Receptor binding and biological activity of the dermorphin analog Tyr-D-Arg2-Phe-Sar (TAPS)

European Journal of Pharmacology

Volumn 416, Issue 1-2, 2001, Pages 83-93

  Vonhof, Stefan ^a,e   Barone, Frank C ^c   Price, William J ^c   Paakkari, Pirkko ^b   Millison, James H ^b   Feuerstein, Giora Z ^c   Sirén, Anna Leena K ^b,d  

^a UNIVERSITY OF GÖTTINGEN   (Germany)

^b Uniformed Services University of the Health Sciences and the Walter Reed National Military Medical Center   (United States)

^c SmithKline Beecham ^*  (United States)

^d MAX PLANCK INSTITUTE OF EXPERIMENTAL MEDICINE   (Germany)

^e Zentrum Innere Medizin   (Germany)

Author keywords

Antinociception; Dermorphin; Opioid; Receptor subtype; TAPS (Tyr D Arg2 Phe Sar4); Tetrapeptide

Indexed keywords

5 GUANYLYLIMIDODIPHOSPHATE; DERMORPHIN DERIVATIVE; GUANOSINE TRIPHOSPHATE; KAPPA OPIATE RECEPTOR; MU OPIATE RECEPTOR; NUCLEOTIDE; OPIATE RECEPTOR; RECEPTOR SUBTYPE; SIGMA OPIATE RECEPTOR; SODIUM; TETRAPEPTIDE; TYROSINYLDEXTROARGINYLPHENYLALANYLSARCOSINE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BINDING SITE; DRUG ACTIVITY; GUINEA PIG; MALE; NOCICEPTION; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR BINDING;

ANALGESICS; ANIMALS; BINDING, COMPETITIVE; CATALEPSY; DOSE-RESPONSE RELATIONSHIP, DRUG; ELECTRIC STIMULATION; GUINEA PIGS; ILEUM; INJECTIONS, SPINAL; MALE; MUSCLE CONTRACTION; NALOXONE; NOCICEPTORS; OLIGOPEPTIDES; OPIOID PEPTIDES; PULMONARY VENTILATION; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, OPIOID; TIME FACTORS;

EID: 0035937529     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(01)00874-3     Document Type: Article

References (40)

1. Pharmacological data on dermorphins, a new class of potent opioid peptides from amphibian skin
2. Kappa opioid antagonist effects of systemically administered nor-binaltorphimine in a thermal antinociception assay in rhesus monkeys
3. Guanine nucleotides differentiate agonist and antagonist interactions with opiate receptors
4. 1 opiate binding sites
5. Opiate binding in calf thalamic membranes: A selective mu1 binding assay
6. Structure-activity relationships of dermorphin synthetic analogues
7. International Union of Pharmacology: XII. Classification of opioid receptors
8. Binding affinity and selectivity of opioids at Mu, Delta and Kappa receptors in monkey brain membranes
9. 2 sites in the guinea pig ileum
10. Visualization of mu1 opiate receptors in rat brain using a computerized autoradiographic subtraction technique
11. Dissociation of opioid antinociception and central gastrointestinal propulsion in the mouse: Studies with naloxonazine
12. Differential regulation of adenylyl cyclase activity by mu and delta opioids in rat caudate putamen and nucleus accumbens
13. Inhibition of norepinephrine release from rat cortex slices by opioids: Differences among agonists in sensitivities to antagonists suggest receptor heterogeneity
14. Characterization of dermorphin binding to membranes of rat brain and heart
15. Dimeric dermorphin analogues as mu-receptor probes on rat brain membranes
16. 1 (high affinity) opioid binding sites
17. Separation of opioid analgesia from respiratory depression: Evidence for different receptor mechanisms
18. Naloxonazine actions in vivo
19. Tritiated kappa receptor antagonist norbinaltorphimine: Synthesis and in vitro binding in three different tissues
20. Autoradiographic distribution of mu1- and mu2-opioid binding in the mouse central nervous system
21. LIGAND: A versatile computerized approach for characterization of ligand-binding systems
22. Affinity of drugs and peptides for U-69593-sensitive and -insensitive kappa opiate binding sites: The U-69593-insensitive sites appears to be the beta endorphin-specific epsilon receptor
23. Antagonism of dermorphin-induced catalepsy with naloxone, TRH-analog CG3703 and the benzodiazepine antagonist, RO 15-1788
24. 1 receptor-mediated effect
25. Evidence for differential opioid mu 1- and 2-receptor-mediated regulation of heart rate in the conscious rat
26. 2-Phe-sarcosine induces opioid analgesia and respiratory stimulation - A role of mu-1 opioid receptors?
27. Identification and characterization of three new alternatively spliced μ-opioid receptor isoforms
28. Isolation and expression of a novel alternatively spliced mu opioid receptor isoform, MOR-1F
29. Differential blockade by naloxonazine of two μ opiate actions: Analgesia and inhibition of gastrointestinal transit
30. Effects of chronic morphine exposure on opioid inhibition of adenylyl cyclase in 7315c cell membranes: A useful model for the study of tolerance at μ opioid receptors
31. Opioid analgesics and antagonists
32. Synthesis and pharmacological activity of dermorphin and its N-terminal sequence
33. 2-dermorphin analog: A potent and long-lasting analgesic activity after subcutaneous administration
34. 2-substituted tetrapeptides
35. 2-opioid receptors in SH-SY5Y cells
36. Time course characteristics of tolerance development to continuously infused antinociceptive agents in rat spinal cord
37. 2-adrenoceptor antagonism
38. Multiple agonist-affinity states of opioid receptors: Regulation of binding by guanyl nucleotides in guinea pig cortical, NG108-15, and 7415c cell membranes
39. Mu opiate isoreceptors: Differentiation with kappa antagonists
40. 2 opioid-receptors