidity and cerebral blood flow in Alzheimer's disease
4. International Union of Pharmacology. XII. Classification of opioid receptors
5. Anticonvulsant effects of U-54494A and U-50488H in genetically epilepsy-prone rats and DBA/2 mice: A possible involvement of glycine/NMDA receptor complex
6. Imaging opiate receptors in the human brain by positron tomography
7. A series of novel, highly potent and selective agonists for the κ-opioid receptor
8. 11C]methyl)naltrindole and PET
9. Pharmacological and anatomical evidence of selective μ, δ, and κ opioid receptor binding in rat brain
10. Synthesis of carbon-11 labeled kappa opiate receptor agonists
11. A potent new class of κ-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylaminomethyl]piperazines
12. 11C](±)U-50488H)
13. 3H]U-69593 binding sites in rat brain: Evidence for κ opioid receptor subtypes
14. Binaltorphimine and nor-binaltrophimine, potent and selective κ-opioid receptor antagonists
15. 11C]GR89696): Synthesis and in vivo binding to kappa opiate receptors
16. Quantification of human opiate receptor concentration and affinity using high and low specific activity [C-11]diprenorphine and positron emission tomography
17. κ-Opioid antagonist improves cellular bioenergetics and recovery after traumatic brain injury
18. U-50,488: A selective and structurally novel non-mu (kappa) opioid agonist
19. The kappa opioid receptor: Evidence for the different subtypes