Yohimbine Hydrochloride

1 Pausinystalia sp. 2 Rauvolfia sp. 3 Uncaria sp.

Yohimbine hydrochloride is an alpha 2-adrenoreceptor antagonist, blocking the pre- and postsynaptic alpha-2 adrenoreceptors and causing an increased release of noradrenaline and dopamine. IC50 value: Target: In vitro: In vivo: Yohimbine hydrochloride (0.2 mg/kg, i.p.) was administered to rats 1h before the stress session daily for 14 consecutive days and its effect was assessed. Results of this section revealed that, immersion of rats in cold water significantly decreased sexual arousal and motivation as indicated by increased latencies and intervals. Decreased copulatory activity was confirmed by decreased testosterone, luteinizing hormone (LH) and follicle-stimulating-hormone (FSH) levels as well as decreased cholesterol content in rat testes. Treatment with yohimbine significantly increased the sexual arousal and potency and corrected the effects induced by stress on the mating behavior of male rats [1].

References:
[1]. Saad MA, et al. Potential effects of yohimbine and sildenafil on erectile dysfunction in rats. [2]. Docherty JR. Yohimbine antagonises α1A- and α1D-adrenoceptor mediated components in addition to the α2A-adrenoceptor component to pressor responses in the pithed rat. Eur J Pharmacol. 2012 Mar 15;679(1-3):90-4. [3]. Lahiri P, et al. Platelet responsiveness to yohimbine hydrochloride and MRS2179 in the context of the interaction between collagen and epinephrine in acute coronary syndrome. Blood Cells Mol Dis. 2009 Jul-Aug;43(1):105-10.

Effect of yohimbine hydrochloride on serum prolactin concentration in the rat: possible antagonist for fescue toxicosis.[Pubmed:3963600]

Am J Vet Res. 1986 Apr;47(4):949-52.

Yohimbine Hydrochloride is an indole alkaloid which blocks alpha 2-adrenergic and dopamine receptors and stimulates serotonergic receptors. Yohimbine was selected for testing as a possible antagonist in fescue toxicosis. Reduced body weight gains in cattle with chronic fescue toxicosis may be due to ergot alkaloids produced by fungi which infect the fescue grass. Ergot alkaloids stimulate dopamine receptors, antagonize serotonin, and lower serum prolactin concentrations. It was hypothesized that yohimbine may reverse or counteract the effects of the toxic fescue. Investigation was made of the treatment effects of multiple doses of yohimbine given in rats by intraperitoneal and oral routes. Given intraperitoneally once a day for 8 days, Yohimbine Hydrochloride increased serum prolactin concentrations. When given orally in feed for 7 days, the drug decreased the serum prolactin concentration. The effects of yohimbine on prolactin concentrations were dependent on the dosages and routes of administration. The inability of yohimbine, when given orally, to increase serum prolactin levels decreased its potential usefulness for prolonged treatment of fescue toxicosis.

Molecular structure, vibrational spectra and HOMO, LUMO analysis of yohimbine hydrochloride by density functional theory and ab initio Hartree-Fock calculations.[Pubmed:21856216]

Spectrochim Acta A Mol Biomol Spectrosc. 2011 Nov;82(1):270-8.

Yohimbine Hydrochloride (YHCl) is an aphrodisiac and promoted for erectile dysfunction, weight loss and depression. The optimized geometry, total energy, potential energy surface and vibrational wavenumbers of Yohimbine Hydrochloride have been determined using ab initio, Hartree-Fock (HF) and density functional theory (DFT/B3LYP) method with 6-311++G(d,p) basis set. A complete vibrational assignment is provided for the observed Raman and IR spectra of YHCl. The UV absorption spectrum was examined in ethanol solvent and compared with the calculated one in gas phase as well as in solvent environment (polarizable continuum model, PCM) using TD-DFT/6-31G basis set. These methods are proposed as a tool to be applied in the structural characterization of YHCl. The calculated highest occupied molecular orbital (HOMO) and lowest unoccupied molecular orbital (LUMO) with frontier orbital gap are presented.

Does yohimbine hydrochloride facilitate fear extinction in virtual reality treatment of fear of flying? A randomized placebo-controlled trial.[Pubmed:22116378]

Psychother Psychosom. 2012;81(1):29-37.

BACKGROUND: Research suggests that Yohimbine Hydrochloride (YOH), a noradrenaline agonist, can facilitate fear extinction. It is thought that the mechanism of enhanced emotional memory is stimulated through elevated noradrenaline levels. This randomized placebo-controlled trial examined the potential exposure-enhancing effects of YOH in a clinical sample of participants meeting DSM-IV criteria for a specific phobia (fear of flying). METHODS: Sixty-seven participants with fear of flying were randomized to 4 sessions of virtual reality exposure therapy (VRET) combined with YOH (10 mg), or 4 sessions of VRET combined with a placebo. Treatment consisted of 4 weekly 1-hour exposure sessions consisting of two 25-minute virtual flights. At pre- and post- treatment, fear of flying was assessed. The YOH or placebo capsules were administered 1 h prior to exposures. The manipulation of the noradrenaline activity was confirmed by salivary alpha-amylase (sAA) samples taken pre-, during and post-exposure. RESULTS: Forty-eight participants completed treatment. Manipulation of noradrenaline levels with YOH was successful, with significantly higher levels of sAA in the YOH group when entering exposure. Results showed that both groups improved significantly from pre- to post-treatment with respect to anxiety reduction. However, although the manipulation of noradrenaline activity was successful, there was no evidence that YOH enhanced outcome. CONCLUSIONS: Participants improved significantly on anxiety measures independently of drug condition, after 4 sessions of VRET. These data do not support the initial findings of exposure-enhancing effects of YOH in this dosage in clinical populations.

Effect of caffeine sodium benzoate, ketamine hydrochloride, and yohimbine hydrochloride on xylazine hydrochloride-induced anorexia in white-tailed deer.[Pubmed:3735587]

J Wildl Dis. 1986 Jul;22(3):403-6.

Fifteen male white-tailed deer (Odocoileus virginianus) were administered xylazine hydrochloride (1 mg/kg BW i.m.), xylazine hydrochloride (1 mg/kg i.m.) followed by caffeine sodium benzoate (10 mg/kg i.m.), xylazine hydrochloride (0.5 mg/kg i.m.) and ketamine hydrochloride (4.5 mg/kg i.m.), and xylazine hydrochloride (1 mg/kg i.m.) followed by Yohimbine Hydrochloride (0.125 mg/kg i.m.), in a Latin Square design. Mean dry matter intake (DMI) for 4 days pre-treatment was compared to each of 4 days post-treatment. A significant (P less than 0.01) decrease in DMI was found only on the first day following treatment for each of the four drug combinations. The percent decreases in DMI on the first 24-hr period after immobilization were: xylazine hydrochloride 47%, xylazine hydrochloride/caffeine sodium benzoate 36%, xylazine hydrochloride/Yohimbine Hydrochloride 36%, and xylazine hydrochloride/ketamine hydrochloride 31%. The xylazine hydrochloride/ketamine hydrochloride combination was found to be insufficient to adequately sedate the deer. The use of caffeine or Yohimbine Hydrochloride is recommended to reduce recumbency time, but offers no improvement in xylazine hydrochloride-induced anorexia.

Yohimbine dimers exhibiting selectivity for the human alpha 2C-adrenoceptor subtype.[Pubmed:12438517]

J Pharmacol Exp Ther. 2002 Dec;303(3):979-84.

Yohimbine is a potent and selective alpha2- versus alpha1-adrenoceptor antagonist. To date, drugs with high specificity for the alpha2-adrenoceptor show marginal selectivity among the three alpha2-adrenoceptor subtypes. Initial studies showed that yohimbine was about 4- and 15-fold more selective for the human alpha2C-adrenoceptor in comparison with the alpha2A- and alpha2B-adrenoceptors, respectively. To improve on this alpha2-adrenoceptor subtype selectivity, a series of yohimbine dimers (varying from n = 2 to 24 spacer atoms) were prepared and evaluated for receptor binding on human alpha2-adrenoceptor subtypes expressed in Chinese hamster ovary cells. Each dimeric analog showed higher affinities for alpha2A- and alpha2C-adrenoceptor versus the alpha2B-adrenoceptor; and yohimbine dimers with spacers of n = 2, 3, 4, 18, and 24 exhibited selectivity for the alpha2C-adrenoceptor. The yohimbine dimers n = 3 and n = 24 showed the highest potency and selectivity (32- and 82-fold. respectively) for the alpha2C-adrenoceptor in receptor binding and in functional studies (42- and 29-fold, respectively) measuring cAMP changes using a cell-based luciferase reporter gene assay. The dimers (n = 3 and n = 24) had high selectivity (>1000-fold) for the alpha2C-adrenoceptor compared with the three alpha1-adrenoceptor subtypes. These findings demonstrate that the addition of spacer linkages to bivalent yohimbine molecules provides a successful approach to the development of ligands that are potent and highly selective for the alpha2C-adrenoceptor.

A re-evaluation of the role of alpha 2-adrenoceptors in the anxiogenic effects of yohimbine, using the selective antagonist delequamine in the rat.[Pubmed:8640349]

Br J Pharmacol. 1995 Oct;116(3):2081-9.

1. The acute behavioural effects of the alpha2-adrenoceptor antagonists, yohimbine, idazoxan and delequamine (RS-15385-197) were compared in two tests of exploratory behaviour in the rat, operated in tandem. These were the elevated X-maze test (5 min) and a modified holeboard test (12 min), which comprised a holeboard arena with a small roof in one corner as a 'refuge'. Rats were first placed into this corner, thus enabling measurements of initial emergence latency and the number of forays. The experiments were always done with a concomitant vehicle control group, with 10-12 rats per group, and with the treatment blinded. 2. In order to validate the tests, the effects of representatives of four classes of psychoactive agents were examined, viz. picrotoxin (anxiogenic), chlordiazepoxide (anxiolytic), (+)-amphetamine (stimulant) and diphenhydramine (sedative). The modified holeboard tended to be more sensitive than the measurement of total arm entries in the elevated X-maze at detecting drug effects on exploratory behaviour, but unlike the X-maze it could not clearly identify each class of agent. Thus, picrotoxin (5 mg kg(-1), i.p.) reduced total arm entries and open arm exploration in the X-maze (P<0.02) and suppressed most measures of activity in the holeboard (P<0.05); chlordiazepoxide (7.5 mg kg(-1), i.p.) increased total arm entries and open arm exploration (P<0.02) in the X-maze, without clear-cut effects in the holeboard; (+)-amphetamine (1 mg kg(-1), i.p.) had no significant effects in the X-maze, but increased most holeboard activities (P<0.05), and diphenhydramine (30 mg kg(-1), i.p.) reduced total arm entries in the X-maze (P<0.002) and hole exploration in the holeboard (P<0.05).

Comparison of the alpha-adrenoceptor antagonist profiles of idazoxan (RX 781094), yohimbine, rauwolscine and corynanthine.[Pubmed:6144048]

Naunyn Schmiedebergs Arch Pharmacol. 1984 Feb;325(2):136-44.

In the present studies the potency and selectivity of idazoxan (RX 781094) were compared with yohimbine and its diastereoisomers rauwolscine and corynanthine in both functional studies and radioligand binding experiments. Prejunctional alpha 2- and postjunctional alpha 1-adrenoceptor antagonist potencies were assessed by determining pA2 values against clonidine on the stimulated rat was deferens and noradrenaline on the anococcygeus muscle, respectively. The rank order of prejunctional alpha 2-adrenoceptor antagonist potency was idazoxan greater than yohimbine greater than rauwolscine much greater than corynanthine. At postjunctional alpha 1-adrenoceptors the rank order of antagonist potency was rauwolscine greater than corynanthine greater than yohimbine greater than idazoxan. The selectivity values (alpha 2/alpha 1) for idazoxan, yohimbine, rauwolscine and corynanthine were 245, 45, 3 and 0.03 respectively. The selectivity and potency profiles established for these antagonists in functional studies were confirmed in radioligand binding studies utilising 3H-idazoxan (alpha 2) and 3H-prazosin (alpha 1) in rat cerebral cortex. In pithed rats intravenously administered idazoxan, yohimbine and rauwolscine fully reversed the inhibitory effects of clonidine on electrically-induced contractions of the vas deferens; idazoxan was approximately ten times more potent than both yohimbine and rauwolscine. Corynanthine was inactive. Idazoxan and yohimbine also fully antagonised the inhibitory effects of guanabenz on electrically-induced contractions of the anococcygeus muscle; idazoxan again was more than ten times more potent than yohimbine in this model. The inhibitory effects of guanabenz were less readily antagonised by rauwolscine indicating that the selectivity of this compound is less than that of yohimbine in this tissue. Corynanthine was again inactive.(ABSTRACT TRUNCATED AT 250 WORDS)

Yohimbine Hydrochloride is an alpha 2-adrenoreceptor antagonist, blocking the pre- and postsynaptic alpha-2 adrenoreceptors and causing an increased release of noradrenaline and dopamine.

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