• PRIYA GUPTA Department of Pharmacology, Oriental College of Pharmacy, Sanpada West, Navi Mumbai, Maharashtra, India.
  • VANITA G KANASE Department of Pharmacology, Oriental College of Pharmacy, Sanpada West, Navi Mumbai, Maharashtra, India.
  • SHALAKA KADAM Department of Pharmacology, Oriental College of Pharmacy, Sanpada West, Navi Mumbai, Maharashtra, India.
  • SALMAN KAPADIA Department of Pharmacology, Oriental College of Pharmacy, Sanpada West, Navi Mumbai, Maharashtra, India.
  • FALAK BAMNE Department of Pharmacology, Oriental College of Pharmacy, Sanpada West, Navi Mumbai, Maharashtra, India.



Histamine, Antihistaminic activity, Allergic rhinitis, Asthma, bronchoconstriction, Leukocytosis, Eosinophilia


Histamine is referred to as common allergic reactions and symptoms. Most of them are compared to histamine intolerance. Some common responses involved with this intolerance may vary but include headaches or migraines, nasal congestion or sinus problems, fatigue, hives, digestive problems, irregular menstrual cycle, nausea, and vomiting. Histamine is derived from a natural amino acid, S-histidine, through the histidine decarboxylase/ aromatic decarboxylase catalysis. Histamine is the compound that the mast cell generates for the immune response. Histamine promotes gastrointestinal secretion and induces capillary dilation, bronchial smooth muscle constriction, and reduced blood pressure. Antihistamines are medicinal products to treat allergic rhinitis and allergies. This includes the in vitro animal model and in-vivo tissue preparation antihistaminic activity. Animal models are significant instruments for understanding the pathological process of human illnesses in experimental medical science. Medicines associated with antihistamine include antiallergy, antivertigo, antimigraine, sedatives, antiemetic, etc. Elderly people are much more likely than youthful people to develop sleepiness from the use of antihistamines. The most common drugs used are cetirizine, levocetirizine, chlorpheniramine, diphenhydramine, loratadine, cimetidine, and fexofenadine. Animal models include histamine-induced bronchoconstriction, passive paw anaphylaxis, milk-induced leukocytosis and eosinophilia, clonidine, and haloperidol-induced catalepsy. While tissue models include isolated goat, and guinea-pig trachea chain preparation, as well as an isolated guinea pig, rat, mice ileum tissue preparation, and the dose-response curve of histamine, were plotted. The focus of the study had been on herbal plants and medicinal products, as they can effectively boost a variety of circumstances without significant adverse side effects. We can assess antihistaminic activity by using plant extracts or any synthetic drug.


Download data is not yet available.


Casale T, Rodbard D, Kaliner M. Characterization of histamine H1-receptors on human peripheral lung. Biochem Pharmacol 1985;34:3285-92.

Herxheimer H. Antihistamines in bronchial asthma. Br Med J 1949;2:901-5.

Wood-Baker R, Holgate S. The comparative actions and adverse effect profile of single doses of H1-receptor antihistamines in the airways and skin of subjects with asthma. J Allergy Clin Immunol 1993;91:1005-14.

Schmidt D, Ruehlmann E, Branscheid D, Magnussen H, Rabe KF. Passive sensitization of human airways increases responsiveness to leukotriene C4. Eur Respir J 1999;14:315-9.

Orzechowski RF, Currie DS, Valancius CA. Comparative anticholinergic activities of 10 histamine H1 receptor antagonists in two functional models. Eur J Pharmacol 2005;506:257-64.

Slater JW, Zechnich AD, Haxby DG. Second-generation antihistamines: A comparative review. Drugs 1999;57:31-47.

Zaseem K, Imitiyaz A, Vanita K. Evaluation of antihistaminic activity. World J Pharm Res 2018;7:278-88.

Saxena AK, Saxena M. Developments in antihistaminics (H1). In: Progress in Drug Research. Basel: Ernst Jucker; 1992. p. 35-126.

Shishoo CJ, Shirsath VS, Rathod IS, Vikas D. Design, synthesis and antihistaminic (H1) activity of some condensed, 3-aminopyrimidin- 4(3H)-ones. Yande Eur J Med Chem 2000;35:351-8.

Kubo N, Shirakawa O, Kuno T, Tanaka C. Antimuscarinic effect of antihistamines: Quantitative evaluation by receptor binding assay. Jpn J Pharmacol 1987;43:277-82.

Laak AM, den Kelder GM, Bast A, Timmerman H. Is there a difference in the affinity of histamine H1 receptor antagonists for CNS and peripheral receptors? An in vitro study. Eur J Pharmacol 1993;232:199-205.

Hindmarch I, Shamsi Z. Antihistamines: Models to assess sedative properties, assessment of sedation, safety and other side-effects. Clin Exp Allergy 1999;29:133-42.

Garrison JC. Histamine, bradykinine, 5-hydroxytryptamine and their antagonists. In: Gilman AG, Rall TE, Nies AS, Taylor P, editors. The Pharmacological Basis of Therapeutics. 8th ed. New York: Pergamon Press; 1990. p. 575.

Green JP, Weinstein H. Psychopharmacology: A Generation of Progress. New York: Raven Press; 1978. p. 319.

Thurmond RL, Gelfand EW, Dunford PJ. Review: The role of histamine H1 and H4 receptors in allergic inflammation: The search for new antihistamines. Nat Rev Drug Discov 2008;7:41-53.

Yong YK, Zakaria ZA, Kadir AA, Somchit MN, Lian GE, Ahmad Z. Chemical constituents and antihistamine activity of Bixa orellana leaf extract. BMC Complement Alternat Med 2013;13:1-7.

Rozenberg I, Sluka SH, Rohrer L, Hofman J, Becher B, Akhmedov A, et al. Histamine H1 receptor promotes atherosclerotic lesion formation by increase vascular permeability for low-density lipoproteins. Arterioscler Thromb Vasc Biol 2010;30:923-30.

Mobarakeh JI, Sakurada S, Katsuyama S, Kutsuwa M, Kuramasu A, Lin ZY, et al. Role of histamine H1 receptor in pain perception: A study of the receptor gene knockout mice. Eur J Pharmacol 2000;391:81-9.

Jutel M, Akdis M, Akdis CA. Histamine, histamine receptors and their role in immune pathology. Clin Exp Allergy 2009;39:1786-800.

Singh S, Agrawal SS. Broncho-relaxant activity of Belamcanda chinensis. Indian J Pharmacol 1990;22:107-9.

Tripathi RM, Das PK. Studies on anti-asthmatic and anti-anaphylactic activity of Albizia lebbeck. Indian J Pharmacol 1977;9:189.

Kumar D, Bhujbal SS, Deoda RS, Mudgade SC. In-vitro and in-vivo antiasthmatic studies of Ailanthus excelsa Roxb. On guinea pigs. J Sci Res 2010;2:196-202.

Gokhale AB, Saraf MN. Bronchoprotective effect of ethanolic extract of Tephrosia purpurea in-vivo. Indian Drugs 1996;37:346-7.

Evans WC, Trease EV. Pharmacognosy. 14th ed. London: W.B. Sunders Company; 1997. p. 250-1.

Nimgulkar CC, Patil SD, Kumar BD. Anti-asthmatic and anti-anaphylactic activities of Blatta orientalis mother tincture. Homeopathy 2011;100:138-43.

Okpo SO, Eze GI, Ajaanonwu IH, Ijei OL, Uwaya DO, Ologe V. Evaluation of the anti-asthma activity of aqueous root, bark extract of Ficus exasperata Vahl (Moraceae). Int J Health Res 2012;5:5-12.

Sharma P, Hullatti KK, Kuppasth IJ, Sharma S. Studies on anti-asthmatic property of Cyamopsis tetragonoloba (L.) Taub. Leaf extracts. J Natl Remed 2010;10:81-6.

Munish G, Chancal G. Effect of Phyllanthus urinaria in biochemical profile of experimental hyperglycemic albino rats. Res J Pharm Sci 2012;1:2-6.

Saxena P, Saxena P. In-vitro and in-vivo evaluation of anti-asthmatic activity of rhizomes extract of Acorus calamus (Linn.) in guinea pigs. Res J Pharm Sci 2014;2319:555.

Mitra SK, Gopumadhavan S, Venkataranganna MV, Anturlikar SD. Antiasthmatic and antianaphylactic effect of E-721B, a herbal formulation. Indian J Pharmacol 1999;31:133.

Slvvsn KS, Anbu J, Anjana A, Sumithra M, Sathish R. Influence of ethanolic leaf extract of Sargassum wightii and Adiantum capillus on histamine induced asthma in animal model. Int J Pharm Pharm Sci 2012;4:121-3.

Gosh MN. Fundamental of Experimental Pharmacology. 2nd ed. Calcutta: Scientific Book Agency; 1984. p. 132.

Kaushik D, Rani R, Kaushik P, Sacher D, Yadav J. In vivo and in vitro antiasthmatic studies of plant Piper longum Linn. Int J Pharmacol 2012;8:192-7.

Bhargava KP, Singh N. Antistress activity of Ocimum sanctum (linn). Indian J Med Res 1981;73:443-51.

Horn BR, Robin ED. Total eosinophils count in the management of bronchial asthma. N Engl J Med 1975;292:1152-5.

Mitra SK. Anti-asthmatic and anti-anaphylactic effect of e-721b: An herbal formulation. Indian J Pharmacol 1999;31:133-7.

Brekhman II, Dardymov IV. New substances of plant origin which increase nonspecific resistance. Annu Rev Pharmacol 1969;9:419-30.

Vadnere G, Somani R, Singhai AK. Studies on antiasthmatic activity of aqueous extract of Clerodendrum phlomidis. J Pharm Pharmacol 2006;58:164.

Taur DJ, Nirmal SA, Patil RY, Karma MD. Antistress and antiallergic effects of Ficus benghalensis bark in asthma. Nat Prod Res 2007;21:1266-70.

Mali RG, Dhake AS. Evaluation of effects of Bauhinia variegata stem bark extracts against milk-induced eosinophilia in mice. J Adv Pharm Technol Res 2011;2:132

Rajasekaran S. Evaluation of effects of Parthenium hysterophorus l, leaves extracts against, milk-induced eosinophilia in mice. Int J Pharm Sci Res 2014;5:1303-06.

Dusser D. Role of eosinophils in asthma. Rev Mal Respir 2000;17:195-201.

Kumar D, Bhujbal SS, Patil PS, Buge PV. In-vitro and in-vivo activities of stem bark of methanolic extract of Ailanthus excelsa Roxb. In the management of asthma. Int J Pharmacol 2010;6:284-9.

Ferré S, Guix T, Prat G, Jane F, Casas M. Is experimental catalepsy properly measured? Pharmacol Biochem Behav 1990;35:753-7.

Kumar D, Bhat ZA, Singh P, Bhujbal SS, Deoda RS. Antihistaminic activity of aqueous extract of stem bark of Ailanthus excelsa Roxb. Pharmacogn Res 2011;3:220.

Sanberg PR. Haloperidol-induced catalepsy is mediated by postsynaptic dopamine receptors. Nature 1980;284:472-3.

Chaudhari KN, Lahiri SC. Role of goat trachea for an isolated tracheal chain preparation. Indian J Pharmacol 1974;6:149-51.

Kulshrestha S, Misra SS, Sharma AL, Sharma P, Singhal D. Response of the goat trachea to some autonomic drugs. Indian J Pharmacol 1983;15:107-10.

Kiritikar KD, Basu BD. Indian Medicinal Plants. 1st ed. New Delhi: Periodical Experts Books Agency; 1991.

Nag CA, Lahiri SC. Use of goat trachea for an isolated tracheal chain preparation. Indian J Pharmacol 1974;6:149.

Hajare R, Darvhekar VM, Shewale A, Patil V. Evaluation of antihistaminic activity of piper betel leaf in guinea pig. Afr J Pharm Pharmacol 2011;5:113-7.

Castillo JC. The tracheal chain: I. A preparation for the study of antispasmodics with particular reference to bronchodilator drugs. J Pharmacol Exp Ther 1947;90:104-9.

Patil SD, Ahale SV, Surana SJ. Evaluation of antiasthmatic and antianaphylactic activity of Balanites aegyptiaca (delile), (balanitaceae). Asian J Pharm Clin Res 2011;4:52-5.

Manekar SS, Manoj S. Evaluation of anti-asthmatic activity of methanolic extract of Barleria prionitis Linn. Aerial parts. Int J Curr Pharm Res 2018;10:30-4.

Sirisha K, Achaiah G, Rao AR. Design, synthesis and evaluation of new 2, 6-dihydroimidazo [1, 2-c] pyrimido [5, 4-e]-Pyrimidine-5 (3H)- thiones as possible antihistaminic/antiasthmatic agents. Indian J Pharm Sci 2014;76:519.

Kaley G, Weiner R. Prostaglandin ‘E’a potential mediator. Ann N Y Acad Sci 1971;180:347-8.

Sagar R, Sahoo HB. Evaluation of antiasthmatic activity of ethanolic extract of Elephantopus scaber L. leaves. Indian J Pharmacol 2012;44:398.

Ghosh MN. Fundamentals of Experimental Pharmacology. Kolkata, India: Scientific Book Agency; 1984. p. 60-3.

Singh N, Nath R, Gupta ML, Kohli RP. An experimental evaluation of anti-asthmatic potentialitis of Inula racemosa (Puskar Mul). Quart J Crude Drug Res 1980;18:89-96.

Pandit P, Singh A, Bafna AR, Kadam PV, Patil MJ. Evaluation of antiasthmatic activity of Curculigo orchioides Gaertn. Rhizomes. Indian J Pharm Sci 2008;70:440.

Nagarajan K, Sharan G, Jeshvanth A, Nightingale T, Dheeneswari P, Sumanthi A. Evaluation of anti-histaminic activity of leaves of Acalypha canescana in isolated ileum of rabbit. Int J Pharm Pharm Sci 2010;2:19-20.

Afreen A, Kashyap P, Sawarkar H, Deshmukh V, Upadhyay A, Pal S.In-vitro and In-vivo models for evaluation of anti-asthmatic activity: A review. Int J Herbal Drug Res 2011;1:19-27.

Adusumalli SU, Ranjit PM, Harish MS. Antiasthmatic activity of aqueous extract of Pistacia integerrima galls. Int J Pharm Pharm Sci 2013;5 Suppl 2:116-21.

Taur DJ, Patil RN, Patil RY. Antiasthmatic related properties of Abrus precatorius leaves on various models. J Tradit Complement Med 2017;7:428-32.

Vogel GH, Vogel WH. Drug Discovery and Evaluation. Berlin: Spinger Verlag; 1998.

Butler A, Elswood CJ, Burridge J, Ireland SJ, Bunce KT, Kilpatrick GJ, et al. The pharmacological characterization of 5-HT3 receptors in three isolated preparations derived from guinea-pig tissues. Br J Pharmacol 1990;101:591-8.

Saikia B, Barua CC, Haloi P, Patowary P. Anticholinergic, antihistaminic, and antiserotonergic activity of n-hexane extract of Zanthoxylum alatum seeds on isolated tissue preparations: An ex vivo study. Indian J Pharmacol 2017;49:42.



How to Cite

GUPTA, P., V. G. KANASE, S. KADAM, S. KAPADIA, and F. BAMNE. “ANTIHISTAMINIC ACTIVITY MODELS”. Asian Journal of Pharmaceutical and Clinical Research, vol. 13, no. 8, Aug. 2020, pp. 51-55, doi:10.22159/ajpcr.2020.v13i8.38016.



Review Article(s)