BP 2.94

BP 2.94, or BP-294, also known as FUB-94, is a histamine H₃ receptor agonist which was under development for the treatment of asthma, inflammation, pain, and peptic ulcers but was never marketed.^[1]^[2]^[3]^[4]^[5] It is taken orally.^[1]

Other namesBP-294; BP 2-94; BP2-94; BP294; FUB-94; FUB94

Routes of
administrationOral^[1]

Drug classHistamine H₃ receptor agonist

ATC code

None

Quick facts Clinical data, Other names ...

BP 2.94
Clinical data

Other names	BP-294; BP 2-94; BP2-94; BP294; FUB-94; FUB94
Routes of administration	Oral^[1]
Drug class	Histamine H₃ receptor agonist
ATC code	None
Identifiers
IUPAC name 2-[N-[(2R)-1-(1H-imidazol-5-yl)propan-2-yl]-C-phenylcarbonimidoyl]phenol
PubChem CID	135422935
ChemSpider	23208952
ChEMBL	ChEMBL335419
Chemical and physical data
Formula	C₁₉H₁₉N₃O
Molar mass	305.381 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES C[C@H](CC1=CN=CN1)N=C(C2=CC=CC=C2)C3=CC=CC=C3O
InChI InChI=1S/C19H19N3O/c1-14(11-16-12-20-13-21-16)22-19(15-7-3-2-4-8-15)17-9-5-6-10-18(17)23/h2-10,12-14,23H,11H2,1H3,(H,20,21)/t14-/m1/s1 Key:SBUFZXRNKJQHLD-CQSZACIVSA-N

Pharmacology

The drug functions as an orally active prodrug of (R)-α-methylhistamine, which in turn acts as a potent and selective agonist of the histamine H₃ receptor.^[4]^[5] BP 2.94 has shown anti-inflammatory,^[4]^[5] antinociceptive,^[4]^[5] gastric anti-secretory,^[6] and sedative and hypnotic effects in animals.^[7] It has been found to increase slow wave sleep in animals, including dramatically so in cats.^[8]^[9]

Development

BP 2.94 was under development by Bioprojet.^[1]^[2]^[3] It reached phase 2 clinical trials prior to the discontinuation of its development.^[3]^[1]^[2]

References

[1]
"BP 294". AdisInsight. 28 November 2007. Retrieved 6 October 2025.
[2]
"Delving into the Latest Updates on BP-294 with Synapse". Synapse. 13 September 2025. Retrieved 6 October 2025.
[3]
Fozard JR (September 2000). "BP-294 Ste Civile Bioprojet". Current Opinion in Investigational Drugs. 1 (1): 86–89. PMID 11249601.
[4]
Rouleau A, Garbarg M, Ligneau X, Mantion C, Lavie P, Advenier C, et al. (June 1997). "Bioavailability, antinociceptive and antiinflammatory properties of BP 2-94, a histamine H3 receptor agonist prodrug". The Journal of Pharmacology and Experimental Therapeutics. 281 (3): 1085–1094. doi:10.1016/S0022-3565(24)36743-6. PMID 9190840.
[5]
Rouleau A, Stark H, Schunack W, Schwartz JC (October 2000). "Anti-inflammatory and antinociceptive properties of BP 2-94, a histamine H(3)-receptor agonist prodrug". The Journal of Pharmacology and Experimental Therapeutics. 295 (1): 219–225. doi:10.1016/S0022-3565(24)38890-1. PMID 10991982.
[6]
Soldani G, Bertini S, Rouleau A, Schwartz JC, Coruzzi G (December 1999). "Gastric antisecretory effects of compound BP 2-94: a histamine H3-receptor agonist prodrug". Digestive Diseases and Sciences. 44 (12): 2380–2385. doi:10.1023/a:1026606231771. PMID 10630485.
[7]
Monti JM, Jantos H, Ponzoni A, Monti D (July 1996). "Sleep and waking during acute histamine H3 agonist BP 2.94 or H3 antagonist carboperamide (MR 16155) administration in rats". Neuropsychopharmacology. 15 (1): 31–35. doi:10.1016/0893-133X(95)00151-3. PMID 8797189.
[8]
Thakkar MM (February 2011). "Histamine in the regulation of wakefulness". Sleep Medicine Reviews. 15 (1): 65–74. doi:10.1016/j.smrv.2010.06.004. PMC 3016451. PMID 20851648. Oral administration of BP 2.94 (20e30 mg/kg) produces a dosedependent increase in NREM sleep without affecting wakefulness or REM sleep in rats. Pretreatment with H3 receptor antagonist carboperamide (30 mg/kg) blocks the sleep inducing effects of BP 2.94 in rats. Conversely, oral administration of carboperamide (20e30 mg/kg) produces a dose-dependent increase in wakefulness with a concomitant decrease in NREM and REM sleep.60 Similarly, oral administration of H3 receptor agonist BP 2.94 induces a dramatic increase in NREM sleep in cats.61
[9]
Lin JS (October 2000). "Brain structures and mechanisms involved in the control of cortical activation and wakefulness, with emphasis on the posterior hypothalamus and histaminergic neurons". Sleep Medicine Reviews. 4 (5): 471–503. doi:10.1053/smrv.2000.0116. PMID 17210278. Indeed, as shown in Figure 6, oral application of BP2-94, a H3-receptor agonist (kindly provided by Bioprojet, Paris, France) induces a dramatic increase in the power spectral density of cortical slow activity in the cat, accompanied by a significant increase in SWS [23], whereas, in contrast, oral application of ciproxifan, a H3-receptor antagonist (also from Bioprojet, see Ref. 99), causes total suppression of cortical slow activity and spindles and marked enhancement of fast rhythms, and consequently induces waking (see details in Fig. 7).

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Pharmacology

Development

See also

References

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