Gene expression of histamine H1 receptor in guinea pig primary sensory neurons: a relationship between H1 receptor mRNA-expressing neurons and peptidergic neurons

Kashiba, Hitoshi; Fukui, Hirokazu; Morikawa, Yoshihiro; Senba, Emiko

doi:10.1016/s0169-328x(98)00346-5

Cited by 88 publications

(47 citation statements)

References 38 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…21,22) First AHs have been suggested to have analgesic effects on both somatic and visceral pain. 17) In the present study, 1st AHs exhibited analgesic effects in the writhing test in both C3H/HeN and H1R-KO mice.…”

Section: Discussionmentioning

confidence: 99%

Analgesic Effects of 1st Generation Anti-histamines in Mice

Takahashi

Shima

Tsuchiya

et al. 2016

Biological & Pharmaceutical Bulletin

View full text Add to dashboard Cite

Pain is sensed, transmitted, and modified by a variety of mediators and receptors. Histamine is a wellknown mediator of pain. In addition to their anti-histaminic effects, the classical, or 1st generation, anti-histamines (1st AHs) possess, to various degrees, anti-muscarinic, anti-serotonergic, anti-adrenergic, and other pharmacologic effects. Although there have been attempts to use 1st AHs as analgesics and/or analgesic adjuvants, the advent of non-steroidal anti-inflammatory drugs (NSAIDs) discouraged such trials. We previously reported that in patients with temporomandibular disorders, osteoporosis, and/or osteoarthritis, the analgesic effects of certain 1st AHs (chlorpheniramine and diphenhydramine) are superior to those of the NSAIDs flurbiprofen and indomethacin. Here, we compared analgesic effects among 1st AHs and NSAIDs against responses shown by mice to intraperitoneally injected 0.7% acetic acid. Since 1st AHs are water soluble, we selected water-soluble NSAIDs. For direct comparison, drugs were intravenously injected 30 min before the above tests. Histamine-H1-receptor-deficient (H1R-KO) mice were used for evaluating H1-receptor-independent effects. The tested 1st AHs (especially cyproheptadine) displayed or tended to display analgesic effects comparable to those of NSAIDs in normal and H1R-KO mice. Our data suggest that the anti-serotonergic and/or anti-adrenergic effects of 1st AHs make important contributions to their analgesic effects. Moreover, combination of a 1st AH with an NSAID (cyclooxygenase-1 inhibitor) produced remarkably potent analgesic effects. We propose that a 1st AH, by itself or in combination with a cyclooxygenase-1 inhibitor, should undergo testing to evaluate its usefulness in analgesia.

show abstract

Section: Discussionmentioning

confidence: 99%

Analgesic Effects of 1st Generation Anti-histamines in Mice

Takahashi

Shima

Tsuchiya

et al. 2016

Biological & Pharmaceutical Bulletin

View full text Add to dashboard Cite

show abstract

“…Histamine seems to be a key mast cell mediator, having sensitizing effects on nociceptors 39 , and is capable of inducing severe burning pain when applied to the skin of patients suffering from postherpetic neuralgia 40 . In addition, neuronal histamine receptors are upregulated after a crush injury to the sciatic nerve 41 . These studies suggest that activated mast cells contribute directly to neuropathic pain by releasing algogenic mediators after degranulation.…”

Section: Fig 1: Summary Of Various Mechanism Involved In the Pathophmentioning

confidence: 99%

Untitled

2012

IJPSR

View full text Add to dashboard Cite

Neuropathic pain is considered as an inappropriate response caused by a lesion or dysfunction in the PNS or CNS). Neuropathic pain can manifest itself as either without a stimulus (stimulus-independent pain) and/ or as pain hypersensitivity elicited after a stimulus (stimulus-evoked pain). Stimulusindependent pain includes symptoms described by the patient such as (a) continuous, burning pain (b) intermittent shooting, lancinating pain (c) some dysaesthesias. Conversely, stimulus-evoked pain describes signs the physician induces after mechanical, thermal or chemical stimulation, and usually involves hyperalgesia or allodynia. The mechanism(s) underlying neuropathic pain are not completely understood but are considered to be complex, multifactorial and to evolve over time. Neuropathic pain can be trauma (surgical and non-surgical), accidents, and exposure to toxins, infection, viruses, metabolic diseases, nutritional deficiency, ischemia, and stroke. Current research studies indicate that both peripheral and central mechanisms have been involved in pathogenesis of neuropathic pain.

show abstract

“…In parallel, nerve injury triggers an up-regulation of mRNAs (3-to 4-fold) for the histamine H1 receptor in small peptidergic dorsal root ganglion neurons (Kashiba et al, 1999). Under normal conditions, neurons that express mRNA for H1 receptors are unmyelinated, small-diameter neurons that are both nonpeptidergic and capsaicin-insensitive.…”

Section: Novel Histamine Antagonist In Treatment Of Persistent Pain 1235mentioning

confidence: 99%

“…Histamine H1 receptors are localized in the superficial dorsal horn (Ninkovic et al, 1982;Seybold, 1985) where they seem to be predominantly localized on the terminals of smalldiameter primary afferents (Ninkovic and Hunt, 1985;Kashiba et al, 1999). Histamine can hence act as a neurotransmitter and several studies suggest a role of the histaminergic system in nociception (Raffa, 2001).…”

mentioning

confidence: 99%

ReN-1869 [(R)-1-(3-(10,11-Dihydro-5 H-dibenzo[a,d]cyclohepten-5-ylidene)-1-propyl)-3-piperidine Carboxylic Acid], a Novel Histamine H1 Receptor Antagonist, Produces Potent and Selective Antinociceptive Effects on Dorsal Horn Neurons after Inflammation and Neuropathy

Suzuki

Edwards²,

Dickenson³

2004

The Journal of Pharmacology and Experimental Therapeutics

View full text Add to dashboard Cite

We characterized the effect of a novel selective histamine H1 receptor antagonist, (R)-1-(3-(10,11-dihydro-5H-dibenzo [a,d] cyclohepten-5-ylidene)-1-propyl)-3-piperidine carboxylic acid (ReN-1869), on the responses of dorsal horn neurons in anesthetized rats after carrageenan induced-inflammation and peripheral neuropathy (L5/6 spinal nerve ligation; SNL). ReN-1869 was administered systemically (0.1-4 mg/kg), and drug effects were assessed using a wide range of peripheral electrical and natural stimuli (brush, von Frey filaments, and heat). Comparisons were made between unoperated naive groups and either carrageenan inflamed or SNL rats. ReN-1869 produced little effect on the electrically evoked responses (wind-up, A␤-, A␦-, and C-fiber-evoked responses); however, it significantly attenuated neuronal responses to noxious heat in carrageenan and SNL rats. A robust effect was seen with the low-threshold mechanical punctate (von Frey 9 g) stimuli, which were selectively inhibited by ReN-1869 after tissue and nerve injury. These inhibitory actions were in marked contrast to the naive animal group, where only nonsignificant effects were observed. To investigate whether the actions of ReN-1869 are mediated via the antagonism of histamine H1 receptors, the effects of this novel compound were compared with that of another H1 receptor antagonist, mepyramine (1-20 mg/kg). Systemic mepyramine produced strong inhibitions of the 9-g von Freyevoked responses in carrageenan and SNL rats. The similar pharmacological profile of these two compounds suggests for a similar mechanism of action. We propose that ReN-1869 may represent a novel agent for the treatment of certain modalities of persistent pain states, in particular for the treatment of mechanical allodynia.

show abstract

Gene expression of histamine H1 receptor in guinea pig primary sensory neurons: a relationship between H1 receptor mRNA-expressing neurons and peptidergic neurons

Cited by 88 publications

References 38 publications

Analgesic Effects of 1st Generation Anti-histamines in Mice

Analgesic Effects of 1st Generation Anti-histamines in Mice

Untitled

ReN-1869 [(R)-1-(3-(10,11-Dihydro-5 H-dibenzo[a,d]cyclohepten-5-ylidene)-1-propyl)-3-piperidine Carboxylic Acid], a Novel Histamine H1 Receptor Antagonist, Produces Potent and Selective Antinociceptive Effects on Dorsal Horn Neurons after Inflammation and Neuropathy

Contact Info

Product

Resources

About