The objective of this study was to compare the antispasmodic activities of atropine, verapamil, (-)scopolamine n-butyl bromide and propinox in the isolated human and guinea pig gallbladder strip models. Concentration-response curves for each of the agents were obtained in both models following administration of carbachol. Atropine was the only drug to show marked activity in the guinea pig gallbladder model (ED50 = 2.75 x 10(-7) M); the remaining drugs elicited less inhibition of a similar order of magnitude (ED50 = 1.65 x 10(-5), 4.18 x 10(-6) and 2.71 x 10(-5) M for verapamil, [-]scopolamine n-butyl bromide and propinox, respectively). In contrast, results obtained from the human gallbladder strip model revealed differences among the drugs (ED50 = 5.03 x 10(-8), 1.34 x 10(-6), 6.63 x 10(-6) and 5.45 x 10(-5) M for atropine, propinox, verapamil and [-]scopolamine n-butyl bromide, respectively). Based on these results, propinox showed a relative potency in the human gallbladder that was 20.22-fold higher than that in the guinea pig model followed by atropine (5.47-fold) and verapamil (2.49-fold), whereas (-)scopolamine n-butyl bromide was 0.07 times more potent in the guinea pig model. Regression analysis of ED50 values showed a lack of correlation between the two models (r = 0.44). Considering interspecies variations, further studies in human tissues are needed to evaluate the efficacy of antispasmodic drugs.

Download full-text PDF

Source
http://dx.doi.org/10.1358/mf.1999.21.10.795736DOI Listing

Publication Analysis

Top Keywords

guinea pig
20
n-butyl bromide
16
pig gallbladder
12
gallbladder strip
12
isolated human
8
human guinea
8
strip models
8
antispasmodic drugs
8
-scopolamine n-butyl
8
bromide propinox
8

Similar Publications

Background: Adjusting thickening agent proportions in nanoemulsion gel (NG) balances its transdermal and topical delivery properties, making it more effective for dermatophytosis treatment.

Methods: Carbomer 940 and α-pinene were used as model thickening agent and antifungal, respectively. A series of α-pinene NGs (αNG1, αNG2, αNG3) containing 0.

View Article and Find Full Text PDF

5-Hydroxyindoleacetic acid (5-HIAA), a vital metabolite of serotonin (5-HT), is crucial for understanding metabolic pathways and is implicated in various mental disorders. In situ monitoring of 5-HIAA is challenging due to the lack of affinity ligands and issues with electrochemical fouling. We present an advanced sensing approach that integrates customizable molecular imprinting polymer (MIP) with self-driven galvanic redox potentiometry (GRP) for precise, real-time in vivo monitoring of 5-HIAA.

View Article and Find Full Text PDF

Background: There is limited research on how rodent owners use and perceive veterinary services and what the demand for pet insurance for these species is.

Methods: An online survey of owners of pet rodents (guinea pigs, hamsters, rats, gerbils and mice) measured owner confidence in recognising signs of illness, their opinions on and use of veterinary services and their willingness to purchase pet insurance.

Results: A total of 1700 respondents completed the survey.

View Article and Find Full Text PDF

Novel Hsp90α inhibitor inhibits HSV-1 infection by suppressing the Akt/β-catenin pathway.

Int J Antimicrob Agents

January 2025

School of Pharmacy, Shenzhen University Medical School, Shenzhen University, Shenzhen 518055, China. Electronic address:

The prevalence of herpes simplex virus type 1 (HSV-1) infection and the emergence of drug-resistant HSV-1 strains posts a significant global health challenge, necessitating the urgent development of effective anti-HSV-1 drugs. As one of the most prevalent molecular chaperones, heat shock protein 90 α (Hsp90α) has been extensively demonstrated to regulate a range of viral infections, thus representing a promising antiviral target. In this study, we identified JD-13 as a novel Hsp90α inhibitor and explored its capability in inhibiting HSV-1 infection.

View Article and Find Full Text PDF

An understanding of intracellular mechanisms by which fentanyl and other synthetic opioids exert adverse effects on breathing is needed. Using freely moving adult male guinea pigs, we administered the nitric oxide synthase (NOS) inhibitor, L-NAME (N-nitro-L-arginine methyl ester), to determine whether nitrosyl factors, such as nitric oxide and S-nitrosothiols, play a role in fentanyl-induced respiratory depression. Ventilatory parameters were recorded by whole body plethysmography to determine the effects of fentanyl (75 μg/kg, IV) in guinea pigs that had received a prior injection of vehicle (saline), L-NAME or the inactive D-isomer, D-NAME (both at 50 μmol/kg, IV), 15 min beforehand.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!