Epinastine (WAL 810CL) modulates the noncholinergic contraction in guinea-pig airways in vitro by a prejunctional 5-HT1-like receptor

European Respiratory Journal

Volumn 9, Issue 7, 1996, Pages 1433-1438

  Dupont, L J ^a   Meade, C J ^b   Demedts, M G ^a   Verleden, G M ^a  

^a UNIVERSITY OF LEUVEN   (Belgium)

^b BOEHRINGER INGELHEIM PHARMA GMBH AND CO KG   (Germany)

Author keywords

5 HT1 like receptor; epinastine; guinea pig airways; neuropeptides; nonadrenergic noncholinergic contraction

Indexed keywords

ACETYLCHOLINE; ALPHA ADRENERGIC RECEPTOR BLOCKING AGENT; ATROPINE; CHLORPHENIRAMINE; EPINASTINE; INDOMETACIN; KETANSERIN; METHYSERGIDE; METITEPINE; PHENTOLAMINE; SEROTONIN 1 ANTAGONIST; SEROTONIN 1 RECEPTOR; SEROTONIN 2 ANTAGONIST; SEROTONIN 3 ANTAGONIST; SUBSTANCE P; TACHYKININ; THIOPERAMIDE; TROPISETRON; DIBENZAZEPINE DERIVATIVE; HISTAMINE H1 RECEPTOR ANTAGONIST; IMIDAZOLE DERIVATIVE; SEROTONIN AGONIST; SEROTONIN RECEPTOR;

AIRWAY; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG RECEPTOR BINDING; ELECTROSTIMULATION; FEMALE; GUINEA PIG; MALE; NONADRENERGIC NONCHOLINERGIC NERVE; NONHUMAN; PRIORITY JOURNAL; SMOOTH MUSCLE CONTRACTION; ANIMAL; BRONCHUS; DRUG EFFECT; IN VITRO STUDY; MUSCLE CONTRACTION; PHYSIOLOGY; SMOOTH MUSCLE; TRACHEA;

ANIMALS; BRONCHI; DIBENZAZEPINES; FEMALE; GUINEA PIGS; HISTAMINE H1 ANTAGONISTS; IMIDAZOLES; MALE; MUSCLE CONTRACTION; MUSCLE, SMOOTH; RECEPTORS, SEROTONIN; SEROTONIN AGONISTS; TRACHEA;

EID: 0029661802     PISSN: 09031936     EISSN: None     Source Type: Journal    
DOI: 10.1183/09031936.96.09071433     Document Type: Article

References (32)

1. Jackson WR, Copp FC, Cullen JD, et al. Chemical design of peripherally acting compounds. Clin Exp Pharmacol Physiol 1992; 19: 17-23.
2. 1 receptor antagonists for CNS and peripheral receptors? An in vitro study. Eur J Pharmacol 1993; 232: 199-205.
3. 1-antihistaminic properties: chemistry of epinastine. Arzneim Forsch (Drug Res) 1990; 40: 440-446.
4. 1-antagonist 3-amino-9,13b-dihydro-1H-dibenz[c,f]imidazol[1,5-a]azepine hydrochloride in volunteers. Arzneim Forsch (Drug Res) 1987; 37: 569-572.
5. Adamus WS, Oldigs-Kerber J, Lohmann H. Antihistamine activity and central effects of WAL 801 CL in man. Eur J Pharmacol 1987; 33: 381-385.
6. Fügner A, Bechtel WD, Kühn FJ, Mierau J. In vitro and in vivo studies of the nonsedating antihistamine epinastine. Arzneim Forsch (Drug Res) 1988; 38: 1446-1453.
7. Tasaka K, Kamei C, Izushi K, Tsujimoto S, Yoshida T. Comparison of pharmacological properties of optical isomers and a racemic mixture of epinastine. Arzneim Forsch (Drug Res) 1991; 41: 219-223.
8. Tasaka, K, Kamei C, Nakamura S. Inhibitory effect of epinastine on bronchoconstriction induced by histamine, platelet-activating factor and serotonin in guinea-pigs and rats. Arzneim Forsch (Drug Res) 1994; 44: 327-329.
9. Kanai Y, Misawa M. Effect of WAL 801, a new antiallergic drug, on chemical mediator-induced broncho-constriction in guinea-pigs. Eur J Pharmacol 1990; 183: 227-228.
10. Misawa M, Kanai Y. Effect of the new antiallergic drug epinastine on chemical mediator-induced bronchocon-strictions in guinea-pigs. Arzneim Forsch (Drug Res) 1991; 41: 1145-1149.
11. Misawa M, Kanai Y, Chiba Y. Effects of the new antiallergic drug epinastine and ketotifen on repeated antigen challenge-induced airway hyperresponsiveness in rats. Arzneim Forsch (Drug Res) 1991; 41: 1277-1280.
12. 1 antiallergic agent epinastine. Arzneim Forsch (Drug Res) 1994; 44: 1338-1342.
13. Grundstrom N, Andersson RGG, Wikberg JES. Pharmacological characterization of the autonomous nervous innervation of the guinea-pig tracheobronchial smooth muscle. Acta Pharmacol Toxicol 1981; 49: 150-157.
14. Maggi CA, Patacchini R, Rovero P, Santicioli P. Tachykinin receptors and noncholinergic bronchoconstriction in the guinea-pig isolated bronchi. Am Rev Respir Dis 1991; 144: 363-367.
15. 2) receptors mediate nonadrenergic noncholinergic responses to electrical field stimulation and resiniferatoxin in guinea-pig trachea. Can J Physiol Pharmacol 1994; 72: 182-188.
16. Martling CR, Saria A, Andersson P, Lundberg JM. Capsaicin preteatment inhibits vagal cholinergic and noncholinergic control of pulmonary mechanisms in the guinea-pig. Naunyn Sch Arch Pharmacol 1984; 325: 343-348.
17. 1-like receptor. J Appl Physiol 1994; 77: 1135-1141.
18. Ward JK, Fox AJ, Barnes PJ, Belvisi MG. Inhibition of excitatory nonadrenergic noncholinergic bronchocon-striction in guinea-pig airways in vitro by activation of an atypical 5-HT receptor. Br J Pharmacol 1994; 111: 1095-1102.
19. Verleden GM, Pype JL, Demedts MG. Ketotifen modulates noncholinergic contraction in guinea-pig airways in vitro by a prejunctional nonhistamine receptor. J Allergy Clin Immunol 1994; 94: 207-214.
20. 1 on nonadrenergic, noncholinergic contraction in guinea-pig bronchi. Br J Pharmacol 1990; 101: 13-14.
21. Glennon RA. Central serotonin receptors as targets for drug research. J Med Chem 1987; 30: 1-12.
22. Stretton D, Miura M, Belvisi MG, Barnes PJ. Calcium-activated potassium channels mediate prejunctional inhibition of peripheral sensory fibres. Proc Natl Acad Sci USA 1992; 89: 1325-1329.
23. Richardson BP, Hoyer D. Selective agonists and antagonists at 5-hydroxytryptamine receptor subtypes. In: Paoletti R, ed. Serotonin: From Cell Biology to Pharmacology and Therapeutics. Norwell, Kluwer Academic Publishers, 1990; pp. 265-275.
24. Kamikawa Y. Inhibitory effects of antiallergic drugs on cholinergic and noncholinergic neurotransmission of guinea-pig bronchial smooth muscle in vitro. Ann Allergy 1989; 63: 59-63.
25. 2-adrenoceptors and opiate receptors. Eur J Pharmacol 1989; 163: 15-23.
26. Li CG, Rand MJ. Evidence that part of the NANC relaxant response of guinea-pig trachea to electrical field stimulation is mediated by nitric oxide. Br J Pharmacol 1991; 102: 91-94.
27. Verleden GM, Pype JL, Demedts MG. Furosemide and bumetamide, but not nedocromil sodium, modulate nonadrenergic relaxation in guinea-pig trachea in vitro. Am J Respir Crit Care Med 1994; 149: 138-144.
28. Belvisi MG, Miura M, Stretton D, Barnes PJ. Endogenous vasoactive intestinal peptide and nitric oxide modulate cholinergic neurotransmission in guinea-pig trachea. Eur J Pharmacol 1993; 231: 97-102.
29. Bradley PB, Engel G, Feniuk W, et al. Proposals for the classification and nomenclature of functional receptors for 5-hydroxytryptamine. Neuropharmacology 1986; 25: 563-576.
30. Barnes PJ. Asthma as an axon reflex. Lancet 1986; i: 242-245.
31. Takishima T, Tamura G, Yamauchi K, Miyamoto T, Shida T. Clinical study of WAL 801 CL (epinastine) on adult bronchial asthma: multicenter, double-blind, controlled study vs ketotifen fumarate. J Clin Ther Med 1992; 8 (Suppl 1): 169-197.
32. Bousquet J, Godard P, Michel FB. Antihistamines in the treatment of asthma. Eur Respir J 1992; 5: 1137-1142.