Regional differences in vascular responsiveness of nasal mucosae isolated from naive guinea pigs

Chiba, Yoshihiko; Matsuo, Kikuo; Sakai, Hiroyasu; Abe, Kazuho; Misawa, Miwa

doi:10.1016/j.anl.2006.09.014

Cited by 7 publications

(5 citation statements)

References 10 publications

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“…The EC 50 values (potencies) were in the low micromolar range. The low potency of the catecholamines at a-adrenoceptors agrees with their contractile potency in the human nasal mucosa [8,26]. The EC 50 values at HEK293 cells, however, are higher than those reported in the literature for, e.g.…”

Section: Figuresupporting

confidence: 79%

Alpha‐adrenoceptor agonistic activity of oxymetazoline and xylometazoline

Haenisch

Walstab

Herberhold

et al. 2010

Fundamemntal Clinical Pharma

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Oxymetazoline and xylometazoline are both used as nasal mucosa decongesting α-adrenoceptor agonists during a common cold. However, it is largely unknown which of the six α-adrenoceptor subtypes are actually present in human nasal mucosa, which are activated by the two alpha-adrenoceptor agonists and to what extent. Therefore, mRNA expression in human nasal mucosa of the six α-adrenoceptor subtypes was studied. Furthermore, the affinity and potency of the imidazolines oxymetazoline and xylometazoline at these α-adrenoceptor subtypes were examined in transfected HEK293 cells. The rank order of mRNA levels of α-adrenoceptor subtypes in human nasal mucosa was: α(2A) > α(1A) ≥ α(2B) > α(1D) ≥ α(2C) >> α(1B) . Oxymetazoline and xylometazoline exhibited in radioligand competition studies higher affinities than the catecholamines adrenaline and noradrenaline at most α-adrenoceptor subtypes. Compared to xylometazoline, oxymetazoline exhibited a significantly higher affinity at α(1A) - but a lower affinity at α(2B) -adrenoceptors. In functional studies in which adrenoceptor-mediated Ca(2+) signals were measured, both, oxymetazoline and xylometazoline behaved at α(2B) -adrenoceptors as full agonists but oxymetazoline was significantly more potent than xylometazoline. Furthermore, oxymetazoline was also a partial agonist at α(1A) -adrenoceptors; however, its potency was relatively low and it was much lower than its affinity. The higher potency at α(2B) -adrenoceptors, i.e. at receptors highly expressed at the mRNA level in human nasal mucosa, could eventually explain why in nasal decongestants oxymetazoline can be used in lower concentrations than xylometazoline.

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Section: Figuresupporting

confidence: 79%

Alpha‐adrenoceptor agonistic activity of oxymetazoline and xylometazoline

Haenisch

Walstab

Herberhold

et al. 2010

Fundamemntal Clinical Pharma

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“…The nasal mucosa contains a highly dense vasculature [30]. The dilation of the nasal vascular system is considered to mediate the reduction of isometric tension in the nasal mucosa, resulting in the induction of nasal congestion [22,31]. As shown in figure 2, BW245c induced relaxation of the nasal mucosa.…”

Section: Discussionmentioning

confidence: 99%

“…LTs and TX are produced after an allergen challenge in the nose [35]. Chiba et al [22] reported regional differences in vasculature responsiveness to contractile and expanding agents in nasal mucosa. LTs and TX have been reported to induce vasoconstriction of arterioles and venules [36], and to increase the vascular permeability of the nasal mucosa [37].…”

Section: Discussionmentioning

confidence: 99%

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The Potential Role of Prostaglandin D<sub>2</sub> in Nasal Congestion Observed in a Guinea Pig Model of Allergic Rhinitis

Takahashi

Tanaka

Higuchi

et al. 2012

Int Arch Allergy Immunol

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Background: Allergic rhinitis is the most common allergic disease, displaying the typical nasal symptom of congestion. Prostaglandin D₂ (PGD₂), a chemical mediator released in large amounts by mast cells upon allergic stimulation in humans, is known to be involved in nasal congestion. However, the mechanism by which this congestion occurs remains unclear. Methods: The effect of PGD₂ on the nasal airflow in guinea pigs was measured using a noninvasive approach that avoided any anesthetic effect. Isometric tension of isolated nasal mucosa and the nasal vascular corrosion resin cast technique were used to clarify the area of nasal mucosal vessels affected by PGD₂, and to examine the mechanism of PGD₂-induced nasal congestion. Moreover, the involvement of second messengers in PGD₂-induced mucosal relaxation was investigated. Results: PGD₂ induced an increase in intranasal pressure in a guinea pig model of rhinitis. Additionally, sinusoidal microvessel dilatation appeared around the septum using the vascular corrosion resin cast technique in the nasal mucosa. Moreover, relaxation of the nasal mucosa following stimulation of the prostanoid DP-1 receptor was associated with cAMP levels in the tissue. Conclusions: PGD₂-induced nasal congestion is caused by direct dilatation of the sinusoid vessels through the increase of cAMP levels in the nasal mucosa, demonstrating that the mechanism of PGD₂-induced nasal congestion is different from other chemical mediators. Consequently, antagonists for the prostanoid DP-1 receptor would be an alternative approach for the relief of nasal congestion. Alternatively, the combined administration with antagonists for other mediators involved in nasal congestion may also be a valuable therapy for allergic rhinitis.

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“…При этом низкая сила связывания с рецепторами у эпинефрина, нафазолина, тетризолина и фенилэфрина коррелирует с их клиническими возможностями: кратковременностью и/или недостаточностью эффекта вазоконстрикции (табл. 2) [7,8].…”

Section: единая классификация ринита отсутствует но наиболее распросunclassified

Modern Combination Drugs in the Treatment of Patients With Various Types of Rhinitis

Эдже¹,

Ovchinnikov²

2016

Med. sov.

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В работе обобщены данные о месте деконгестантов в современных алгоритмах терапии ринита различного генеза, показаны их преимущества и недостатки, а также целесообразность комбинации с препаратами других фармакологических групп, в частности с антихолинергическим средством ипратропия бромид. Обоснованы показания к применению ксилометазолина в сочетании с ипратропия бромидом. Представлены данные литературы, в которых доказано, что при клиническом использовании комбинированной схемы при равной эффективности устранения заложенности носа достоверно уменьшается ринорея.

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Regional differences in vascular responsiveness of nasal mucosae isolated from naive guinea pigs

Cited by 7 publications

References 10 publications

Alpha‐adrenoceptor agonistic activity of oxymetazoline and xylometazoline

Alpha‐adrenoceptor agonistic activity of oxymetazoline and xylometazoline

The Potential Role of Prostaglandin D<sub>2</sub> in Nasal Congestion Observed in a Guinea Pig Model of Allergic Rhinitis

Modern Combination Drugs in the Treatment of Patients With Various Types of Rhinitis

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