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Pharmacological Effects of Hachi-mi-jio-gan Extract (Harncare®)on the Contractile Response and on Pharmacologically Relevant Receptors in the Rat Bladder
- Source :
- YAKUGAKU ZASSHI. 129:957-964
- Publication Year :
- 2009
- Publisher :
- Pharmaceutical Society of Japan, 2009.
-
Abstract
- Hachi-mi-jio-gan extract (Harncare®; HE), a galenical produced from the traditional Chinese herbal mixture Ba-Wei-Die-Huang-Wan, has been reported to improve lower urinary tract symptoms (LUTS) in patients. The present study was undertaken to clarify the pharmacological effects of HE on smooth muscle contraction and on pharmacologically relevant (muscarinic, 1,4-DHP and purinergic) receptors in the rat bladder. Additionally, the effects of repeated oral treatment with HE on the hepatic cytochrome P-450 (CYP) and on blood biochemical values in rats were examined. HE (10 mg/ml) inhibited significantly the acetylcholine-induced contraction of isolated rat bladder strips. The pD2 value in the absence and presence of HE (10 mg/ml) was 5.14±0.16 and 3.99±0.17, respectively. HE (0.1 to 10 mg/ml) inhibited the specific binding of [N-methyl-3H]scopolamine methyl chloride ([3H]NMS), (+)-[3H]PN 200-110 and αβ-methylene ATP [2,8-3H]tetrasodium salt ([3H]αβ-MeATP) in the rat bladder in a concentration-dependent manner. The respective IC50 values were 6.85±0.94, 7.08±0.72 and 1.34±0.23 mg/ml. Based on IC50 values, the binding activity of HE for purinergic receptors was shown to be significantly (about 7 times) greater than that for muscarinic and 1,4-DHP receptors. Repeated oral administration of HE (10, 30 and 100 mg/kg/day) for 4 weeks had little or no effect on the level and activity of hepatic CYP or on blood biochemical values in rats. In conclusion, the present study has shown that HE exerts significant binding activity for pharmacologically relevant receptors in the rat bladder and a relaxant effect on the acetylcholine-induced contraction of isolated muscle strips. HE seemed to exhibit little pharmacokinetic interaction with drugs.
- Subjects :
- Pharmacology
medicine.medical_specialty
Contraction (grammar)
business.industry
Purinergic receptor
Pharmaceutical Science
Smooth muscle contraction
medicine.disease
Endocrinology
Lower urinary tract symptoms
Oral administration
Internal medicine
Muscarinic acetylcholine receptor
medicine
medicine.symptom
Receptor
business
Muscle contraction
Subjects
Details
- ISSN :
- 13475231 and 00316903
- Volume :
- 129
- Database :
- OpenAIRE
- Journal :
- YAKUGAKU ZASSHI
- Accession number :
- edsair.doi...........643a9a0f895add253ad4f0d7993f4853