. 2019 Jun 7;177(3):580–599. doi: 10.1111/bph.14696

Table 1.

A summary of the effects produced by histamine receptor ligands in animal models of neuropathic pain

Drug	Model	Strain	Test	Effect	Reference
H₁ antagonists
Astemizole	Neurectomy	Sabra rats	Score	i.p. suppressed autotomy	Seltzer, Paran, Eisen, & Ginzburg, 1991
Chlorpheniramine	TNT	Wistar rats	Acetone	i.p. reduced allodynia and prevented cold plate avoidance behaviour	Khalilzadeh et al., 2018
			von Frey
			Double plate
			Open field
	PLSN	Wistar rats	Hargreaves	i.p. suppressed and alleviated hyperalgesia	Zuo et al., 2003
	PLSN	Wistar rats	Randall‐Selito	i.p. suppressed and alleviated hyperalgesia	Zuo et al., 2003
Fexofenadine	TNT	Wistar rats	Acetone	p.o. reduced allodynia and prevented cold plate avoidance behaviour	Khalilzadeh et al., 2018
			von Frey
			Double plate
			Open field
http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7216	Peripheral axotomy	Sprague–Dawley rats	Score of autotomy	i.p. did not block analgesic effects of histidine on pain behaviour but alone suppressed autotomy	Yu et al., 2013
Mepyramine (pyrilamine)	PLSN	Sprague–Dawley rats	von Frey	Intrathecally, i.c.v. blocked analgesic effects of histidine on pain behaviour	Yu et al., 2016
	PLSN	Sprague–Dawley rats	IR laser		Yu et al., 2016
	SNL	Hannover‐Wistar rats	von Frey	Intrathecally did not attenuate the antihypersensitivity effect of histamine	Wei, Viisanen, You, & Pertovaara, 2016
	SNL	Hannover‐Wistar rats	Radiant heat		Wei, Viisanen, You, & Pertovaara, 2016
	SNL	Hannover‐Wistar rats	von Frey test	Into LC did not attenuate the antihypersensitivity effect of histamine and alone failed to influence pain	Wei, Jin, Viisanen, You, & Pertovaara, 2014
	SNL	Hannover‐Wistar rats	Radiant heat		Wei, Jin, Viisanen, You, & Pertovaara, 2014
	PLSN	Rats	von Frey	i.c.v was ineffective	Huang, Adachi, Nagaro, Liu, & Arai, 2007
http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=7282	Vincristine induced	Wistar albino rats	Pinprick	i.p. reduced hyperalgesia and allodynia	Jaggi, Kaur, Bali, & Singh, 2017
			Acetone
			Hot plate
H₂R antagonists
Cimetidine	PLSN	Sprague–Dawley rats	von Frey	Intrathecally, i.c.v. did not block histidine's analgesic effects on pain behaviour	Yu et al., 2016
	PLSN	Sprague–Dawley rats	IR laser		Yu et al., 2016
	PLSN	Wistar rats	Hargreaves	i.p. suppressed and alleviated hyperalgesia	Zuo et al., 2003
	PLSN	Wistar rats	Randall‐Selito	i.p. suppressed and alleviated hyperalgesia	Zuo et al., 2003
Famotidine	TNT	Wistar rats	Acetone	p.o. was ineffective in all tests	Khalilzadeh et al., 2018
			von Frey
			Double plate
			Open field
	PLSN	Sprague–Dawley rats	von Frey	i.p. reduced allodynia and hyperalgesia	Yue et al., 2014
	PLSN	Sprague–Dawley rats	Diode laser	i.p. reduced allodynia and hyperalgesia	Yue et al., 2014
Ranitidine	TNT	Wistar rats	Acetone	i.p. reduced allodynia and prevented cold plate avoidance behaviour	Khalilzadeh et al., 2018
			von Frey
			Double plate
			Open field
	Vincristine induced	Wistar rats	Pinprick	i.p. reduced hyperalgesia and allodynia	Jaggi et al., 2017
			Acetone
			Hot plate
	PLSN	Rats	von Frey	i.c.v. increased hypersensitivity	Huang et al., 2007
Zolantidine	SNL	Hannover‐Wistar rats	von Frey	i.t. attenuated the antihypersensitivity effect of histamine	Wei et al., 2016
	SNL	Hannover‐Wistar rats	Radiant heat		Wei et al., 2016
	SNL	Hannover‐Wistar rats	von Frey	Into LC attenuated histamine's analgesic effect but alone failed to influence pain	Wei et al., 2014
	SNL	Hannover‐Wistar rats	Radiant heat		Wei et al., 2014
H₃R antagonists and H₃R antagonists/inverse agonist
A‐960656	SNL	Hannover‐Wistar rats	von Frey	Into LC reduced hypersensitivity	Wei et al., 2014
	SNL	Hannover‐Wistar rats	Radiant heat	Into LC reduced hypersensitivity	Wei et al., 2014
	SNL	Hannover‐Wistar rats	von Frey	i.t. reduced hypersensitivity	Wei et al., 2016
	SNL	Hannover‐Wistar rats	Radiant heat	i.t. reduced hypersensitivity	Wei et al., 2016
	SNL	Sprague–Dawley rats	von Frey	p.o. reduced hypersensitivity	Cowart et al., 2012
http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?ligandId=1265	SNI	BL6 mice	Hargreaves	i.p. was ineffective	Zhang et al., 2012
	SNI	BL6 mice	Dynamic plantar aesthesiometer	i.p. was ineffective	Zhang et al., 2012
E‐162	CCI	Swiss CD1 mice	von Frey	i.p. reduced hypersensitivity	Popiolek‐Barczyk et al., 2018
			Cold plate
			Tail‐flick
GSK189254	CCI	Random‐hooded rats	von Frey	p.o. reduced allodynia and hyperalgesia	Medhurst et al., 2008
	CCI	Random‐hooded rats	Randall‐Selito	p.o. reduced allodynia and hyperalgesia	Medhurst et al., 2008
	SNL	Sprague–Dawley rats	von Frey	i.p. reduced allodynia	Hsieh et al., 2010
GSK334429	CCI	Random‐hooded rats	von Frey	p.o. reduced allodynia and hyperalgesia	Medhurst et al., 2008
GSK334429	CCI	Random‐hooded rats	Randall‐Selito	p.o. reduced allodynia and hyperalgesia	Medhurst et al., 2008
Pitolisant	SNI	BL6 mice	Hargreaves	i.p. was ineffective, high doses increased thermal but not mechanical hypersensitivity	Zhang et al., 2012
Pitolisant	SNI	BL6 mice	Dynamic plantar aesthesiometer		Zhang et al., 2012
S38093	CCI and oxaliplatin induced	Sprague–Dawley rats	Randall‐Selito	p.o. reduced hypersensitivity	Chaumette et al., 2018
S38093	CCI and oxaliplatin induced	Sprague–Dawley rats	Tail‐immersion (10°C)	p.o. reduced hypersensitivity	Chaumette et al., 2018
ST‐889	SNI	BL6 mice	Hargreaves	i.p. was ineffective	Zhang et al., 2012
ST‐889	SNI	BL6 mice	Dynamic plantar aesthesiometer	i.p. was ineffective	Zhang et al., 2012
Thioperamide	PLSN	Rats	von Frey	i.c.v. increased but i.p. reduced hypersensitivity	Huang et al., 2007
Thioperamide	PLSN	Sprague–Dawley rats	Randall‐Selito	i.p. increased hypersensitivity	Smith et al., 2007
H₄R agonists
ST‐1006	SNI	CD1 mice	Hargreaves	i.c.v. reduced allodynia and hyperalgesia	Sanna et al., 2015
ST‐1006	SNI	CD1 mice	Dynamic plantar aesthesiometer	i.c.v. reduced allodynia and hyperalgesia	Sanna et al., 2015
VUF‐8430	SNI	CD1 mice	Hargreaves	i.c.v. reduced allodynia and hyperalgesia	Sanna et al., 2015
	SNI	CD1 mice	Dynamic plantar aesthesiometer	i.c.v. reduced allodynia and hyperalgesia	Sanna et al., 2015
	SNI	CD1 mice	Hargreaves	i.t.reduced allodynia and hyperalgesia	Sanna, Lucarini, et al., 2017
	SNI	CD1 mice	Dynamic plantar aesthesiometer	i.t.reduced allodynia and hyperalgesia	Sanna, Lucarini, et al., 2017
	PLSN	Sprague–Dawley rats	Randall‐Selito	i.p. reduced hypersensitivity	Smith et al., 2007
H₄R antagonists
JNJ7777120	PLSN	Sprague–Dawley rats	Randall‐Selito	i.p. increased hypersensitivity	Smith et al., 2007
JNJ7777120	SNL	Sprague–Dawley rats	von Frey	i.p. reduced allodynia	Hsieh et al., 2010
JNJ10191584	SNI	CD1 mice	Hargreaves	p.o. blocked the analgesic effect of i.c.v. ST‐1006 and VUF‐8430 and was ineffective alone	Sanna et al., 2015
	SNI	CD1 mice	Dynamic plantar aesthesiometer		Sanna et al., 2015
	SNI	CD1 mice	Hargreaves	p.o. blocked the analgesic effect of i.t. VUF‐8430 and was ineffective alone	Sanna et al., 2015
	SNI	CD1 mice	Dynamic plantar aesthesiometer		Sanna et al., 2015
TR‐7	CCI	Swiss CD1 mice	von Frey	i.p. reduced hypersensitivity	Popiolek‐Barczyk et al., 2018
			Cold plate
			Tail‐flick

Abbreviations: CCI, chronic constriction nerve injury; LC, locus coeruleus; PLSN, partial ligation of sciatic nerve; SNI, spared nerve injury; SNL, spinal nerve ligation; TNT, tibial nerve transection.