Ten spinal-cord-injured males who exhibited autonomic dysreflexia during electroejaculation were given sublingual calcium channel blocker nifedipine pretreatment to prevent this complication. Nifedipine was successful in decreasing peak systolic, diastolic, and mean blood pressures during the procedure. The use of nifedipine resulted in fewer aborted trials and allowed higher energy delivery du...

We previously reported the small organic N-type calcium channel blocker NP078585 that while efficacious in animal models for pain, exhibited modest L-type calcium channel selectivity and substantial off-target inhibition against the hERG potassium channel. Structure-activity studies to optimize NP078585 preclinical properties resulted in compound 16, which maintained high potency for N-type cal...

BACKGROUND The macrolide antibiotics clarithromycin and erythromycin may potentiate calcium-channel blockers by inhibiting cytochrome P450 isoenzyme 3A4. However, this potential drug interaction is widely underappreciated and its clinical consequences have not been well characterized. We explored the risk of hypotension or shock requiring hospital admission following the simultaneous use of cal...

High conductance, calcium- and voltage-activated potassium (BK) channels are widely expressed in mammals. In some tissues, the biophysical properties of BK channels are highly affected by coexpression of regulatory (beta) subunits. beta1 and beta2 subunits increase apparent channel calcium sensitivity. The beta1 subunit also decreases the voltage sensitivity of the channel and the beta2 subunit...

Introduction Single-center and observational studies have suggested that calcium channel blocking agents may decrease the expression of sepsis in individual populations. In the renal transplant population, a role for calcium channel blockers in allograft protection and in prevention of sepsis has been postulated. We hypothesized that any important survival benefit or risk related to chronic use...

Peptide toxins have proved to be useful agents, both in discriminating between different components of native calcium channel currents and in the molecular isolation and designation of their cloned channel counterparts. Here, we describe the isolation and characterization of the biochemical and physiological properties of a novel 74-amino acid peptide toxin (DW13.3) extracted from the venom of ...

BACKGROUND We have previously shown that calcium channel antagonists inhibit in vitro meningioma growth. This study examines the effect of calcium channel antagonists on in vivo xenograft meningioma growth. METHODS Meningioma cells taken from human patients were mixed with Matrigel and injected into the subcutaneous space in the flank of nude mice. These animals were treated with calcium chan...

AIMS/INTRODUCTION Recent studies have shown the association between blood pressure variability and cardiovascular events. The present study was designed to investigate the relationship between antihypertensive drug class and home blood pressure variability in patients with type 2 diabetes. MATERIALS AND METHODS We compared home blood pressure variability among patients treated with calcium ch...

Large-conductance calcium-activated potassium (BK) channels are colocalized with calcium channels at sites of exocytosis at the presynaptic terminals throughout the nervous system. It is expected that their activation would provide negative feedback to transmitter release, but the opposite is sometimes observed. Attempts to resolve this apparent paradox based on alterations in action potential ...

BACKGROUND This report presents 13 years of experience with vasodilator therapy for primary pulmonary hypertension (PPH) in children. Two eras were involved: between 1982 and 1987, oral calcium channel blockers were the only agents available for long-term therapy; after 1987, prostacyclin (PGI2) has been available for long-term intravenous use. METHODS AND RESULTS Seventy-four children underw...