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ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammation.
Eur J Pharmacol. 2002 Jan 18; 435(1):43-57.EJ

Abstract

The tricyclic compound (R)-1-(3-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-propyl)-3-piperidine carboxylic acid (ReN 1869) is a novel, selective histamine H(1) receptor antagonist. It is orally available, well tolerated, easily enters the central nervous system (CNS) but no adverse effects are seen in mice at 300 mg/kg. ReN 1869 at 0.01-10 mg/kg is antinociceptive in tests of chemical nociception in rodents (formalin, capsaicin, phenyl quinone writhing) but not in thermal tests (hot plate and tail flick). ReN 1869 amplifies the analgesic action of morphine but does not show tolerance after chronic dosing. Moreover, the compound is effective against inflammation of neurogenic origin (antidromic nerve stimulation, histamine-evoked edema) but not in carrageenan-induced inflammation. We suggest that ReN 1869, via H(1) blockade, counteracts the effect of histamine liberated from activated mast cells and inhibits pain transmission in the dorsal spinal cord. ReN 1869 represents a new class of antihistamines with pain-relieving properties that probably is mediated centrally through histamine H(1) receptors but alternative mechanisms of action cannot be excluded.

Authors+Show Affiliations

Department of General Pharmacology, Novo Nordisk A/S, 2760 Maaloev, Denmark.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

11790377

Citation

Olsen, Uffe B., et al. "ReN 1869, a Novel Tricyclic Antihistamine, Is Active Against Neurogenic Pain and Inflammation." European Journal of Pharmacology, vol. 435, no. 1, 2002, pp. 43-57.
Olsen UB, Eltorp CT, Ingvardsen BK, et al. ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammation. Eur J Pharmacol. 2002;435(1):43-57.
Olsen, U. B., Eltorp, C. T., Ingvardsen, B. K., Jørgensen, T. K., Lundbaek, J. A., Thomsen, C., & Hansen, A. J. (2002). ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammation. European Journal of Pharmacology, 435(1), 43-57.
Olsen UB, et al. ReN 1869, a Novel Tricyclic Antihistamine, Is Active Against Neurogenic Pain and Inflammation. Eur J Pharmacol. 2002 Jan 18;435(1):43-57. PubMed PMID: 11790377.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - ReN 1869, a novel tricyclic antihistamine, is active against neurogenic pain and inflammation. AU - Olsen,Uffe B, AU - Eltorp,Christina T, AU - Ingvardsen,Bente K, AU - Jørgensen,Tine K, AU - Lundbaek,Jens A, AU - Thomsen,Christian, AU - Hansen,Anker J, PY - 2002/1/16/pubmed PY - 2002/4/3/medline PY - 2002/1/16/entrez SP - 43 EP - 57 JF - European journal of pharmacology JO - Eur J Pharmacol VL - 435 IS - 1 N2 - The tricyclic compound (R)-1-(3-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-propyl)-3-piperidine carboxylic acid (ReN 1869) is a novel, selective histamine H(1) receptor antagonist. It is orally available, well tolerated, easily enters the central nervous system (CNS) but no adverse effects are seen in mice at 300 mg/kg. ReN 1869 at 0.01-10 mg/kg is antinociceptive in tests of chemical nociception in rodents (formalin, capsaicin, phenyl quinone writhing) but not in thermal tests (hot plate and tail flick). ReN 1869 amplifies the analgesic action of morphine but does not show tolerance after chronic dosing. Moreover, the compound is effective against inflammation of neurogenic origin (antidromic nerve stimulation, histamine-evoked edema) but not in carrageenan-induced inflammation. We suggest that ReN 1869, via H(1) blockade, counteracts the effect of histamine liberated from activated mast cells and inhibits pain transmission in the dorsal spinal cord. ReN 1869 represents a new class of antihistamines with pain-relieving properties that probably is mediated centrally through histamine H(1) receptors but alternative mechanisms of action cannot be excluded. SN - 0014-2999 UR - https://www.unboundmedicine.com/medline/citation/11790377/ReN_1869_a_novel_tricyclic_antihistamine_is_active_against_neurogenic_pain_and_inflammation_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0014299901015564 DB - PRIME DP - Unbound Medicine ER -