Vasodilatation with pinacidil. Mode of action in rat resistance vessels.

Abstract:

:Pinacidil is a newly developed antihypertensive vasodilator, proposed to belong to the new group of smooth muscle relaxants, the K+ channel openers. The in vitro effects of pinacidil on induced tone, smooth muscle membrane potential and 86Rb and 42K efflux from rat resistance vessels (internal diameter about 200 microns) were studied. Tone induced with noradrenaline was concentration-dependently inhibited by pinacidil. Responses to electrical field stimulation were also inhibited. However, tone induced with high K+ depolarisation, noradrenaline in the presence of high K+, caffeine-induced contractions and noradrenaline contractions in the presence of felodipine were little affected by pinacidil. Pinacidil caused concentration-dependent hyperpolarisation of the resting smooth muscle. Pinacidil caused only a small and transient increase of the 86Rb efflux rate constant, while the same concentrations of pinacidil produced a significant increase in the 42K efflux rate constant. Our results seem to indicate that the relaxant effect of pinacidil is the result of an increase in K+ permeability, thus causing hyperpolarisation and relaxation. The opened K+ channels appear to be selective for K+ over Rb+.

journal_name

Drugs

journal_title

Drugs

authors

Videbaek LM,Aalkjaer C,Mulvany MJ

doi

10.2165/00003495-198800367-00006

subject

Has Abstract

pub_date

1988-01-01 00:00:00

pages

33-40

eissn

0012-6667

issn

1179-1950

journal_volume

36 Suppl 7

pub_type

杂志文章

相关文献

DRUGS文献大全
  • Detecting and Targeting NTRK Fusions in Cancer in the Era of Tumor Agnostic Oncology.

    abstract::Gene rearrangements involving the neurotrophic receptor kinase genes NTRK1, NTRK2, and NTRK3 (referred to as TRK, encoding TRKA, TRKB, and TRKC, respectively) result in highly oncogenic fusions. TRK fusions are rare, with a prevalence of < 1% in solid tumors. Detection of TRK fusions can be based on fluorescence in-si...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-020-01459-w

    authors: Rohrberg KS,Lassen U

    更新日期:2021-01-05 00:00:00

  • Fluoroquinolones and surgical prophylaxis.

    abstract::The objective of surgical prophylaxis is to prevent wound infections associated with surgery. The rates of wound infections vary according to the procedure: less than 3 infections per 100 for clean procedures; up to 4 per 100 for clean-contaminated procedures; and up to 9 per 100 for contaminated procedures. Surgical ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199300453-00018

    authors: Dellamonica P,Bernard E

    更新日期:1993-01-01 00:00:00

  • Updated national and international hypertension guidelines: a review of current recommendations.

    abstract::Despite the availability of effective pharmacological treatments to aid the control of blood pressure, the global rate of uncontrolled blood pressure remains high. As such, further measures are required to improve blood pressure control. Recently, several national and international guidelines for the management of hyp...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-014-0306-5

    authors: Kjeldsen S,Feldman RD,Lisheng L,Mourad JJ,Chiang CE,Zhang W,Wu Z,Li W,Williams B

    更新日期:2014-11-01 00:00:00

  • Rational use of disease-modifying antirheumatic drugs.

    abstract::The currently available, most frequently used disease-modifying antirheumatic drugs (DMARDs) include auranofin, azathioprine, D-penicillamine, gold sodium thiomalate, hydroxychloroquine, methotrexate (amethopterin) and sulphasalazine. Controlled trials of these agents are reviewed to compare their relative efficacy an...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199039010-00003

    authors: Furst DE

    更新日期:1990-01-01 00:00:00

  • Oral etoposide in lymphoma.

    abstract::Etoposide is one of the most active agents for the therapy of lymphomas. Oral etoposide has proven to be active in and clearly beneficial for patients with previously treated lymphomas. The optimal dose and schedule of oral etoposide for use in combination chemotherapy are still uncertain, but low daily doses (50 to 1...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199958003-00006

    authors: Greco FA

    更新日期:1999-01-01 00:00:00

  • Management of chronic obstructive pulmonary disease.

    abstract::Chronic obstructive pulmonary disease (COPD) is characterised by insidiously progressive airflow limitation. The necessarily multifactorial management programme should include smoking cessation, prevention of infections, bronchodilator and steroid therapy, supplemental oxygen, physical therapy, pulmonary rehabilitatio...

    journal_title:Drugs

    pub_type: 临床试验,杂志文章,评审

    doi:10.2165/00003495-198938010-00007

    authors: Kesten S,Rebuck AS

    更新日期:1989-07-01 00:00:00

  • Treatment of nausea and vomiting in terminally ill cancer patients.

    abstract::Nausea and vomiting is a common and distressing symptom complex in patients with far-advanced cancer, affecting up to 60% of individuals at some stage of their illness. The current approach to the palliative care of patients with nausea and vomiting is based on identifying the cause, understanding its pathophysiology ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/0003495-200868180-00004

    authors: Glare PA,Dunwoodie D,Clark K,Ward A,Yates P,Ryan S,Hardy JR

    更新日期:2008-01-01 00:00:00

  • Optimal therapeutic strategies for resectable oesophageal or oesophagogastric junction cancer.

    abstract::Oesophageal cancer is the eighth most common cancer diagnosed worldwide, with almost half a million new cases diagnosed each year. Despite improvements in surgical and radiotherapy techniques and refinements of chemotherapeutic regimens, long-term survival, even from localized oesophageal cancer, remains poor. Surgica...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/11585460-000000000-00000

    authors: Bystricky B,Okines AF,Cunningham D

    更新日期:2011-03-26 00:00:00

  • Peramivir: A Review in Uncomplicated Influenza.

    abstract::Intravenous peramivir (Alpivab™; Rapivab®; Rapiacta®; PeramiFlu®), the most recent globally approved inhibitor of influenza neuraminidase, is indicated for the treatment of uncomplicated influenza in adults and children from the age of 2 years. This article, written from an EU perspective, reviews the clinical use of ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-018-0981-8

    authors: Scott LJ

    更新日期:2018-09-01 00:00:00

  • Bisphosphonates. Pharmacology and use in the treatment of tumour-induced hypercalcaemic and metastatic bone disease.

    abstract::The geminal bisphosphonates are a new class of drugs characterised by a P-C-P bond. Consequently, they are analogues of pyrophosphate, but are resistant to chemical and enzymatic hydrolysis. The bisphosphonates bind strongly to hydroxyapatite crystals and inhibit their formation and dissolution. This physicochemical e...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199142060-00003

    authors: Fleisch H

    更新日期:1991-12-01 00:00:00

  • Coming to terms with nonsteroidal anti-inflammatory drug gastropathy.

    abstract::Despite well known complications, oral nonsteroidal anti-inflammatory drugs (NSAIDs) remain the most commonly prescribed medications in the US for musculoskeletal disorders such as osteoarthritis. Although there has been a recent focus on the cardiovascular and renal complications associated with these agents, NSAID g...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/11633740-000000000-00000

    authors: Roth SH

    更新日期:2012-05-07 00:00:00

  • Targeting Bruton's Tyrosine Kinase Across B-Cell Malignancies.

    abstract::Bruton's tyrosine kinase (BTK) is crucial in B-cell development and survival. The role of BTK as a downstream kinase in the B-cell receptor (BCR) signaling pathway is well described. As a key player in the pathogenesis of B-cell malignancies, targeting of dysregulated BCR signaling has been explored by development of ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-018-1003-6

    authors: da Cunha-Bang C,Niemann CU

    更新日期:2018-11-01 00:00:00

  • Why Biologics and Biosimilars Remain So Expensive: Despite Two Wins for Biosimilars, the Supreme Court's Recent Rulings do not Solve Fundamental Barriers to Competition.

    abstract::Biologics and biosimilars are medicines made from living cells that treat common and serious diseases such as cancer, diabetes, rheumatoid arthritis, and other inflammatory diseases. They are highly targeted, efficacious, and represent an increasingly important part of physicians' armamentaria in the combat against th...

    journal_title:Drugs

    pub_type: 杂志文章

    doi:10.1007/s40265-018-1009-0

    authors: Chen BK,Yang YT,Bennett CL

    更新日期:2018-11-01 00:00:00

  • Pharmacokinetics of cefoperazone: a review.

    abstract::The pharmacokinetics of cefoperazone in normal subjects, and in patients with hepatic and renal dysfunction are reviewed. After intravenous administration of 2 g of cefoperazone, levels in serum ranged from 202 to 375 microgram/ml depending on the period of drug administration. After intramuscular injection of 2 g of ...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-198100221-00010

    authors: Craig WA,Gerber AU

    更新日期:1981-01-01 00:00:00

  • The optimal management of hairy cell leukaemia.

    abstract::Hairy cell leukaemia is an uncommon B cell chronic lymphoproliferative disorder characterised by circulating lymphocytes displaying prominent cytoplasmic projections. Therapy is initiated for severe cytopenias or recurrent infections. Splenectomy, the first standard treatment, is now less commonly used as primary trea...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199549060-00006

    authors: Gollard R,Lee TC,Piro LD,Saven A

    更新日期:1995-06-01 00:00:00

  • Tranexamic acid: a review of its use in surgery and other indications.

    abstract:UNLABELLED:Tranexamic acid is a synthetic derivative of the amino acid lysine that exerts its antifibrinolytic effect through the reversible blockade of lysine binding sites on plasminogen molecules. Intravenously administered tranexamic acid (most commonly 10 mg/kg followed by infusion of 1 mg/kg/hour) caused reductio...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199957060-00017

    authors: Dunn CJ,Goa KL

    更新日期:1999-06-01 00:00:00

  • Community-associated meticillin-resistant Staphylococcus aureus infections: epidemiology, recognition and management.

    abstract::Meticillin-resistant Staphylococcus aureus (MRSA) is an important cause of infection, particularly in hospitalized patients and those with significant healthcare exposure. In recent years, epidemic community-associated MRSA (CA-MRSA) infections occurring in patients without healthcare risk factors have become more fre...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-200969060-00004

    authors: Patel M

    更新日期:2009-01-01 00:00:00

  • Capecitabine.

    abstract::Capecitabine is an orally administered fluoropyrimidine carbamate used for the treatment of paclitaxel- or anthracycline-refractory breast cancer. Capecitabine is metabolised via a 3-step process to the active agent fluorouracil. The final step of this process occurs preferentially in malignant tissue. In patients wit...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199958010-00006

    authors: Dooley M,Goa KL

    更新日期:1999-07-01 00:00:00

  • Severe asthma: prevention is better than cure.

    abstract::Asthmatic patients during sympton-free periods almost invariably have abnormalities in lung mechanics and gas exchange. Tentacious secretions and mucosal thickening exaggerate maldistribution of ventilation and cause flow limitation in small airways. Hence, the maximal expiratory flow volume loop in these patients wil...

    journal_title:Drugs

    pub_type: 杂志文章

    doi:10.2165/00003495-197816030-00007

    authors: Goldstein RS,Slutsky AS,Rebuck AS

    更新日期:1978-09-01 00:00:00

  • Is tiaprofenic acid different from other NSAIDs with regard to effects on renal function in the elderly?

    abstract::In a study of the effects of various NSAIDs on renal function in the elderly, indomethacin, tiaprofenic acid and sulindac were administered to patients ranging in age from 54 to 97 years for a period of 3 months. Indomethacin sustained release (25 mg tid) was administered to 66 patients, tiaprofenic acid (200 mg tid) ...

    journal_title:Drugs

    pub_type: 杂志文章

    doi:10.2165/00003495-198800351-00022

    authors: Ishioka T

    更新日期:1988-01-01 00:00:00

  • Drugs and receptors. An overview of the current state of knowledge.

    abstract::This paper reviews the theoretical concepts and methods utilised with isolated tissues to characterise drugs and drug receptors. Specifically the impact, on the in vitro measurement of agonist affinity and relative efficacy, of the idea that receptors bind to transduction proteins in the lipid bilayer of the cell memb...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199040050-00003

    authors: Kenakin T

    更新日期:1990-11-01 00:00:00

  • [Review of current pharmacologic treatment of pain].

    abstract::Pain is the main reason prompting patients to consult their physicians. In acute conditions, pain has a very particular significance as a warning sign, enabling the physician to attempt a diagnosis. Nevertheless, its detrimental effect upon the individual (even in the case of acute pain) and its cost to society are no...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199700532-00005

    authors: Brasseur L

    更新日期:1997-01-01 00:00:00

  • Antiviral therapy in human immunodeficiency virus infections. Current status (Part II).

    abstract::Part I of this article reviewed the targets against which anti-HIV drugs can be directed, problems in assessing active compounds (e.g. resistance development and use of surrogate end-points). and nucleoside analogues effective against HIV reverse transcriptase. Intensive research is currently being undertaken in labor...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199345050-00002

    authors: Sandström E,Oberg B

    更新日期:1993-05-01 00:00:00

  • Exenatide Extended-Release: An Updated Review of Its Use in Type 2 Diabetes Mellitus.

    abstract::Exenatide extended-release (exenatide ER) [Bydureon(®)] is a glucagon-like peptide-1 receptor agonist, approved for the treatment of type 2 diabetes mellitus. It is injected subcutaneously by patients once weekly, with no dose titration required. This article updates an earlier review of exenatide ER in the management...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-015-0420-z

    authors: Syed YY,McCormack PL

    更新日期:2015-07-01 00:00:00

  • Felodipine in hypertensive patients. A dose finding study in patients refractory to beta-blocker monotherapy.

    abstract::In a double-blind study, 128 patients with essential hypertension, refractory to beta-blocker monotherapy, were randomised to 1 of 4 treatment groups. Felodipine 2.5 mg twice daily, 5mg twice daily, 10mg twice daily or matched placebo twice daily were administered in addition to the beta-blocker for 4 weeks. Mean supi...

    journal_title:Drugs

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.2165/00003495-198700343-00023

    authors: Sluiter HE

    更新日期:1987-01-01 00:00:00

  • Management of onychomycoses.

    abstract::Onychomycoses, infections of the nail caused by fungi, are amongst the most common illnesses. Because of the high incidence of these infections and problems involved in their therapy, they have received much attention, particularly as concerns a better characterisation of the causative micro-organisms. Onychomycosis c...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199958020-00005

    authors: Niewerth M,Korting HC

    更新日期:1999-08-01 00:00:00

  • Diagnosis and Treatment of Non-24-h Sleep-Wake Disorder in the Blind.

    abstract::Non-24-h sleep-wake disorder (non-24) is a circadian rhythm disorder occurring in 55-70% of totally blind individuals (those lacking conscious light perception) in which the 24-h biological clock (central, hypothalamic, circadian pacemaker) is no longer synchronized, or entrained, to the 24-h day. Instead, the overt r...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.1007/s40265-017-0707-3

    authors: Emens JS,Eastman CI

    更新日期:2017-04-01 00:00:00

  • Colloid volume expanders. Problems, pitfalls and possibilities.

    abstract::Colloid solutions have been developed and used over the past 70 years as expanders of the intravascular space, based on an understanding of Starling's law. Increasing osmotic pressure with colloidal products has remained an attractive theoretical premise for volume resuscitation. Indeed, colloids have been shown to in...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199855050-00002

    authors: Roberts JS,Bratton SL

    更新日期:1998-05-01 00:00:00

  • Influence of carvedilol on blood glucose and glycohaemoglobin A1 in non-insulin-dependent diabetics.

    abstract::Pharmacological treatment of hypertension can, cause clinically significant alterations in endocrine function and glucose homeostasis. The aim of this study was to investigate the antihypertensive efficacy and the influence on carbohydrate metabolism of carvedilol and metoprolol in non-insulin-dependent diabetics with...

    journal_title:Drugs

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.2165/00003495-198800366-00023

    authors: Ehmer B,van der Does R,Rudorf J

    更新日期:1988-01-01 00:00:00

  • Antiviral therapy in human immunodeficiency virus infections. Current status (Part I).

    abstract::Antiviral therapy has in the past met with limited success and only a few antiviral drugs have been available. The human immunodeficiency virus (HIV) epidemic has created an urgent need for the development of antiviral therapy against this infection. HIV replication offers several targets for inhibitory compounds, the...

    journal_title:Drugs

    pub_type: 杂志文章,评审

    doi:10.2165/00003495-199345040-00002

    authors: Sandström E,Oberg B

    更新日期:1993-04-01 00:00:00