In mice, yohimbine appears to accentuate the normal "alarm" reactions (alerting, flight) to external stimuli. Imipramine increases this effect and at the same time converts a non-lethal dose of yohimbine into a lethal one. The effect of imipramine is greatly reduced by adrenalectomy or by treatment with reserpine, syrosingopine, ganglion-blocking drugs or adrenaline antagonists acting on sympathetic beta-receptors. Hypnotic, anti-convulsant or anaesthetic agents, tetrabenazine or antagonists of 5-hydroxytryptamine do not reduce the imipramine effect. A variety of drugs which, like imipramine, are known to interfere with the tissue binding of noradrenaline also increase the toxicity of yohimbine. Yohimbine significantly reduces brain noradrenaline content; adrenal catechol amines are slightly reduced. The results suggest that yohimbine releases noradrenaline from stores or nerves as a consequence of increased central sympathetic activity. Imipramine increases the actions and toxicity of yohimbine by increasing the effects of the released noradrenaline on beta-receptors. The lethal effects of a high dose of yohimbine alone are not reduced by any of the treatments tested, and appear not to result from activation of sympathetic mechanisms.
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http://dx.doi.org/10.1111/j.1476-5381.1963.tb01501.x | DOI Listing |
Int J Mol Sci
November 2024
Department of Physiotherapy, Nicolas Copernicus University in Toruń, Collegium Medicum in Bydgoszcz, ul. Techników 3, 85-801 Bydgoszcz, Poland.
A natural compound derived from the Pausinystalia yohimbe tree-yohimbine, has a rich history of use in traditional medicine and is currently being explored for its potential therapeutic applications. This indole alkaloid primarily acts as an antagonist of α2-adrenergic receptors. Initially recognized for its purported aphrodisiac properties, yohimbine has been investigated for a wide range of applications, including sports or the treatment of erectile dysfunction and metabolic disorders.
View Article and Find Full Text PDFBiochem Pharmacol
December 2024
Department of Applied Biology, CSIR-Indian Institute of Chemical Technology (IICT), Hyderabad 500007, India; Academy of Science and Innovative Research (AcSIR), Ghaziabad, Uttar Pradesh 201 002, India. Electronic address:
Idiopathic pulmonary fibrosis (IPF) is a devastating interstitial lung disorder characterized by the accumulation of extracellular matrix and collagen, resulting in significant parenchymal scarring and respiratory failure that leads to mortality. Yohimbine (YBH) is an α-2 adrenergic receptor antagonist with anti-oxidant and anti-inflammatory properties. In the current study, we aimed to investigate the anti-inflammatory, anti-oxidant and anti-fibrotic activity of YBH against LPS/TGF-β-induced differentiation in BEAS-2B/LL29 cells and bleomycin (BLMN) induced pulmonary fibrosis model in rats.
View Article and Find Full Text PDFJ Med Chem
June 2024
Institute of Organic Chemistry and Biochemistry of the Czech Academy of Sciences, Flemingovo nám. 2, Prague 6 160 00, Czech Republic.
Yohimbine, a natural indole alkaloid and a nonselective adrenoceptor antagonist, possesses potential benefits in treating inflammatory disorders and sepsis. Nevertheless, its broader clinical use faces challenges due to its low receptor selectivity. A structure-activity relationship study of novel yohimbine analogues identified amino esters of yohimbic acid as potent and selective ADRA2A antagonists.
View Article and Find Full Text PDFPhotodiagnosis Photodyn Ther
June 2024
Department of Physics & Astronomy, Western Kentucky University, Bowling Green, KY 42101, USA. Electronic address:
Efflux pumps are active transporters, which allow the cell to remove toxic substances from within the cell including antibiotics and photosensitizer complexes. Efflux pump inhibitors (EPIs), chemicals that prevent the passage of molecules through efflux pumps, play a crucial role in antimicrobial effectiveness against pathogen. In this work, we studied the effect of EPI, namely, reserpine, on photodeactivation rate of pathogens when used with Ag NPs and methylene blue (MB).
View Article and Find Full Text PDFJ Appl Toxicol
August 2024
Health and Environmental Sciences Institute, Washington, DC, USA.
Botanicals contain complex mixtures of chemicals most of which lack pharmacokinetic data in humans. Since physicochemical and pharmacokinetic properties dictate the in vivo exposure of botanical constituents, these parameters greatly impact the pharmacological and toxicological effects of botanicals in consumer products. This study sought to use computational (i.
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