Blockade of voltage-gated calcium channel Cav1.2 and α1-adrenoceptors increases vertebral artery blood flow induced by the antivertigo agent difenidol.

@article{Murakami2012BlockadeOV,
  title={Blockade of voltage-gated calcium channel Cav1.2 and $\alpha$1-adrenoceptors increases vertebral artery blood flow induced by the antivertigo agent difenidol.},
  author={Kohji Murakami and Naoki Inoue and Chiaki Fuchikami and Koyuki Tajima and Asami Hashino and H Fukui and Kumiko Noda and Michiko Oka},
  journal={European journal of pharmacology},
  year={2012},
  volume={689 1-3},
  pages={
          165-71
        }
}
Difenidol (1,1-diphenyl-4-piperidino-1-butanol hydrochloride) is an effective drug for the treatment of vertigo and dizziness. This drug is known to improve the blood flow in vertebral arteries, though the precise mechanism underlying this action remains unclear. In the present study, we investigated the effect of difenidol on voltage-gated calcium channel Ca(v)1.2 and α(1)-adrenoceptor subtypes that regulate the intracellular calcium concentration ([Ca(2+)](i)), as well as their possible… 
Overview of Antagonists Used for Determining the Mechanisms of Action Employed by Potential Vasodilators with Their Suggested Signaling Pathways
TLDR
The aim of this paper is to suggest the most appropriate type of antagonists that correspond to receptors that would be involved during the mechanistic studies, as well as the latest signaling pathways trends that are being studied in order to determine the route(s) that atest compound employs for inducing vasodilation.
Electrochemiluminescence Sensor Based on Electrospun Three-Dimensional Carbon Nanofibers for the Detection of Difenidol Hydrochloride
TLDR
A novel electrochemiluminescence (ECL) sensor for the simple and effective detection of difenidol hydrochloride was fabricated by modifying a glassy carbon electrode with three-dimensional carbon nanofibers (3D-CNFs).
Fatal diphenidol poisoning: a case report and a retrospective study of 16 cases
TLDR
A case of a 23-year-old female who suffered from DPN poisoning that resulted in death and the circumstances indicated that the manner of death was suicide is reported.
Pd/Cu-cocatalyzed aerobic oxidative carbonylative homocoupling of arylboronic acids and CO: a highly selective approach to diaryl ketones.
A highly selective Pd/Cu-cocatalyzed aerobic oxidative carbonylative homocoupling of arylboronic acids has been developed. This method employs a simple catalytic system, readily available boronic

References

SHOWING 1-10 OF 42 REFERENCES
Cerebrovascular selectivity and vasospasmolytic action of the novel calcium antagonist (+/-)-(E)-1-(3-fluoro-6, 11-dihydrodibenz[b,e]oxepin-11-yl)-4-(3-phenyl-2-propenyl)-piperazine dimaleate in isolated cerebral arteries of the rabbit and dog.
TLDR
The results suggest that the PKC-dependent system which is mediated by influx of extracellular Ca2+ profoundly contributes to the contraction of the cerebral artery and that the cerebroselective-vasodilating effect of AJ-3941 may depend, at least partly, on the inhibition of thePKC-mediated contractile response.
Failure of AH11110A to functionally discriminate between α1-adrenoceptor subtypes A, B and D or between α1- and α2-adrenoceptors
TLDR
AH11110A enhanced the general contractility of rat vas deferens, produced a bell-shaped dose–response curve of vasodilation in perfused rat kidney, and its antagonism in most other tissues was not simply competitive.
Flunarizine blocks voltage-gated Na+ and Ca2+ currents in cultured rat cortical neurons: A possible locus of action in the prevention of migraine
TLDR
Investigation of the effects of FLN on Na(+) and Ca(2+) channels of cultured rat cortical neurons found that blockade of these currents might help explain the mechanism underlying the preventive effect of flunarizine on migraine attacks.
NS-49, a novel alpha 1a-adrenoceptor-selective agonist characterization using recombinant human alpha 1-adrenoceptors.
TLDR
Using the Chinese hamster ovary cells stably expressing the cloned human alpha 1-adrenoceptor subtypes, a newly synthesized phenethylamine class agonist (NS-49) is compared with imidazoline class agonists and NS-49 is more efficacious than oxymetazoline in their binding affinities and intrinsic activities in causing transient increases of cytosolic Ca2+ concentrations.
Ifenprodil and SL 82.0715 as cerebral anti-ischemic agents. II. Evidence for N-methyl-D-aspartate receptor antagonist properties.
TLDR
The results indicate that ifenprodil is a noncompetitive NMDA antagonist which has a mechanism of action distinct from either the reference competitive NMDA receptor antagonists (CPP and 2-amino-5-phosphonovalerate) or the noncompetitiveNMDA channel blockers (phencyclidine, TCP and MK 801).
BMY 7378 is a selective antagonist of the D subtype of α1-adrenoceptors
BMY 7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8- azaspiro[4.5]decane-7,9-dione dihydrochloride), a 5-HT1A receptor partial agonist, also binds to alpha 1-adrenoceptors. Competition assays
BMY 7378 is a selective antagonist of the D subtype of alpha 1-adrenoceptors.
BMY 7378 (8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8- azaspiro[4.5]decane-7,9-dione dihydrochloride), a 5-HT1A receptor partial agonist, also binds to alpha 1-adrenoceptors. Competition assays
Ionic mechanism for contractile response to hyposmotic challenge in canine basilar arteries.
TLDR
Results suggest that a hyposmotic challenge activates cation channels, which presumably cause Ca( 2+) influx, thereby activating Ca(2+)-activated Cl(-) channels, and the subsequent membrane depolarization is likely to increaseCa(2+) influx through VDCC and elicit contraction.
Vasodilating effects of the new calcium antagonist benidipine hydrochloride in anesthetized dogs and cats.
TLDR
Coronary vasodilating effect of KW-3049 was influenced neither by propranolol, atropine, diphenhydramine nor by aminophylline, and did not affect the vasodillator effect of adenosine.
A knockout approach indicates a minor vasoconstrictor role for vascular alpha1B-adrenoceptors in mouse.
TLDR
By combining antagonist pharmacology and genetics, this work provides a simplified analysis ofalpha(1)-mediated vasoconstriction, demonstrating that alpha(1D) and alpha(2A) are the major subtypes involved in vasoconStriction, with a minor but definite contribution from alpha( 1B) in every vessel.
...
1
2
3
4
5
...