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Antiallergic activity and mode of action of N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(6-methyl-3- pyridyl)acrylamide in experimental animals.
Arzneimittelforschung. 1993 Feb; 43(2):148-54.A

Abstract

Antiallergic effects of AL-3264 (N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(6-methyl-3- pyridyl)acrylamide, CAS 118420-47-6) were compared with those of ketotifen, oxatomide, azelastine and tranilast in experimental animals. AL-3264 inhibited passive cutaneous anaphylaxis (PCA) in rats with an ED50 value of 6.1 mg/kg p.o. In inhibiting PCA, AL-3264 was the most potent among the antiallergic drugs examined. The anti-PCA effect of AL-3264 was long-lasting. Tolerance was not produced by repeated administration of AL-3264. AL-3264 inhibited antigen-induced bronchoconstriction in actively sensitized rats and in passively sensitized guinea pigs, with ED50 values of 14.5 and 0.44 mg/kg p.o., respectively. In the in vitro experiments, AL-3264 inhibited 5-lipoxygenase activity of guinea pig leukocytes with an IC50 value of 4.9 mumol/l, being the most potent among antiallergic drugs examined, and suppressed the antigen-induced histamine release from rat peritoneal mast cells with an IC50 value of 12.2 mumol/l. AL-3264 antagonized histamine-induced contractions in isolated guinea pig trachea with an IC50 value of 0.16 mumol/l. These results suggest that AL-3264 is an orally active, potent and long-lasting antiallergic compound which inhibits 5-lipoxygenase activity, histamine release and histamine H1 receptors at the similar concentrations.

Authors+Show Affiliations

Department of Pharmacology, Dainippon Pharmaceutical Co., Ltd, Suital Osaka, Japan.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

7681286

Citation

Ishii, K, et al. "Antiallergic Activity and Mode of Action of N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(6-methyl-3- Pyridyl)acrylamide in Experimental Animals." Arzneimittel-Forschung, vol. 43, no. 2, 1993, pp. 148-54.
Ishii K, Yakuo I, Seto Y, et al. Antiallergic activity and mode of action of N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(6-methyl-3- pyridyl)acrylamide in experimental animals. Arzneimittelforschung. 1993;43(2):148-54.
Ishii, K., Yakuo, I., Seto, Y., Kita, A., Nakamura, H., & Nishikawa, Y. (1993). Antiallergic activity and mode of action of N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(6-methyl-3- pyridyl)acrylamide in experimental animals. Arzneimittel-Forschung, 43(2), 148-54.
Ishii K, et al. Antiallergic Activity and Mode of Action of N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(6-methyl-3- Pyridyl)acrylamide in Experimental Animals. Arzneimittelforschung. 1993;43(2):148-54. PubMed PMID: 7681286.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Antiallergic activity and mode of action of N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(6-methyl-3- pyridyl)acrylamide in experimental animals. AU - Ishii,K, AU - Yakuo,I, AU - Seto,Y, AU - Kita,A, AU - Nakamura,H, AU - Nishikawa,Y, PY - 1993/2/1/pubmed PY - 1993/2/1/medline PY - 1993/2/1/entrez SP - 148 EP - 54 JF - Arzneimittel-Forschung JO - Arzneimittelforschung VL - 43 IS - 2 N2 - Antiallergic effects of AL-3264 (N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(6-methyl-3- pyridyl)acrylamide, CAS 118420-47-6) were compared with those of ketotifen, oxatomide, azelastine and tranilast in experimental animals. AL-3264 inhibited passive cutaneous anaphylaxis (PCA) in rats with an ED50 value of 6.1 mg/kg p.o. In inhibiting PCA, AL-3264 was the most potent among the antiallergic drugs examined. The anti-PCA effect of AL-3264 was long-lasting. Tolerance was not produced by repeated administration of AL-3264. AL-3264 inhibited antigen-induced bronchoconstriction in actively sensitized rats and in passively sensitized guinea pigs, with ED50 values of 14.5 and 0.44 mg/kg p.o., respectively. In the in vitro experiments, AL-3264 inhibited 5-lipoxygenase activity of guinea pig leukocytes with an IC50 value of 4.9 mumol/l, being the most potent among antiallergic drugs examined, and suppressed the antigen-induced histamine release from rat peritoneal mast cells with an IC50 value of 12.2 mumol/l. AL-3264 antagonized histamine-induced contractions in isolated guinea pig trachea with an IC50 value of 0.16 mumol/l. These results suggest that AL-3264 is an orally active, potent and long-lasting antiallergic compound which inhibits 5-lipoxygenase activity, histamine release and histamine H1 receptors at the similar concentrations. SN - 0004-4172 UR - https://www.unboundmedicine.com/medline/citation/7681286/Antiallergic_activity_and_mode_of_action_of_N_[4_[4__diphenylmethyl__1_piperazinyl]butyl]_3__6_methyl_3__pyridyl_acrylamide_in_experimental_animals_ L2 - https://medlineplus.gov/allergy.html DB - PRIME DP - Unbound Medicine ER -