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A novel proaporphine-tryptamine dimer alkaloid, named phoebegrandine C 1, was isolated from the leaves of Phoebe grandis (Nees) Merr. Its structural elucidation was carried out using spectroscopic techniques, notably 2D NMR.
It is generally accepted that platelets from the main constituent of a thrombus. Experimental work has shown that 5-hydroxy-tryptamine (5 HT) in a concentration of 0.06 mg/ml produces clumping of the platelets. In view of this it was decided to estimate platelet 5 HT in thrombotic and non-thrombotic diseases. Thirty-five patients were investigated. Estimations of 5 HT were made on washed platelets rather than platelet-rich plasma which has been used in previous studies. Three groups were recognized on the basis of platelet 5 HT values. The first group consisted of five subjects who were clinically asymptomatic at the time of investigation but died 24 to 48 hours later and were shown at autopsy to have deep-vein thrombosis and pulmonary embolism; they had the highest level of platelet 5 HT. The second group comprised eight patients with cerebral thrombosis whose platelet 5 HT ranged between 1529 and 2183 ng/10-9. There were 22 subjects in the third group (11 apparently normal and 11 with different pathologies). Their platelet 5 HT ranged from 611 to 877 ng/10-9 and did not vary in the different pathological conditions studied. Since the highest level of platelet 5 HT was observed in patients prior to the formation or embolization of a thrombus, it is suggested that this may have some role in initiating thrombus formation.
Foxy is slang for 5-methoxy-N,N-diisopropyltryptamine. It has hallucinogenic properties, similar to other tryptamine compounds, and is mildly euphoric. This case report describes a 21-year-old Caucasian man who ingested a pill called Foxy containing an unknown amount of drug. He was observed in hospital for 2 h, during which time he had mild hallucinations and could not move his limbs. A urine sample was collected approximately 4 h after drug ingestion. The patient was then discharged with no follow up assessment. The 5-methoxy-N,N-diisopropyltryptamine was identified in the urine by gas chromatography-mass spectrometry. Standards prepared from the pure material were used in the identification. Quantitative analysis using the same analytical technique resulted in a urinary concentration of 1.7 micro g/mL. Through oxidative deamination, the metabolite, 5-methoxy-indole acetic acid, was formed. It was identified in the urine, and the concentration was determined to be 1.3 micro g/mL using gas chromatography-mass spectrometry. Two other compounds were discovered in the urine sample as a result of a routine drug screen. From their mass spectra, they were tentatively identified as 5-methoxy-N-isopropyltryptamine and 5-methoxy-N,N-diisopropyltryptamine-N'-oxide.
The previously unknown crystal structure of the biogenic compound tryptamine, in the form of a free base (C(10)H(12)N(2)), has been solved from X-ray powder diffraction data using simulated annealing followed by restrained Rietveld refinement [space group P2(1)2(1)2(1), a = 12.28593 (6), b = 8.53351 (4), c = 8.49385 (4) A, Z = 4, final reduced-chi(2) = 5.255]. A restrained Rietveld refinement was carried out in which the global weight factor, f, of the stereochemical restraints was gradually lowered. The effect of the relaxation of restraints on the crystal structure and on chi(2) was studied and a criterion for the final choice of f is reported. The crystal structure reported here shows efficient packing involving weak intermolecular hydrogen bonding and a herringbone-type packing pattern.
A single dose of perphenazine (5.0 mg/kg) was administered intraperitoneally to male Wistar rats. The time-related alterations in serum levels of perphenazine, striatal 3H-spiperone binding ex vivo and the regional brain metabolism of dopamine and 5-hydroxy-tryptamine were studied. Low serum levels of perphenazine were observed together with increased Kd of 3H-spiperone. No significant changes in Bmax were observed. Since Kd of 3H-spiperone binding peaked several hours after the maximal serum levels of perphenazine, perphenazine in serum appeared not to directly reflect the events at the receptor level. The concentrations of 3,4-dihydroxyphenylacetic acid (DOPAC) and 3-methoxy, 4-hydroxyphenylacetic acid (HVA) in the striatum were increased after perphenazine. They were maximal 1-3 h after the drug administration and showed positive correlations (correlation coefficient 0.93 and 0.80, respectively) with the serum levels of perphenazine. Increased levels of HVA were also observed both in the olfactory tubercle and in the frontal cortex. However, in the olfactory tubercle, administration of perphenazine did not significantly increase the DOPAC concentrations. In the olfactory tubercle 5-hydroxyindoleacetic acid (5-HIAA) was decreased 1-24 h after administration of perphenazine. In the striatum and in the frontal cortex only slight changes in 5-HIAA were seen. Thus, in the olfactory tubercle 5-hydroxytryptaminergic mechanisms could modulate the dopaminergic neurotransmission.
There are two kinds of tryptamine receptor in the guinea-pig ileum, namely the M receptors which can be blocked with morphine and the D receptors which can be blocked with dibenzyline. Atropine, an atropine-like drug, cocaine, and methadone inhibit effects due to the M receptors, even after dibenzyline, but have no additional effect after morphine. Lysergic acid diethylamide, dihydroergotamine and 5-benzyloxygramine inhibit effects due to the D receptors, even after morphine, but have no additional effect after dibenzyline. The M receptors are probably in the nervous tissue and the D receptors are probably in the muscles.
On the guinea-pig ileum, 5-hydroxytryptamine appeared to act in the same way as tryptamine on two types of receptor (morphine-sensitive and phenoxybenzamine(Dibenzyline)-sensitive). The actions of analogues of 5-hydroxytryptamine on the phenoxybenzamine-sensitive receptors resembled their actions on the rat uterus, and the actions on the morphine-sensitive receptors slightly resembled those on the rat fundus strip. The guinea-pig ileum preparation, however, did not appear to be more suitable than the rat uterus and rat fundus strip for testing the ability of compounds to imitate or antagonize 5-hydroxytryptamine.
1 Reactivity of goat isolated pulmonary arteries and veins to a variety of vasoactive agents was investigated. 2 Bradykinin (Bk), acetylcholine (ACh), noradrenaline (NA), prostaglandin A1 (PGA1), PGE2, PGF2 alpha and histamine induced dose-dependent contractile responses on veins; 5-hydroxytryptamine (5-HT) induced veno-relaxation. Angiotensin was virtually inactive. 3 Angiotensin, NA, Bk, histamine and 5-HT produced concentration-dependent contractile responses on the arterial strips; these arteries failed to respond to ACh, PGA1, PGE2 or PGF2 alpha. 4 The pulmonary veno-relaxant response to 5-HT was found to be resistant to propranolol, indomethacin, metiamide, cimetidine, methysergide, atropine and morphine. These findings appear to exclude the involvement of adrenergic mechanisms and prostaglandin generation as well as activation of classical M and D-tryptamine receptors by 5-HT in the goat pulmonary veins. This response may be mediated via a presynaptic inhibitory 5-HT receptor. 5 5-HT-induced arterial contractile responses were antagonized by methysergide, showing the occurrence of classical D receptors in the goat pulmonary artery. 6 It is concluded that differential reactivity of pulmonary arteries and veins to vasoactive agents may play differential role(s) in the pathophysiology of pulmonary disease. 5-HT may exert an antiinflammatory activity in goat pulmonary veins.
The psychoactive drugs imipramine, chlorpromazine and lithium chloride inhibit tryptamine tetrazolium reductase activity in vitro by 68, 60 and 33% respectively at a concentration of 1 x 10(-3) M while amphetamine negligibly inhibits the enzyme activity. No change in enzyme activity is observed in vivo.
We studied the dural plasma protein extravasation response after unilateral electrical stimulation of the trigeminal ganglion in mice lacking serotonin 5-HT1B (5-HT1D beta) receptors by modifying a technique previously described in rats or guinea pigs. We investigated the inhibitory effects of six 5-HT1 receptor agonists in this model: 3-(1,2,5,6-tetrahydropyrid-4-yl)pyrrolo[3,2-b]pyrid-5-one (CP-93,129), sumatriptan, serotonin-5-O-carboxymethyl-glycyl -tyrosinamide (GTI), 5-methylaminosulfonylmethyl-3-(N-methylpyrrolidin-2R -ylmethyl)-1H-indole (CP-122,288), 5-carboxamido-tryptamine (5-CT), and dihydroergotamine. The plasma extravasation response did not differ between wild-type and mutant after vehicle injection. The potency of sumatriptan, CP-122,288, CP-93,129, and 5-CT in wild-type mice was similar to that previously reported for rats. CP-122,288 (1 nmol kg), 5-CT (1 nmol/kg), and dihydroergotamine (72 nmol/kg) inhibited plasma protein extravasation within dura mater after electrical trigeminal ganglion stimulation in both wild-type and knockout mice, which suggests that these agonists act predominantly via receptors other than 5-HT1B. Unlike the wild-type mice, CP-93,129 (1.4 mumol/kg), a specific 5-HT1B receptor agonist, had no effect in knockout mice. The same held true for sumatriptan (0.7 mumol/kg) and GTI (0.6 mumol/kg). These results suggest that CP-93,129, sumatriptan, and GTI exert their effects via 5-HT1B (5-HT1D beta) receptors in mice.
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