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Effect of a major metabolite of the antiallergic drug repirinast on phosphodiesterase and adenylate cyclase activities.
Arzneimittelforschung. 1995 Jan; 45(1):33-5.A

Abstract

MY-1250 (5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano [3,2-c]quinoline-2-carboxylic acid, CAS 63768-47-8), a major metabolite of the antiallergic drug repirinast (MY-5116, CAS 73080-51-0), inhibits antigen-induced histamine release from rat peritoneal mast cells. MY-1250 causes a rapid increase in cyclic adenosine monophosphate (AMP) levels in rat peritoneal mast cells. MY-1250 inhibited cyclic AMP phosphodiesterase activities from rat peritoneal cells and guinea pig lung tissue in a concentration dependent manner with IC50 values of 2000 mumol/l and 1670 mumol/l, respectively. However, MY-1250 showed no effect on adenylate cyclase activity from rat peritoneal cells. These results suggest that the inhibitory effect of MY-1250 on histamine release may be partly due to the inhibition of cyclic AMP phosphodiesterase activity.

Authors+Show Affiliations

Pharmaceuticals Laboratory, Mitsubishi Kasei Corporation, Yokohama, 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

7534459

Citation

Yamada, N, et al. "Effect of a Major Metabolite of the Antiallergic Drug Repirinast On Phosphodiesterase and Adenylate Cyclase Activities." Arzneimittel-Forschung, vol. 45, no. 1, 1995, pp. 33-5.
Yamada N, Arai Y, Funayama K, et al. Effect of a major metabolite of the antiallergic drug repirinast on phosphodiesterase and adenylate cyclase activities. Arzneimittelforschung. 1995;45(1):33-5.
Yamada, N., Arai, Y., Funayama, K., Kadowaki, S., Takahashi, K., & Umezu, K. (1995). Effect of a major metabolite of the antiallergic drug repirinast on phosphodiesterase and adenylate cyclase activities. Arzneimittel-Forschung, 45(1), 33-5.
Yamada N, et al. Effect of a Major Metabolite of the Antiallergic Drug Repirinast On Phosphodiesterase and Adenylate Cyclase Activities. Arzneimittelforschung. 1995;45(1):33-5. PubMed PMID: 7534459.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of a major metabolite of the antiallergic drug repirinast on phosphodiesterase and adenylate cyclase activities. AU - Yamada,N, AU - Arai,Y, AU - Funayama,K, AU - Kadowaki,S, AU - Takahashi,K, AU - Umezu,K, PY - 1995/1/1/pubmed PY - 1995/1/1/medline PY - 1995/1/1/entrez SP - 33 EP - 5 JF - Arzneimittel-Forschung JO - Arzneimittelforschung VL - 45 IS - 1 N2 - MY-1250 (5,6-dihydro-7,8-dimethyl-4,5-dioxo-4H-pyrano [3,2-c]quinoline-2-carboxylic acid, CAS 63768-47-8), a major metabolite of the antiallergic drug repirinast (MY-5116, CAS 73080-51-0), inhibits antigen-induced histamine release from rat peritoneal mast cells. MY-1250 causes a rapid increase in cyclic adenosine monophosphate (AMP) levels in rat peritoneal mast cells. MY-1250 inhibited cyclic AMP phosphodiesterase activities from rat peritoneal cells and guinea pig lung tissue in a concentration dependent manner with IC50 values of 2000 mumol/l and 1670 mumol/l, respectively. However, MY-1250 showed no effect on adenylate cyclase activity from rat peritoneal cells. These results suggest that the inhibitory effect of MY-1250 on histamine release may be partly due to the inhibition of cyclic AMP phosphodiesterase activity. SN - 0004-4172 UR - https://www.unboundmedicine.com/medline/citation/7534459/Effect_of_a_major_metabolite_of_the_antiallergic_drug_repirinast_on_phosphodiesterase_and_adenylate_cyclase_activities_ DB - PRIME DP - Unbound Medicine ER -