Yohimbine produces antinociception in the formalin test in rats: involvement of serotonin 1A receptors

Shannon, Harlan E.; Lutz, Elizabeth A.

doi:10.1007/s002139900343

Cited by 29 publications

(15 citation statements)

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“…Yohimbine (2.5–7.5 mg/kg) disrupted prepulse inhibition [37] and produced antinociception [43] in rats via the action at 5-HT1A receptors but not at alpha2-adrenoceptors. Ability of alpha2-adrenoblockers to affect 5-HT1A receptors is not unique for yohimbine: BRL-44408 recognizes 5-HT1A receptors along with being alpha2-adrenoceptor antagonist [31].…”

Section: Discussionmentioning

confidence: 99%

Yohimbine is a 5-HT1A agonist in rats in doses exceeding 1mg/kg.

Zaretsky

Zaretskaia

DiMicco

et al. 2015

Neuroscience Letters

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Yohimbine is a prototypical alpha2-adrenergic receptor antagonist. Due to its relatively high selectivity, yohimbine is often used in experiments whose purpose is to examine the role of these receptors. For example, yohimbine has been employed at doses of 1–5 mg/kg to reinstate drug-seeking behavior after extinction or to antagonize general anesthesia, an effects presumably being a consequence of blocking alpha2-adrenergic receptors. In this report we characterized dose-dependent autonomic and behavioral effects of yohimbine and its interaction with an antagonist of 5-HT1A receptors, WAY 100635. In low doses (0.5 – 2 mg/kg i.p.) yohimbine induced locomotor activation which was accompanied by a tachycardia and mild hypertension. Increasing the dose to 3–4.5 mg/kg reversed the hypertension and locomotor activation and induced profound hypothermia. The hypothermia as well as the suppression of the locomotion and the hypertension could be reversed by the blockade of 5-HT1A receptors with WAY 100635. Our data confirm that yohimbine possesses 5-HT1A properties, and demonstrated that in doses above 1 mg/kg significantly activate these receptors.

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Section: Discussionmentioning

confidence: 99%

Yohimbine is a 5-HT1A agonist in rats in doses exceeding 1mg/kg.

Zaretsky

Zaretskaia

DiMicco

et al. 2015

Neuroscience Letters

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“…However, in an animal model 19) following nerve injury, there appears to be an increase in alpha-2 like AR sites at peripheral sensory neurons and cutaneous nociceptor in rabbit become sensitive to adrenergic agonist. And also chronic inflammation initiates circumstances in which alpha-2 AR-mediated sympathetic activity excites some nociceptor 20) . Some studies demonstrated that alpha-2 AR is more important in neuropathic pain 3,11,14,18,26,29,31) .…”

Section: Discussionmentioning

confidence: 99%

“…Yohimbine produces antinociception 4,15,20) . Shannon and Lutz 20) demonstrated that yohimbine produces dose-related antinociception in formalin test in rats which is mediated in part by agonistic action at 5-HT1A receptor.…”

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confidence: 99%

Involvement of Selective Alpha-2 Adrenoreceptor in Sympathetically Maintained Pain

Park

Yong

Lee

2010

J Korean Neurosurg Soc

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Objective : Peripheral nerve injury often leads to neuropathic pain, which is characterized by burning pain, allodynia, and hyperalgesia. The role of the sympathetic nervous system in neuropathic pain is a complex and controversial issue. It is generally accepted that the alpha adrenoreceptor (AR) in sympathetic nerve system plays a significant role in the maintenance of pain. Among alpha adrenoreceptor, alpha-1 receptors play a major role in the sympathetic mediated pain. The primary goal of this study is to test the hypothesis that sympathetically maintained pain involves peripheral alpha-2 receptors in human. Methods : The study was a randomized, prospective, double-blinded, crossover study involving twenty patients. The treatments were : Yohimbine (30 mg mixed in 500 mL normal saline), and Phentolamine (1 mg/kg in 500 mL normal saline) in 500 mL normal saline at 70 mL/hr initially then titrated. The patients underwent infusions on three different appointments, at least one month apart. Thus, all patients received all 2 treatments. Pain measurement was by visual analogue scale, neuropathic pain questionnaire, and McGill pain questionnaire. Results : There were significant decreases in the visual analogue scale, neuropathic score, McGill pain score of yohimnine, and phentolamine. Conclusion : We conclude that alpha-2 adrenoreceptor, along with alpha-2 adrenoreceptor, may be play role in sympathetically maintained pain in human. KEY WORDS :Reflex sympathetic dystrophy˙ Yohimbine˙ Alpha-2 antagonist.

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“…α 2 -adrenergic receptor antagonist block the (classically presynaptic) α 2 -receptors, resulting in facilitation of NE release from the presynaptic neuron or activation of the postsynaptic neuron, in the case of postsynaptic α 2 -receptors (80). Yohimbine is not only an α 2 -adrenergic antagonist but also a 5-HT 1A agonist (81-83). Animal studies have demonstrated that yohimbine has pro- ejaculatory effects (84-87).…”

Section: Yohimbinementioning

confidence: 99%

The drug treatment of delayed ejaculation

Abdel‐Hamid¹,

Elsaied²,

Mostafa³

2016

Transl. Androl. Urol.

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Delayed ejaculation (DE) is an uncommon and a challenging disorder to treat. It is often quite concerning to patients and it can affect psychosocial well-being. Here we reviewed how DE is treated pharmacologically .We also highlighted specific settings where drugs could be introduced to medical practice. Electronic databases were searched from 1966 to February 2016, including PubMed MEDLINE, EMBASE, EBCSO Academic Search Complete, Cochrane Systematic Reviews Database, and Google Scholar using key words; delayed ejaculation, retarded ejaculation, inhibited ejaculation, drugs, treatment, or pharmacology. To achieve the maximum sensitivity of the search strategy and to identify all studies, we combined “delayed ejaculation” as Medical Subject Headings (MeSH) terms or keywords with each of “testosterone” or “cabergoline” or “bupropion” or “amantadine” or “cyproheptadine” or “midodrine” or “imipramine” or “ephedrine” or “pseudoephedrine” or “yohimbine” or “buspirone” or “oxytocin” or “bethanechol” as MeSH terms or keywords. There are a number of drugs to treat patients with DE including: testosterone, cabergoline, bupropion, amantadine, cyproheptadine, midodrine, imipramine, ephedrine, pseudoephedrine, yohimbine, buspirone, oxytocin, and bethanechol. Although there are many pharmacological treatment options, the evidence is still limited to small trials, case series or case reports. Review of literature showed that evidence level 1 (Double blind randomized clinical trial) studies were performed with testosterone, oxytocin, buspirone or bethanechol treatment. It is concluded that successful drug treatment of DE is still in its infancy. The clinicians need to be aware of the pathogenesis of DE and the pharmacological basis underlying the use of different drugs to extend better care for these patients. Various drugs are available to address such problem, however their evidence of efficacy is still limited and their choice needs to be individualized to each specific case.

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Yohimbine produces antinociception in the formalin test in rats: involvement of serotonin 1A receptors

Abstract: The present results demonstrate that yohimbine produces a dose-related antinociception in the formalin test in rats which is mediated in part by the agonistic actions at 5-HT(1A) receptors.

Cited by 29 publications

References 0 publications

Yohimbine is a 5-HT1A agonist in rats in doses exceeding 1mg/kg.

Yohimbine is a 5-HT1A agonist in rats in doses exceeding 1mg/kg.

Involvement of Selective Alpha-2 Adrenoreceptor in Sympathetically Maintained Pain

The drug treatment of delayed ejaculation

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