Amyl nitrite appears as a clear colorless to yellowish liquid with a fragrant, fruity odor and pungent aromatic taste. Flash point below 73°F. Boiling point 205-210°F (96-99°C). Less dense than water and insoluble in water. Hence floats on water. Vapors are heavier than air. Produces toxic oxides of nitrogen during combustion. Used in medicine and to make other chemicals.
颜色/状态：
Yellowish liquid
气味：
Peculiar ethereal, fruity odor
味道：
Pungent, aromatic taste
蒸汽密度：
4 (NTP, 1992) (Relative to Air)
蒸汽压力：
3.97 mm Hg at 25 °C
自燃温度：
410 °F (USCG, 1999)
分解：
When heated to decomposition it emits toxic fumes of /nitrogen oxides/.
折光率：
Index of refraction: 1.3851 at 20 °C/D
保留指数：
695;706;680
稳定性/保质期：
按规格使用和储存，不会发生分解，应避免与氧化物接触。
计算性质
辛醇/水分配系数(LogP)：
1.8
重原子数：
8
可旋转键数：
4
环数：
0.0
sp3杂化的碳原子比例：
1.0
拓扑面积：
38.7
氢给体数：
0
氢受体数：
3
ADMET
代谢
肝脏。该药物通过可能的氢解脱硝作用迅速代谢；大约三分之一的吸入的氨基戊酸以尿液形式排出体外。
Hepatic. The drug is metabolized rapidly, probably by hydrolytic denitration; approximately one-third of the inhaled amyl nitrite is excreted in the urine.
IDENTIFICATION AND USE: Amyl nitrite is a clear, yellowish liquid. Amyl nitrite is a smooth muscle relaxant that has been used clinically to facilitate uterine relaxation in difficult deliveries. The use of amyl nitrite has been associated with sexual risk behavior and HIV infection among gay and bisexual men. HUMAN STUDIES: Inhalation of amyl nitrite by human volunteers in a gas mask and from ampoules crushed close to the nose did not induce hemoglobin oxidation, but it was associated with headache, tiredness, dizziness, and a fall in blood pressure. Two cases of amyl nitrite poisoning were presented. In both cases, severe methemoglobinemia developed after ingestion of approximately 10 mL of amyl nitrite. When admitted to hospital, both patients were deeply cyanosed, and arterial blood samples were noticed to be chocolate brown. There is also a case of a 37-year-old black man with HIV who developed chemical leukoderma in the nasal and perioral areas within 4 weeks of spilling liquid amyl nitrite, which he had been inhaling as a recreational drug, on his lower face. A case of blinding bilateral acute optic nerve disease was reported in a 15-year-old male apparently induced by inhalation of amyl nitrite. A patient with HIV infection developed a profound hemolytic anemia after repeated inhalation of large quantities of amyl nitrite. Amyl nitrite 'poppers' are recreational drugs, which are a potent source of nitric oxide. The use of 'poppers' can cause psychoactive stimulation, reduced blood pressure, tachycardia and involuntary muscle relaxation. In addition, research has found that popper use suppresses natural killer (NK) cell function, which increases vulnerability to infectious agents, produces sustained alterations in the immune system, and may be a Kaposi's sarcoma (KS) cofactor. The combined data implicate that the use of poppers may well pose as a significant risk factor for seroconversion. ANIMAL STUDIES: Amyl nitrite i.v. produced HbFe3+ much more rapidly than NaNO2 in dogs, cats, rabbits, and rats. In dogs, i.m. injection of amyl nitrite was followed by a very slow linear increase in the HbFe3+ content. Inhalation of amyl nitrite did not lead to HbFe3+ formation in dogs unless it was rebreathed in a closed (bag) or not completely open (gas mask) system. HbFe3+ was produced by oral amyl nitrite in dogs, the effect being enhanced by addition of DMSO. Intratracheal inhalation of amyl nitrite in the pentobarbitone/urethane anesthetized rabbit caused reductions in tidal volume and both inspiratory and expiratory times, without a preceding apnea, that were independent of the associated hypotension and of reflex influences from the carotid sinus region but dependent on supra-abdominal vagal integrity. In artificially ventilated, paralyzed rabbits amyl nitrite caused a pronounced sensitization of pulmonary stretch receptors during the inflation phase, typically with a reduction in the level of activity during the deflation phase. When tested for genotoxicity, amyl nitrite, was negative in the mouse lymphoma assay, but it was positive in the Salmonella typhimurium mutagenicity assay.
Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand-valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR as necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Nitrates, nitrites, and related compounds/
Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if necessary. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for shock and treat if necessary ... . Anticipate seizures and treat as necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 mL/kg up to 200 mL of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool. Administer activated charcoal ... . /Nitrates, nitrites, and related compounds/
Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious or is in severe respiratory distress. Monitor cardiac rhythm and treat arrhythmias if necessary. Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's (LR) if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. If unresponsive to these measures, vasopressors may be helpful. Watch for signs of fluid overload ... . Treat seizures with diazepam (Valium) or lorazepam (Ativan) ... . Administer 1% solution methylene blue if patient is symptomatic with severe hypoxia, cyanosis, and cardiac compromise not responding to oxygen. ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Nitrates, nitrites, and related compounds/
If this chemical gets into the eyes, remove any contact lenses at once and irrigate immediately for at least 15 min, occasionally lifting upper and lower lids. Seek medical attention immediately. If this chemical contacts the skin, remove contaminated clothing and wash immediately with soap and water. Seek medical attention immediately. If this chemical has been inhaled, remove from exposure, begin rescue breathing (using universal precautions, including resuscitation mask) if breathing has stopped and CPR if heart action has stopped. Transfer promptly to a medical facility. When this chemical has been swallowed, get medical attention. /Amyl nitrites/
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
吸收
Amyl nitrite vapor通过肺泡迅速吸收，吸入后一分钟即可显现治疗效果。
Amyl nitrite vapors are absorbed rapidly through the pulmonary alveoli, manifesting therapeutic effects within one minute after inhalation.
Novel pteridines of formula (I), ##SPC1## wherein R is a lower alkyl group, optionally substituted with a hydroxy group and R.sup.1 and R.sup.2 are the same or different and each is a lower alkyl group having together at least 3 carbon atoms or R.sup.1 and R.sup.2, together with the carbon atom in the pteridine ring structure, form a spirocycloalkyl ring system having 4 to 6 carbon atoms outside the pteridine ring structure, and their method of preparation. The above compounds have bacteriostatic activity.
Novel pteridines of formula (I), ##SPC1## wherein R is an optionally substituted phenoxyalkyl group, and R.sup.1 and R.sup.2 are the same or different and each is a lower alkyl group or R.sup.1 and R.sup.2, together with the carbon atom in the pteridine ring structure, form a spirocycloalkyl ring system having 4 to 6 carbon atoms outside the pteridine ring structure, And their method of preparation. The above compounds have bacteriostatic activity.
Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer.
Transition-metal complexes containing phosphorus ligands. Part IV. Convenient syntheses of some phosphine (and arsine) halogenonitrosyl derivatives of rhodium and iridium
作者：S. D. Robinson、M. F. Uttley
DOI：10.1039/j19710001254
日期：——
Convenient, single-stage syntheses involving addition of rhodium or iridium halides and N-methyl-N-nitrosotoluene-p-sulphonamide to a solution of the appropriate phosphine (or arsine) in a boiling alcoholic solvent have been used to prepare a selection of the halogenonitrosyl complexes, MX2(NO)(PR3)2 and MX2(NO)(AsPh3)2(M = Rh or Ir; X = Cl, Br, or I; R = alkyl, aryl, or mixed alkyl aryl). A mechanism
方便的单阶段合成涉及将铑或铱的卤化物和N-甲基-N-亚硝基甲苯-对磺酰胺添加到沸腾的醇溶剂中的合适的膦（或a）溶液中，用于制备卤代亚硝基配合物MX 2（NO）（PR 3）2和MX 2（NO）（AsPh 3）2（M = Rh或Ir; X = Cl，Br或I; R =烷基，芳基或混合的烷基芳基）。涉及铑（III）和铱（III）氢化物MX 2 H（PR 3）3的亚硝酰基形成机理，作为中间体进行了讨论。还报道了在这些反应中使用亚硝酸戊酯作为亚硝酰基配体的来源。
.beta.-thiopropionyl-aminoacid derivatives and their use as
申请人：SmithKline Beecham p.l.c.
公开号：US06048852A1
公开（公告）日：2000-04-11
A method of treatment of bacterial infections in humans or animals which comprises administering, in combination with a .beta.-lactam antibiotic, a therapeutically effective amount of an amino acid derivative of Formula (I) or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, ##STR1## wherein: R is hydrogen, a salt forming cation or an in vivo hydrolysable ester-forming group; R.sub.1 is hydrogen, (C.sub.1-6)alkyl optionally substituted by up to three halogen atoms or by a mercapto, (C.sub.1-6)alkoxy, hydroxy, amino, nitro, carboxy, (C.sub.1-6)alkylcarbonyloxy, (C.sub.1-6)alkoxycarbonyl, formyl or (C.sub.1-6)alkylcarbonyl group, (C.sub.3-7)cycloalkyl, (C.sub.3-7)cycloalkyl(C.sub.2-6)alkyl, (C.sub.2-6)alkenyl, (C.sub.2-6)alkynyl, aryl, aryl(C.sub.1-6)alkyl, heterocyclyl or heterocyclyl(C.sub.1-6)alkyl; R.sub.2 is hydrogen, (C.sub.1-6)alkyl or aryl(C.sub.1-6)alkyl; R.sub.3 is hydrogen, (C.sub.1-6)alkyl optionally substituted by up to three halogen atoms, (C.sub.3-7)cycloalkyl, fused aryl(C.sub.3-7)cycloalkyl, (C.sub.3-7)cycloalkyl(C.sub.2-6)alkyl, (C.sub.2-6)alkenyl, (C.sub.2-6)alkynyl, aryl, aryl-(CHR.sub.10).sub.m --X--(CHR.sub.11).sub.n, heterocyclyl or heterocyclyl-(CHR.sub.10).sub.m --X--(CHR.sub.11).sub.n, where m is 0 to 3, n is 1 to 3, each R.sub.10 and R.sub.11 is independently hydrogen or (C.sub.1-4)alkyl and X is O, S(O).sub.x where x is 0-2, or a bond; R.sub.4 is hydrogen, or an in vivo hydrolysable acyl group; and R.sub.5 and R.sub.6 are independently hydrogen and (C.sub.1-6)alkyl or together represent (CH.sub.2).sub.p where p is 2 to 5. Some compounds are claimed per se.
