Pregnancy related hormones increase CYP3A mediated buprenorphine metabolism in human hepatocytes: a comparison to CYP3A substrates nifedipine and midazolam
This study quantified the impact of PRHs on CYP3A protein concentrations and buprenorphine metabolism in human hepatocytes, and compared the magnitude of these effects to nifedipine and midazolam metabolism.Methods: Sandwich-cultured human hepatocytes (SCHH) from female donors were exposed to PRHs, administered in combination across a range of physiologically relevant concentrations, for 72 h. Absolute protein concentrations of CYP3A4, CYP3A5, and CYP3A7 in SCHH membrane fractions were quantified by nanoLC-MS/MS, and norbuprenorphine (nor-BUP), dehydro-nifedipine (dehydro-NIF), and 1-hydroxy-midazolam (1-OH-MDZ) formation...
Source: Frontiers in Pharmacology - July 5, 2023 Category: Drugs & Pharmacology Source Type: research

Pharmacological Studies on the Ca < sup > 2+ < /sup > Influx Pathways in Platelet-Activating Factor (PAF)-Induced Mouse Urinary Bladder Smooth Muscle Contraction
In this study, we examined the Ca2+ influx pathways involved in PAF-induced BTI and OC in the mouse UBSM. PAF (10-6 M) induced BTI and OC in mouse UBSM. However, the PAF-induced BTI and OC were completely suppressed by extracellular Ca2+ removal. PAF-induced BTI and OC frequencies were markedly suppressed by voltage-dependent Ca2+ channel (VDCC) inhibitors (verapamil (10-5 M), diltiazem (10-5 M), and nifedipine (10-7 M)). However, these VDCC inhibitors had a minor effect on the PAF-induced OC amplitude. The PAF-induced OC amplitude in the presence of verapamil (10-5 M) was strongly suppressed by SKF-96365 (3 × 10-5 M), an...
Source: Biological and Pharmaceutical Bulletin - July 2, 2023 Category: Drugs & Pharmacology Authors: Ge Liu Keisuke Obara Kento Yoshioka Yoshio Tanaka Source Type: research

Pharmacological Studies on the Ca < sup > 2+ < /sup > Influx Pathways in Platelet-Activating Factor (PAF)-Induced Mouse Urinary Bladder Smooth Muscle Contraction
In this study, we examined the Ca2+ influx pathways involved in PAF-induced BTI and OC in the mouse UBSM. PAF (10-6 M) induced BTI and OC in mouse UBSM. However, the PAF-induced BTI and OC were completely suppressed by extracellular Ca2+ removal. PAF-induced BTI and OC frequencies were markedly suppressed by voltage-dependent Ca2+ channel (VDCC) inhibitors (verapamil (10-5 M), diltiazem (10-5 M), and nifedipine (10-7 M)). However, these VDCC inhibitors had a minor effect on the PAF-induced OC amplitude. The PAF-induced OC amplitude in the presence of verapamil (10-5 M) was strongly suppressed by SKF-96365 (3 × 10-5 M), an...
Source: Biological and Pharmaceutical Bulletin - July 2, 2023 Category: Drugs & Pharmacology Authors: Ge Liu Keisuke Obara Kento Yoshioka Yoshio Tanaka Source Type: research

Pharmacological Studies on the Ca < sup > 2+ < /sup > Influx Pathways in Platelet-Activating Factor (PAF)-Induced Mouse Urinary Bladder Smooth Muscle Contraction
In this study, we examined the Ca2+ influx pathways involved in PAF-induced BTI and OC in the mouse UBSM. PAF (10-6 M) induced BTI and OC in mouse UBSM. However, the PAF-induced BTI and OC were completely suppressed by extracellular Ca2+ removal. PAF-induced BTI and OC frequencies were markedly suppressed by voltage-dependent Ca2+ channel (VDCC) inhibitors (verapamil (10-5 M), diltiazem (10-5 M), and nifedipine (10-7 M)). However, these VDCC inhibitors had a minor effect on the PAF-induced OC amplitude. The PAF-induced OC amplitude in the presence of verapamil (10-5 M) was strongly suppressed by SKF-96365 (3 × 10-5 M), an...
Source: Biological and Pharmaceutical Bulletin - July 2, 2023 Category: Drugs & Pharmacology Authors: Ge Liu Keisuke Obara Kento Yoshioka Yoshio Tanaka Source Type: research

Blood pressure medication use and postpartum hospital readmission among preeclampsia patients
CONCLUSION: We found that low dose of blood pressure medication was associated with increased odds for readmission within 6 weeks among those with preeclampsia. We recommend that clinicians balance the preference to reduce a blood pressure medication dose with the possible concern that too low a dose may place certain patients on track for hospital readmission after discharge.PMID:37358058 | DOI:10.1080/10641955.2023.2226210 (Source: Hypertension in Pregnancy)
Source: Hypertension in Pregnancy - June 26, 2023 Category: OBGYN Authors: Timothy Gesner Joshua Fogel Lennox Bryson Source Type: research

Nifedipine Gastro Retentive Drug Delivery System Formulation Characterization and Evaluation
Swati Ughade, R. D. Baw.ar* and D. R. Mundhada (Source: Indian Journal of Pharmaceutical Sciences)
Source: Indian Journal of Pharmaceutical Sciences - June 23, 2023 Category: Drugs & Pharmacology Source Type: research

Molecules, Vol. 28, Pages 4869: Design, Synthesis, Molecular Modeling, and Biological Evaluation of Novel Pyrimidine Derivatives as Potential Calcium Channel Blockers
lsaidan Pyrimidines play an important role in modern medical fields. They have a wide spectrum of biological activities such as antimicrobial, anticancer, anti-allergic, anti-leishmanial, antioxidant agents and others. Moreover, in recent years, 3,4-dihydropyrimidin-2(1H)ones have attracted researchers to synthesize them via Biginelli reaction and evaluate their antihypertensive activities as bioisosters of Nifedipine, which is a famous calcium channel blocker. Our new target compounds were prepared through one-pot reaction of thiourea 1, ethyl acetoacetate 2 and/or 1H-indole-2-carbaldehyde, 2-chloroquinoline-3-carbald...
Source: Molecules - June 20, 2023 Category: Chemistry Authors: Yasser M. Zohny Samir M. Awad Maha A. Rabie Omar Awad Alsaidan Tags: Article Source Type: research

Cannabis arteritis presenting with Raynaud ’s and digital ulcerations: a case-based review of a controversial thromboangiitis obliterans-like condition
AbstractThromboangiitis obliterans (TAO), or Buerger ’s disease, is a non-atherosclerotic inflammatory disease of the small and medium-sized arteries, veins, and nerves of the legs and arms, strongly associated with the use of tobacco products in young adults. Cannabis arteritis (CA), an entity with similar clinical and pathological features, has be en described in marijuana users as a subtype of TAO. Distinction between TAO and CA is challenging, given that most patients use tobacco and marijuana products concomitantly. Herein, we report the case of a male in his late forties who was referred to rheumatology with a 2-mo...
Source: Clinical Rheumatology - June 16, 2023 Category: Rheumatology Source Type: research

Retraction Note: Influence of nimodipine and nifedipine on intrapulmonary shunting – a comparison to other vasoactive drugs
(Source: Intensive Care Medicine)
Source: Intensive Care Medicine - June 16, 2023 Category: Intensive Care Source Type: research