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The effect of 4-acetyl-4-(3-chlorphenyl)-1-3'-dimethylaminopropyl)- -piperidine dihydrochloride on central nervous system, cardio-vasculary system and isolated organs of experimental animals was checked. Its analgesic and spasmalotytic properties were evaluated and the acute toxicity -- determined.
A series of new platinum(II) complexes of the type [Pt(II)(mmap)X] (where mmap, 1-methyl-4-(methylamino)piperidine and X, 1,1-cyclobutanedicarboxylato (CBDCA), oxalato, malonato, methylmalonato, dimethylmalonato, ethylmalonato, diethylmalonato or 2,3-naphthalene dicarboxylato (NDCA)) have been synthesized and characterized by elemental analysis, infrared (IR), and 13C and 195Pt nuclear magnetic resonance (NMR) spectroscopy. The crystal structure of the analogue [Pt(II)(mmap)(oxalate)] was determined using the single crystal X-ray diffraction method. Based upon a total of 4964 collected reflections, we determined that the compound crystallizes in the monoclinic space group P2(1)/c (with a=11.890(2) A, b=9.6695(19) A, c=9.875(2) A, beta=102.03(3) degrees, Z=4, and R=0.0428). In this complex, platinum has a slightly distorted square planar geometry with the two adjacent corners being occupied by two nitrogen atoms of the mmap ligand, whereas the remaining cis positions are occupied by two oxygen atoms of the oxalate molecule. The mmap ligand is in a boat conformation and forms six-membered chelating rings as well as the oxalate molecule forms five-membered chelating rings with platinum. The complexes were evaluated for their cytotoxic potential against the sensitive A2780 tumor model and cisplatin-resistant clone derived in vitro from potential cells.
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Both title compounds, C(30)H(33)BrN(2)O(3) and C(23)H(27)BrN(2)O(2), respectively, are brominated derivatives of the potent opioid cis-beta-hydroxy-3-methylfentanyl (ohmefentanyl). Ohmefentanyl has three asymmetric C atoms and, therefore, has eight possible stereoisomers. The absolute configurations of the title compounds were determined to assign the proper configuration of two of these stereoisomers and the compounds have the same stereochemistry at two of the three asymmetric C atoms.
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Products of decomposition of eight quaternary salts, derivatives of 1-[alpha-alkylthio-(p-dimethylamino)benzylidene]-piperidinium, in water, ethanol, pyridine and glacial acetic acid were investigated. IR and UV spectra of the obtained decomposition products were measured, and the compounds were tested for cytostatic activity.
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The previously reported oxytocin antagonist L-371,257 (2) has been modified at its acetylpiperidine terminus to incorporate various pyridine N-oxide groups. This modification has led to the identification of compounds with improved pharmacokinetics and excellent oral bioavailability. The pyridine N-oxide series is exemplified by L-372,662 (30), which possessed good potency in vitro (Ki = 4.1 nM, cloned human oxytocin receptor) and in vivo (intravenous AD50 = 0.71 mg/kg in the rat), excellent oral bioavailability (90% in the rat, 96% in the dog), good aqueous solubility (>8.5 mg/mL at pH 5.2) which should facilitate formulation for iv administration, and excellent selectivity against the human arginine vasopressin receptors. Incorporation of a 5-fluoro substituent on the central benzoyl ring of this class of oxytocin antagonists enhanced in vitro and in vivo potency but was detrimental to the pharmacokinetic profiles of these compounds. Although lipophilic substitution around the pyridine ring of compound 30 gave higher affinity in vitro, such substituents were a metabolic liability and caused shortfalls in vivo. Two approaches to prevent this metabolism, addition of a cyclic constraint and incorporation of trifluoromethyl groups, were examined. The former approach was ineffective because of metabolic hydroxylation on the constrained ring system, whereas the latter showed improvement in plasma pharmacokinetics in some cases.
By means of microiontophoresis, we have compared the actions of a putative sleep substance, piperidine, with other neurotransmitters in the rat anaesthetized with urethane. In the pons and midbrain, piperidine mimicked the actions of acetylcholine on more than 200 neurones. Piperidine- and acetylcholine-induced excitations were equally effectively antagonized by hexamethonium or atropine. In 32 neurones piperidine showed no affinity for the receptors for the excitatory amino acid agonists, quisqualate and N-methyl-D-aspartate, piperidine-evoked excitations being unaffected by the antagonists glutamate diethylester or 2-amino-5-phosphonovalerate. Similarly, piperidine-evoked excitations in 23 neurones were unaffected by alpha-methylnoradrenaline, suggesting that piperidine does not act at receptors for noradrenaline. Twenty per cent of neurones responsive to piperidine were inhibited. These inhibitions in 12 neurones were insensitive to either strychnine or bicuculline indicating that piperidine does not act on receptors for glycine or gamma-aminobutyric acid. In a further 68 neurones, neither hexamethonium (4 out of 59 cells) nor atropine (0 out of 9 cells) was effective in antagonizing the inhibitions evoked by piperidine or by acetylcholine. It is suggested that piperidine may exert its central hypnogenic effects by an action at cholinoceptors in brainstem areas involved in sleep regulation.