Histamine

111.15

111.15

200-100-6

820484N8I3

33792

DTXSID4023125

NEEDLES FROM CHLOROFORM

L03AX14

2933290090

54.7

-0.7

White to light yellow Solid

1.1933 g/cm³

83-84 °C

209-210 °C @ Press: 18 Torr

180.3±8.1 °C

1.567

soluble in water, alcohol, and hot chloroform.

−20°C

LD50 i.p. in mice: 2020 mg/kg (Nagai)

PKA1= 9.68; PKA2= 5.88

120 Ų [M+H]+ [CCS Type: DT, Method: single field calibrated with Agilent tune mix (Agilent)]|120.4 Ų [M+H]+ [CCS Type: DT, Method: single field calibrated with ESI Low Concentration Tuning Mix (Agilent)]|120.4 Ų [M+H]+

DELIQUESCENT|PRISMS FROM ETHANOL; MP: 244-246 °C; FREELY SOL IN WATER, METHANOL /DIHYDROCHLORIDE/

Ⅲ

6.1(b)

UN 2811 6.1/PG 3

3

22-36/37/38-42/43

22-26-36/37

MS1050000

Xn

STABLE IN AIR BUT IS AFFECTED BY LIGHT /PHOSPHATE/

P261-P280-P301 + P310-P305 + P351 + P338-P342 + P311

H301-H315-H317-H319-H334-H335

|Danger|H301 (100%): Toxic if swallowed [Danger Acute toxicity, oral]|P261, P264, P270, P271, P272, P280, P285, P301+P310, P302+P352, P304+P340, P304+P341, P305+P351+P338, P312, P321, P330, P332+P313, P333+P313, P337+P313, P342+P311, P362, P363, P403+P233, P405, and P501|Aggregated GHS information provided by 42 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

LD50=807 mg/kg (mouse, oral). Side effects can lead to hypertension, hypotension, headache, dizziness, nervousness and tachycardia. Large overdoses can lead to seizures.

INHIBITORY EFFECT OF METHAMIDE (POTENT H2 ANTAGONIST) ON GASTRIC ACID SECRETION ELICITED BY CONTINUOUS HISTAMINE IV INFUSION IN MAX EFFECTIVE DOSE (20 UMOLE/HR) IN DOGS IS SHOWN TO BE APPROX 20%/10 UMOLE/KG AFTER 1.5 HR. COMPARABLE EFFECTS WERE OBSERVED IN NORMAL HUMANS IN SAME STUDY. /H2-RECEPTOR ANTAGONISTS, FROM TABLE/|IN GUINEA PIGS, DEATH BY ASPHYXIA FOLLOWS QUITE SMALL DOSES OF HISTAMINE, YET ANIMAL MAY SURVIVE A HUNDRED LETHAL DOSES OF HISTAMINE IF GIVEN AN H1-BLOCKING DRUG. IN SAME SPECIES, H1 ANTAGONISTS OFFER STRIKING PROTECTION AGAINST ANAPHYLACTIC BRONCHOSPASM, BUT THIS IS NOT SO IN MAN... /H1-RECEPTOR ANTAGONISTS/

OCCURS WIDELY IN NATURE AS A RESULT OF PUTREFACTIVE PROCESSES.|.../HISTAMINE/ IS A NATURAL CONSTITUENT OF BODY. ... LIBERATED FROM CELLS OF SKIN BY INJURIOUS STIMULI.../&/ INVOLVED IN MANY... DIVERSE PHYSIOLOGICAL PROCESSES...HISTAMINE RECEPTORS...FALL INTO 2 BROAD CLASSES: H1 & H2...|HISTAMINE IS WIDELY, IF UNEVENLY, DISTRIBUTED THROUGHOUT ANIMAL KINGDOM & IS PRESENT IN MANY VENOMS, NOXIOUS SECRETIONS, BACTERIA & PLANTS.

Histamine phosphate is indicated as a diagnostic aid for the evaluation of gastric acid secretory function.|Ceplene maintainance therapy is indicated for adult patients with acute myeloid leukaemia in first remission concomitantly treated with interleukin-2 (IL-2). The efficacy of Ceplene has not been fully demonstrated in patients older than age 60.

EXPTL USE: IN VET MEDICINE PRIMARILY FOR EXPTL PRODN OF ULCERS IN DOGS & HOGS, & OCCASIONALLY TO DETERMINE STATUS OF HYDROCHLORIC ACID SECRETION IN STOMACH OF DOGS BY USE OF "DIAGNEX BLUE-TEST" OR "GASTRO-TEST"...|EXPTL USE: ...ATTEMPTS HAVE BEEN MADE TO DESENSITIZE PT /TO HISTAMINE ALLERGIES/ WITH COURSES OF HISTAMINE INJECTIONS. THERE IS NO EXPTL EVIDENCE THAT SUCH REGIMES INDUCE SIGNIFICANT TOLERANCE...& PROCEDURE HAS NOT MET WITH GENERAL ACCEPTANCE.|PRACTICAL APPLICATIONS OF HISTAMINE FALL INTO TWO CATEGORIES: 1ST, ITS USES AS DIAGNOSTIC AGENT, WHICH FOR MOST PART ARE ON A SOUND PHYSIOLOGICAL BASIS; &, 2ND, ITS MORE CONTROVERSIAL USES IN THERAPY, ESP OF DISEASES OF ALLERGY.|AS DIAGNOSTIC AGENT IT IS OF VALUE IN TESTING FOR FUNCTIONAL CAPACITY OF GASTRIC GLANDS. IF NO ACID IS SECRETED FOLLOWING INJECTION OF 0.25-0.5 MG (USUALLY AS 1:1000 SOLN), A TRUE GASTRIC ACHYLIA EXISTS.|For more Therapeutic Uses (Complete) data for HISTAMINE (10 total), please visit the HSDB record page.

/WHEN HISTAMINE IS EMPLOYED TOPICALLY TO EYE IN CONCN FROM 0.1 TO 10% IT CAUSES/ VASODILATION & EDEMA OF CONJUNCTIVA.

Histamine stimulates gastric gland secretion, causing an increased secretion of gastric juice of high acidity. This action is probably due mainly to a direct action on parietal and chief gland cells.

Drugs that bind to and activate histamine receptors. Although they have been suggested for a variety of clinical applications histamine agonists have so far been more widely used in research than therapeutically. (See all compounds classified as Histamine Agonists.)

Readily absorbed after parenteral administration.|HISTAMINE IS READILY ABSORBED AFTER PARENTERAL INJECTION...|THE VARIOUS METAB, WHICH HAVE LITTLE OR NO PHARMACOLOGICAL ACTIVITY, ARE EXCRETED IN URINE.|HISTAMINE & N-METHYLHISTAMINE ACCUM IN TISSUE DEPOTS.

Primarily hepatic. Histamine is rapidly metabolized by methylation and oxidation. Methylation involves ring methylation and catalyzation by the enzyme histamine-N-methyltransferase, producing N-methylhistamine, which is mostly converted to N-methyl imidazole acetic acid. 2 to 3% excreted as free histamine, 4 to 8% as N-methylhistamine, 42 to 47% as N-methyl imidazole acetic acid, 9 to 11% as imidazole acetic acid, and 16 to 23% as imidazole acetic acid riboside.|IN MAN THERE ARE 2 MAJOR PATHS OF HISTAMINE METAB. MORE IMPORTANT ONE INVOLVES RING METHYLATION & IS CATALYZED BY...HISTAMINE-N-METHYLTRANSFERASE (IMIDAZOLE-N-METHYLTRANSFERASE, INMT). MOST OF PRODUCT, METHYLHISTAMINE, IS CONVERTED BY MONOAMINE OXIDASE TO METHYL IMIDAZOLE ACETIC ACID (METHYL IMAA).|IN OTHER PATH, HISTAMINE UNDERGOES OXIDATIVE DEAMINATION CATALYZED MAINLY BY DIAMINOXIDASE (DAO), ALSO CALLED "HISTAMINASE"... THE PRODUCTS ARE IMIDAZOLE ACETIC ACID (IMAA) &, EVENTUALLY, ITS RIBOSIDE.|.../MUCH OF VERY LARGE AMT OF HISTAMINE GIVEN ORALLY/ IS CONVERTED BY INTESTINAL BACTERIA TO N-ACETYLHISTAMINE.

Histamine acts directly on the blood vessels to dilate arteries and capillaries; this action is mediated by both H 1- and H 2-receptors. Capillary dilatation may produce flushing of the face, a decrease in systemic blood pressure, and gastric gland secretion, causing an increased secretion of gastric juice of high acidity. Increased capillary permeability accompanies capillary dilatation, producing an outward passage of plasma protein and fluid into the extracellular spaces, an increase in lymph flow and protein content, and the formation of edema. In addition, histamine has a direct stimulant action on smooth muscle, producing contraction if H 1-receptors are activated, or mostly relaxation if H 2-receptors are activated. Also in humans, the stimulant effect of histamine may cause contraction of the intestinal muscle. However, little effect is noticed on the uterus, bladder, or gallbladder. Histamine has some stimulant effect on duodenal, salivary, pancreatic, bronchial, and lacrimal glands. Histamine also can bind to H3 and H4 receptors which are involved in the CNS/PNS neurotransmitter release and immune system chemotaxis, respectively.|...CONTRACTS MANY SMOOTH MUSCLES, SUCH AS...BRONCHI & GUT, BUT...RELAXES OTHERS...OF FINE BLOOD VESSELS. IT IS...POTENT STIMULUS TO GASTRIC ACID PRODUCTION & ELICITS...OTHER EXOCRINE SECRETIONS. ...BRONCHOCONSTRICTION & CONTRACTION OF GUT...INVOLVE H1 RECEPTORS...GASTRIC SECRETION...INVOLVE ACTIVATION OF H2 RECEPTORS...|...AT CELLULAR LEVEL, MANY RESPONSES TO HISTAMINE ARE CLEARLY ATTRIBUTABLE TO INCR IN MEMBRANE PERMEABILITY THAT ALLOWS COMMON INORG IONS (MAINLY CATIONS) TO FLOW DOWN ELECTROCHEM GRADIENTS & ALTER TRANSMEMBRANE POTENTIAL. IT DOUBTLESS EXPLAINS STIMULANT ACTIONS...OF HISTAMINE ON NERVE ENDINGS OR GANGLION CELLS...|...ESSENTIALLY SIMILAR ACTION /TO THAT AT CELLULAR LEVEL/ APPEARS TO ACCOUNT FOR SECRETION, AT LEAST AS IT OCCURS IN CHROMAFFIN CELLS OF ADRENAL MEDULLA. HERE HISTAMINE...MIMIC PHYSIOLOGICAL SECRETAGOGUE ACH IN DEPOLARIZING THE PLASMALEMMA.|MODE OF ACTION OF HISTAMINE...TO PRODUCE SMOOTH MUSCLE RELAXATION, INCL VASODILATION, HAS NOT BEEN DEFINED.|CLASSICAL...ANTIHISTAMINES ARE...CAPABLE OF BLOCKING...H1 RECEPTORS ONLY... H2 RECEPTORS...ARE INHIBITED PREFERENTIALLY BY H2-RECEPTORS ANTAGONISTS.

OVERDOSAGE WITH HISTAMINE IS RARE, & SYMPTOMS ARE GENERALLY NOT DANGEROUS. HOWEVER, MASSIVE DOSES CAUSE INTENSE HEADACHE, FLUSHING, PROFOUND FALL OF BLOOD PRESSURE, BRONCHOSPASM, DYSPNEA, A METALLIC TASTE, VOMITING & DIARRHEA.|.../EYE EFFECT/ OF AN 8% SOLN OF HISTAMINE HYDROCHLORIDE HAS BEEN DESCRIBED IN CASE OF GIRL WHO SPILLED SOME...ON HER HANDKERCHIEF & CONTAMINATED HER RIGHT EYE... IN 10 MIN CONJUNCTIVAE BECAME HYPEREMIC & LIDS EDEMATOUS, WITHOUT DISCOMFORT. REACTION HAD NEARLY DISAPPEARED IN 5 HR & COMPLETELY GONE NEXT DAY... /HCL SALT/|IN SOME HUMAN GLAUCOMATOUS EYES, APPLICATION OF 3% HISTAMINE HYDROCHLORIDE EYEDROPS HAS BEEN KNOWN TO CAUSE RISE IN OCULAR PRESSURE, PARTICULAR IN CASES OF ACUTE GLAUCOMA. /HCL SALT/|...INJECTED INTRADERMALLY...TRIPLE RESPONSE /FOLLOWS/...RED SPOT...BRIGHTER RED...FLARE...DEVELOPING...MORE SLOWLY, &...LOCALIZED EDEMA...DUE TO LOCAL DILATATION OF MINUTE BLOOD VESSELS /&/...DILATATION OF NEIGHBORING ARTERIOLES.../& EDEMA/ DUE TO DIRECT ACTION...ON WALLS OF...VESSELS TO INCR THEIR PERMEABILITY.

Ceplene

HISTAMINE PHOSPHATE, USP, & HISTAMINE DIHYDROCHLORIDE... HISTAMINE PHOSPHATE INJECTION, USP, CONTAINS 1 MG OF SALT (0.36 MG OF HISTAMINE BASE) IN 1 ML. OTHER AVAIL PREPN CONTAIN 0.275 & 2.75 MG OF HISTAMINE PHOSPHATE IN 1 ML (0.1 & 1 MG OF HISTAMINE BASE IN 1 ML), & ARE PACKAGED IN 1- OR 5-ML AMPULES.

1H-Imidazole-5-ethanamine: ACTIVE

BIOLOGICAL METHOD; 18.067, FLUOROMETRIC METHOD; & 18.072, COLORIMETRIC METHOD FOR DETERMINATION OF HISTAMINE IN FISH & OTHER MARINE PRODUCTS.|DIRECT ANALYSIS OF HISTAMINE BY HPLC THROUGH VISUALIZATION OF EMERGING SUBSTANCES BY EXAM OF ELUATES AT 208 NM USING COLUMN OF MICROPARTICULATE SILICA GEL, TREATED WITH BETA-CYANOETHYLTRIETHOXYSILANE & HCL. METHOD IS SIMPLE, SELECTIVE, PRECISE & SENSITIVE TO 1 MCG/ML.

Human drugs -> Ceplene -> EMA Drug Category|Immunostimulants -> Human pharmacotherapeutic group