ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammation

European Journal of Pharmacology

Volumn 435, Issue 1, 2002, Pages 43-57

  Olsen, Uffe B ^a   Eltorp, Christina T ^a   Ingvardsen, Bente K ^a   Jorgensen, Tine K ^a   Lundbak, Jens A ^a   Thomsen, Christian ^a   Hansen, Anker J ^a  

^a NOVO NORDISK A S   (Denmark)

Author keywords

Histamine; Histamine H1 receptor; Inflammation; Pain; Spinal cord

Indexed keywords

1 [3 (10,11 DIHYDRO 5H DIBENZO[A,D]CYCLOHEPTEN 5 YLIDENE)PROPYL] 3 PIPERIDINECARBOXYLIC ACID; 1 [3(10,11 DIHYDRO 5H DIBENZO[A,D]CYCLOHEPTEN 5 YLIDENE) 1 PROPYL] 3 PIPERIDINE CARBOXYLIC ACID; 1,3 DITOLYLGUANIDINE; 2 DIPROPYLAMINO 7 HYDROXYTETRALIN; AMITRIPTYLINE; ASTEMIZOLE; BENZOMORPHAN DERIVATIVE; CAPSAICIN; CARBOXYLIC ACID DERIVATIVE; CARRAGEENAN; CHLORPROMAZINE; CLOMIPRAMINE; DIPHENHYDRAMINE; DOXEPIN; FORMALDEHYDE; HISTAMINE; HISTAMINE H1 RECEPTOR; HISTAMINE H1 RECEPTOR ANTAGONIST; MEPYRAMINE; MIANSERIN; MORPHINE; PHENYLQUINONE; PROMETHAZINE; SULPIRIDE; THIOPERAMIDE; TRIPROLIDINE; TRITIUM; UNCLASSIFIED DRUG;

ANALGESIC ACTIVITY; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIDROMIC STIMULATION; ANTIINFLAMMATORY ACTIVITY; ANTINOCICEPTION; ARTICLE; CELL ACTIVATION; CENTRAL NERVOUS SYSTEM; CONTROLLED STUDY; DOSE RESPONSE; DRUG ACTIVITY; DRUG EFFICACY; DRUG MECHANISM; DRUG SELECTIVITY; DRUG TOLERANCE; EDEMA; EVOKED RESPONSE; FEMALE; GUINEA PIG; HUMAN; HUMAN CELL; INFLAMMATION; MALE; MAST CELL; MOUSE; NEUROTRANSMISSION; NOCICEPTION; NONHUMAN; PAIN; PRIORITY JOURNAL; RAT; RODENT; SPINAL CORD DORSAL HORN; STIMULATION; THERMAL STIMULATION; WRITHING TEST;

ANIMALS; BENZOQUINONES; BINDING SITES; CALCITONIN GENE-RELATED PEPTIDE; CALCIUM; CALCIUM CHANNELS; CAPSAICIN; CARRAGEENAN; CENTRAL NERVOUS SYSTEM; CHO CELLS; CRICETINAE; DISEASE MODELS, ANIMAL; EDEMA; EXTRAVASATION OF DIAGNOSTIC AND THERAPEUTIC MATERIALS; GENE EXPRESSION; GUINEA PIGS; HISTAMINE; HISTAMINE H1 ANTAGONISTS; MICE; NEUROGENIC INFLAMMATION; PAIN; PAIN MEASUREMENT; PIPERIDINES; PROTO-ONCOGENE PROTEINS C-FOS; PYRILAMINE; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, HISTAMINE H1; SPECIES SPECIFICITY; SPINAL CORD; TRANSFECTION; TRITIUM;

EID: 0037126942     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(01)01556-4     Document Type: Article

References (71)

1. Protein kinase C inhibitors decrease hyperalgesia and C-fiber hyperexcitability in the streptozotocin-diabetic rat
2. Histamine-induced edema in the rat paw. Effect of capsaicin denervation and a CGRP receptor antagonist
3. Evidence of a key-role for histamine from mast cells in the analgesic effect of clomipramine in rats
4. Constitutive activity of the histamine H1 receptor reveals inverse agonism of histamine H1 receptor antagonists
5. Pharmacology of non-sedating H1 antihistamines
6. Effects of cutaneous histamine application in patients with sympathetic reflex dystrophy
7. Dephenhydramine potentiates narcotic but not endogenous opioid analgesia
8. Heterogeneity of histamine H-1 receptors species variations in tritiated mepyramine binding of brain membranes
9. Trigeminal antidromic vaso dilatation and plasma extravasation in the rat
10. The inflammatory reaction induced by formalin in the rat paw
11. Inhibition of calcineurin inhibits the desensitization of capsaicin-evoked currents in cultured dorsal root ganglion neurones from adult rats
12. The effects of substance P on histamine and 5 hydroxy tryptamine release in the rat
13. Effect of neonatal treatment with capsaicin on carrageenan-induced paw edema in the rat
14. Effects of anti depressant drugs on different receptors in the brain
15. Septide and neurokinin-a are high-affinity ligands on the nk-1 receptor - Evidence from homologous versus heterologous binding analysis
16. The binding of tritiated mepyramine to histamine H-1 receptors in guinea-pig brain
17. The tail-flick and formalin tests in rodents: Changes in skin temperature as a confounding factor
18. Possible mechanism of c-fos expression in trigeminal nucleus caudalis following cortical spreading depression
19. Studies on the vascular permeability induced by intrathecal substance P and bradykinin in the rat
20. Direct evidence for neurogenic inflammation and its prevention by denervation and by pretreatment with capsaicin
21. Superficial dorsal horn neurons identified by intracutaneous histamine: Chemonociceptive responses and modulation by morphine
22. Action of peptides and other algesic agents on para vascular pain receptors of the isolated perfused rabbit ear
23. Gene expression of histamine H1 receptor in guinea pig primary sensory neurons: A relationship between H1 receptor mRNA-expressing neurons and peptidergic neurons
24. Antinociception following 1,3,-di-o-tolylguanidine, a selective sigma receptor ligand
25. 1,3-Di-o-tolylguanidine (DTG) differentially affects acute and tonic formalin pain: Antagonism by rimcazole
26. H1-receptor-mediated excitation and facilitation of the heat response by histamine in canine visceral polymodal receptors studied in vitro
27. Investigation into the role of histamine-receptors in rodent antinociception
28. Substance P as neurogenic mediator of antidromic vaso dilation and neurogenic plasma extravasation
29. Mast-cells synthesize, store, and release nerve growth-factor
30. Dorsal root reflexes and cutaneous neurogenic inflammation after intradermal injection of capsaicin in rats
31. The sensory-efferent function of capsaicin-sensitive sensory neurons
32. Gamma-aminobutyric acid-B, but not gamma-aminobutyric acid-A receptor activation, inhibits electrically evoked substance P-like immunoreactivity release from the rat spinal cord in vitro
33. Evidence for hypernociception induction following histamine H1 receptor activation in rodents
34. Antinociceptive actions of spinal nonsteroidal anti-inflammatory agents on the formalin test in the rat
35. Preserved acute pain and reduced neuropathic pain in mice lacking PKC-gamma
36. Inhibition of hyperalgesia by ablation of lamina I spinal neurons expressing the substance P receptor
37. Role of histamine H(1) receptor in pain perception: A study of the receptor gene knockout mice
38. Mu-Opioid receptor-mediated reduction of neuronal calcium current occurs via a G-o-type GTP-binding protein
39. The modulation of inflammatory oedema by calcitonin gene-related peptide
40. Opiate and histamine H1 receptors are present on some substance P-containing dorsal root ganglion cells
41. Localization of opiate and histamine H1-receptors in the primate sensory ganglia and spinal cord
42. Mast cells in the nervous system
43. Antidepressant-induced analgesia in chronic non-malignant pain a meta-analysis of 39 placebo-controlled studies
44. Cutaneous vascular permeability in the rat increases caused by histamine and histamine-like agents
45. The distribution of histamine H-1 receptors in the rat brain an auto radiographic study
46. Histamine-immunoreactive nerve fibers in the mammalian spinal cord
47. The major role of peripheral release of histamine and 5-hydroxytryptamine in formalin-induced nociception
48. Regional distribution of calcitonin gene-related peptide-like substance P-like cholecystokinin-like met-5 enkephalin-like and dynorphin a 1-8-like materials in the spinal cord and dorsal root ganglia of adult rats effects of dorsal rhizotomy and neonatal capsaicin
49. Systemic morphine suppresses noxious stimulus-evoked Fos protein-like immunoreactivity in the rat spinal cord
50. In vivo occupation of cerebral histamine H1-receptors evaluated with 3H-mepyramine may predict sedative properties of psychotropic drugs
51. Antihistamines as analgesics
52. Do dorsal root reflexes augment peripheral inflammation?
53. Clinical efficacy of antihistaminics as analgesics
54. The capsaicin test in mice for evaluating tachykinin antagonists in the spinal cord
55. Peripheral antinociceptive actions of desipramine and fluoxetine in an inflammatory and neuropathic pain test in the rat
56. Specific C-receptors for itch in human skin
57. [H-3] 7-OH-DPAT labels both dopamine-D3 receptors and sigma-sites in the bovine caudate-nucleus
58. P-chlorophenylalanine-reversible reduction of sigma binding sites by chronic imipramine treatment in rat brain
59. Neurotrophins and hyperalgesia
60. Psychophysical studies of the itch sensation and itchy skin allokinesis produced by intracutaneous injection of histamine
61. Regulation of the human histamine H1 receptor stably expressed in Chinese hamster ovary cells
62. Sigma opiates and certain antipsychotic drugs mutually inhibit tritium-labeled dextro skf-10047 2′ hydroxy-5 9-dimethyl-2-allyl-6 7-benzomorphan and tritium-labeled haloperidol binding in guinea-pig brain membranes
63. Is there a difference in the affinity of histamine H-1 receptor antagonists for CNS and peripheral receptors? An in vitro study
64. Tritium labeled doxepin interactions with histamine H-1 receptors and other sites in guinea-pig and rat brain homogenates
65. Radiolabelling of NNC 05-1869, a compound for treatment of neurogenic pain
66. Neurogenic and tissue-mediated components of formalin-induced edema evidence for supraspinal regulation
67. Immunoreactive calcitonin gene-related peptide and substance P coexist in sensory neurons to the spinal cord and interact in spinal behavioral responses of the rat
68. Substance P and calcitonin gene-related peptide synergistically modulate the gain of the nociceptive flexor withdrawal reflex in the rat
69. Electrophysiological and binding studies on intact Ncb-20 cells suggest presence of a low affinity sigma receptor
70. Transport mechanism of an h-1-antagonist at the blood-brain-barrier-transport mechanism of mepyramine using the carotid injection technique
71. (3H)-(+)-pentazocine binding to sigma recognition sites in human cerebellum