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Acrivastine

Synopsis, Chemistry

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Also known as: 87848-99-5, Semprex, Acrivastin, Acrivastinum, Acrivastina, Bw 825c

Molecular Formula

C₂₂H₂₄N₂O₂

Molecular Weight

348.4 g/mol

InChI Key

PWACSDKDOHSSQD-IUTFFREVSA-N

FDA UNII

A20F9XAI7W

Acrivastine is a synthetic alkylamine with non-sedative antihistaminergic activity. Acrivastine competitively blocks the histamine H1 receptor and limits the typical allergic and anaphylactic responses, including bronchoconstriction, vasodilation, increased capillary permeability, and spasmodic contraction of gastrointestinal smooth muscle, caused by actions of histamine on bronchial, and gastrointestinal smooth muscles, and on capillaries. This drug also prevents histamine-induced pain and itching of the skin and mucous membranes. (NCI05)

Acrivastine is a Histamine-1 Receptor Antagonist. The mechanism of action of acrivastine is as a Histamine H1 Receptor Antagonist.

1 2D Structure

Acrivastine

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

(E)-3-[6-[(E)-1-(4-methylphenyl)-3-pyrrolidin-1-ylprop-1-enyl]pyridin-2-yl]prop-2-enoic acid

2.1.2 InChI

InChI=1S/C22H24N2O2/c1-17-7-9-18(10-8-17)20(13-16-24-14-2-3-15-24)21-6-4-5-19(23-21)11-12-22(25)26/h4-13H,2-3,14-16H2,1H3,(H,25,26)/b12-11+,20-13+

2.1.3 InChI Key

PWACSDKDOHSSQD-IUTFFREVSA-N

2.1.4 Canonical SMILES

CC1=CC=C(C=C1)C(=CCN2CCCC2)C3=CC=CC(=N3)C=CC(=O)O

2.1.5 Isomeric SMILES

CC1=CC=C(C=C1)/C(=C\CN2CCCC2)/C3=CC=CC(=N3)/C=C/C(=O)O

2.2 Other Identifiers

2.2.1 UNII

A20F9XAI7W

2.3 Synonyms

2.3.1 MeSH Synonyms

1. Bw 825c

2. Bw-825c

3. Bw825c

4. Semprex

2.3.2 Depositor-Supplied Synonyms

1. 87848-99-5

2. Semprex

3. Acrivastin

4. Acrivastinum

5. Acrivastina

6. Bw 825c

7. Bw-825c

8. Bw A825c

9. Chebi:83168

10. (e)-6-((e)-3-(1-pyrrolidinyl)-1-p-tolylpropenyl)-2-pyridineacrylic Acid

11. 2-propenoic Acid, 3-(6-(1-(4-methylphenyl)-3-(1-pyrrolidinyl)-1-propenyl)-2-pyridinyl)-, (e,e)-

12. A20f9xai7w

13. 2-propenoic Acid,3-[6-[(1e)-1-(4-methylphenyl)-3-(1-pyrrolidinyl)-1-propenyl]-2-pyridinyl]-,(2e)-

14. (e)-3-[6-[(e)-1-(4-methylphenyl)-3-pyrrolidin-1-ylprop-1-enyl]pyridin-2-yl]prop-2-enoic Acid

15. Ncgc00182053-02

16. Acrivastinum [latin]

17. Acrivastina [spanish]

18. Acrivastine [usan:inn:ban]

19. (2e)-3-{6-[(1e)-1-(4-methylphenyl)-3-(pyrrolidin-1-yl)prop-1-en-1-yl]pyridin-2-yl}acrylic Acid

20. Acrivastine (usan/inn)

21. Unii-a20f9xai7w

22. (e)-6-((e)-3-(1-pyrrolidinyl-1-p-tolylpropenyl)-2-pyridinacrylsaeure

23. Acrivastine [mi]

24. Acrivastine [inn]

25. Dsstox_cid_2555

26. Acrivastine [usan]

27. Acrivastine [vandf]

28. Schembl4702

29. Acrivastine [mart.]

30. Chembl1224

31. Dsstox_rid_76625

32. Dsstox_gsid_22555

33. Acrivastine [who-dd]

34. Mls006010115

35. Bidd:gt0209

36. Bw270c

37. Dtxsid6022555

38. Acrivastine, >=98% (hplc)

39. Acrivastine [orange Book]

40. Hms3886e20

41. Bcp06189

42. Hy-b1510

43. Zinc3776633

44. Tox21_113015

45. Ac-912

46. Bdbm50487466

47. Benadryl Allgy Relief Plus Decongest

48. Mfcd00869830

49. S5718

50. Akos005067182

51. Semprex-d Component Acrivastine

52. Cs-6454

53. Db09488

54. Ncgc00182053-03

55. (2e)-3-{6-[(1e)-1-(4-methylphenyl)-3-pyrrolidin-1-ylprop-1-en-1-yl]pyridin-2-yl}prop-2-enoic Acid

56. Acrivastine Component Of Semprex-d

57. As-14623

58. Smr004701250

59. Cas-87848-99-5

60. D02760

61. D70156

62. 848a995

63. A916142

64. Q342745

65. Sr-01000942220

66. Q-200590

67. Sr-01000942220-1

68. (e)-3-{6-[3-pyrrolidino-1-(4-tolyl)prop-1e-enyl]-2-pyridyl}acrylic Acid

69. 6-(3-(1-pyrrolidinyl)-1-p-tolylpropenyl)-2-pyridineacrylic Acid

70. (e)-3-(6-((e)-3-(pyrrolidin-1-yl)-1-(p-tolyl)prop-1-en-1-yl)pyridin-2-yl)acrylic Acid

71. 3-(6-(1-(4-methylphenyl)-3-(1-pyrrolidinyl)-1-propenyl)-2-pyridinyl)-

72. 2-propenoic Acid, 3-[6-[(1e)-1-(4-methylphenyl)-3-(1-pyrrolidinyl)-1-propen-1-yl]-2-pyridinyl]-, (2e)-

2.4 Create Date

2005-09-16

3 Chemical and Physical Properties

Molecular Formula	C₂₂H₂₄N₂O₂
Molecular Weight	348.4 g/mol
XLogP3	1.6
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	6
Exact Mass	348.183778013 g/mol
Monoisotopic Mass	348.183778013 g/mol
Topological Polar Surface Area	53.4 Å²
Heavy Atom Count	26
Formal Charge	0
Complexity	514
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	2
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug Indication

For the relief of symptoms associated with seasonal allergic rhinitis such as sneezing, rhinorrhea, pruritus, lacrimation, and nasal congestion.

FDA Label

5 Pharmacology and Biochemistry

5.1 MeSH Pharmacological Classification

Histamine H1 Antagonists, Non-Sedating

A class of non-sedating drugs that bind to but do not activate histamine receptors (DRUG INVERSE AGONISM), thereby blocking the actions of histamine or histamine agonists. These antihistamines represent a heterogenous group of compounds with differing chemical structures, adverse effects, distribution, and metabolism. Compared to the early (first generation) antihistamines, these non-sedating antihistamines have greater receptor specificity, lower penetration of BLOOD-BRAIN BARRIER, and are less likely to cause drowsiness or psychomotor impairment. (See all compounds classified as Histamine H1 Antagonists, Non-Sedating.)

5.2 FDA Pharmacological Classification

5.2.1 Active Moiety

ACRIVASTINE

5.2.2 FDA UNII

A20F9XAI7W

5.2.3 Pharmacological Classes

Established Pharmacologic Class [EPC] - Histamine-1 Receptor Antagonist

5.3 ATC Code

R - Respiratory system

R06 - Antihistamines for systemic use

R06A - Antihistamines for systemic use

R06AX - Other antihistamines for systemic use

R06AX18 - Acrivastine

5.4 Absorption, Distribution and Excretion

Absorption

Acrivastine was absorbed rapidly from the combination capsule following oral administration and was as bioavailable as a solution of acrivastine. After administration of SEMPREX-D Capsules, maximum plasma acrivastine concentrations were achieved at 1.14 0.23 hour.

Route of Elimination

A mass balance study in 7 healthy volunteers showed that acrivastine is primarily eliminated by the kidneys. Over a 72-hour collection period, about 84% of the administered total radioactivity was recovered in urine and about 13% in feces, for a combined recovery of about 97%.

Volume of Distribution

0.46 0.05 L/kg

Clearance

2.9 0.7 mL/min/kg

5.5 Biological Half-Life

The mean terminal half-life for acrivastine was 1.9 0.3 hours following single oral doses and increased to 3.5 1.9 hours at steady state. The terminal half-life for the propionic acid metabolite was 3.8 1.4 hours.