Synonym
Anacardone; Anacordone; Astrocar; beta-Pyrimidum;
IUPAC/Chemical Name
3-Pyridinecarboxamide, N,N-diethyl-
InChi Key
NCYVXEGFNDZQCU-UHFFFAOYSA-N
InChi Code
InChI=1S/C10H14N2O/c1-3-12(4-2)10(13)9-6-5-7-11-8-9/h5-8H,3-4H2,1-2H3
SMILES Code
O=C(C1=CC=CN=C1)N(CC)CC
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
Nikethamide, one of the respiratory central stimulants, has the potential for respiratory failure research.
In vitro activity:
To investigate the effects of nikethamide on the generation and modulation of rhythmic respiration of neonatal rats and the role of 5-HT(2A) receptor in this course, experiments were performed on the transverse medullary slices of neonatal rats (both sexes, 1-3 d) in vitro. Nikethamide increased RRDA in transverse medullary slices at 0.5-7 μg/mL, and 5 μg/mL was the most effective concentration.
Reference: Sheng Li Xue Bao. 2008 Apr 25;60(2):216-20. https://pubmed.ncbi.nlm.nih.gov/18425309/
|
Solvent |
mg/mL |
mM |
comments |
Solubility |
DMSO |
18.0 |
100.99 |
|
Water |
50.0 |
280.53 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
178.24
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
Qian ZB, Wu ZH. [Role of 5-HT(2A) receptor in increase in respiratory-related rhythmic discharge activity by nikethamide in neonatal rat transverse medullary slices]. Sheng Li Xue Bao. 2008 Apr 25;60(2):216-20. Chinese. PMID: 18425309.
In vitro protocol:
Qian ZB, Wu ZH. [Role of 5-HT(2A) receptor in increase in respiratory-related rhythmic discharge activity by nikethamide in neonatal rat transverse medullary slices]. Sheng Li Xue Bao. 2008 Apr 25;60(2):216-20. Chinese. PMID: 18425309.
1: Lewis JH. Determination of nikethamide and N-ethylnicotinamide in the blood and urine of greyhounds. J Chromatogr. 1979 Apr 21;172:295-302. PubMed PMID: 548532.
2: Schechter MD. Potentiation of cathinone by caffeine and nikethamide. Pharmacol Biochem Behav. 1989 Jun;33(2):299-301. PubMed PMID: 2813469.
3: Chen L, Liao L, Zuo Z, Yan Y, Yang L, Fu Q, Chen Y, Hou J. Simultaneous determination of nikethamide and lidocaine in human blood and cerebrospinal fluid by high performance liquid chromatography. J Pharm Biomed Anal. 2007 Apr 11;43(5):1757-62. Epub 2006 Dec 30. PubMed PMID: 17289323.
4: Qian ZB, Qi Y, Wu ZH. [GABA A receptor participates in respiratory enhancement induced by nikethamide in neonatal rats]. Nan Fang Yi Ke Da Xue Xue Bao. 2008 Mar;28(3):301-4. Chinese. PubMed PMID: 18359677.
5: Delbeke FT, Debackere M. Excretion and metabolism of nikethamide in the horse. Br J Sports Med. 1976 Oct;10(3):116-23. PubMed PMID: 11864; PubMed Central PMCID: PMC1859729.
6: Qian ZB, Wu ZH. [Role of 5-HT(2A) receptor in increase in respiratory-related rhythmic discharge activity by nikethamide in neonatal rat transverse medullary slices]. Sheng Li Xue Bao. 2008 Apr 25;60(2):216-20. Chinese. PubMed PMID: 18425309.
7: Gilston A. Nikethamide for hiccough. Anaesthesia. 1979 Nov-Dec;34(10):1060. PubMed PMID: 539646.
8: CARLSSON A, SERIN F. The toxicity of nikethamide at different times of the day. Acta Pharmacol Toxicol (Copenh). 1950;6(2):187-93. PubMed PMID: 24537965.
9: DRAPER T. Nikethamide. Indian Physician. 1945 Aug;4:187-90. PubMed PMID: 20991346.
10: Nakatani J, Moreira MA, Uehara C, Romaldini H, dos Santos ML. [Use of nikethamide in patients with chronic respiratory acidosis]. AMB Rev Assoc Med Bras. 1979 Nov;25(11):382-4. Portuguese. PubMed PMID: 317728.
11: Okide GB, Odoh UE, Ajali U. Spectrophotometric determination of nikethamide by charge--transfer complexation with chloranilic acid. Boll Chim Farm. 2002 Jul-Aug;141(4):299-303. PubMed PMID: 12426818.
12: PROENCA J, WENNER J. [ON THE EFFECT OF NIKETHAMIDE AND HOMOVERATRIC ACID DIMETHYLAMIDE ON RESPIRATION IN INFANTS]. Monatsschr Kinderheilkd. 1965 Apr;113:341-3. German. PubMed PMID: 14311254.
13: Huang RH, Zhou D, He CQ. [Pharmacokinetics and pharmacodynamics of nikethamide after endotracheal administration in dogs]. Zhongguo Yao Li Xue Bao. 1994 May;15(3):271-4. Chinese. PubMed PMID: 7976386.
14: Guru VK, Singh HS, Sharma IJ, Quadri MA. EFFECT OF NIKETHAMIDE AND DIAZEPAM ON THE LEVELS OF BIOGENIC AMINES IN THE DIFFERENT PARTS OF THE POULTRY BRAIN AT THREE AGE GROUPS. Indian J Physiol Pharmacol. 1999 Jan;43(1):104-8. PubMed PMID: 27093746.
15: Chen CF, Fang HS. Effect of ephedrine and coramine (nikethamide) on hypoxic tolerance in mice. Taiwan Yi Xue Hui Za Zhi. 1974 Jul;73(7):401-3. PubMed PMID: 4530821.
16: LOEWE S. Isobols of dose-effect relations in the combination of nikethamide (coramine) and phenobarbital. J Pharmacol Exp Ther. 1955 Sep;115(1):6-14. PubMed PMID: 13264050.
17: ECKENHOFF JE, HAFKENSCHIEL JH. The effect of nikethamide on coronary blood flow and cardiac oxygen metabolism. J Pharmacol Exp Ther. 1947 Dec;91(4):362-9. PubMed PMID: 20273271.
18: Schmitz H, Schunack W. [Structure-activity relationships in nikethamide type analeptics. 3. Synthesis of 6-methylnikethamide]. Arch Pharm (Weinheim). 1975 May;308(5):359-64. German. PubMed PMID: 240338.
19: Franko BV, Ward JW. Nikethamide and doxapram effects on pentazocine- and morphine-induced respiratory depression. J Pharm Pharmacol. 1971 Sep;23(9):709-10. PubMed PMID: 4398252.
20: Lüdtke AH, Scharrer P, Schmidt L. [The effects of Bemegride, Pentetrazole and Nikethamide on blood pressure, heart rate and respiration in alcohol-intoxicated rats]. Arzneimittelforschung. 1970 Oct;20(10):1482-5. German. PubMed PMID: 4394724.