Chemistry:SCH-50971

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SCH-50971 is a histamine H3 receptor agonist which was under development for the treatment of anxiety disorders, gastrointestinal disorders, and migraine but was never marketed.[1][2]

Pharmacology

The drug acts as a potent, selective, and high-affinity agonist of the histamine H3 receptor.[3][4] It has negligible affinity for the histamine H1 receptor and other assessed receptors.[3] The drug is also not a histamine H2 receptor antagonist.[3] It has greatly improved selectivity compared to the earlier selective histamine H3 receptor agonist (R)-α-methylhistamine.[3][4] The drug is orally active and shows anti-allergy effects, antimigraine effects, sedative and hypnotic effects, and hypolocomotion in animals.[5][6][7] In terms of chemical structure, it is a cyclized pyrrolidine derivative of histamine.[8][3]

Development

SCH-50971 was under development by Schering-Plough.[1] It reached the discovery or preclinical research stage of development.[2] The development of the drug was discontinued by 2001.[1] SCH-50971 was first described in the scientific literature by 1994.[9][10]

See also

References

  1. ↑ 1.0 1.1 1.2 "SCH 50971". 7 September 2001. https://adisinsight.springer.com/drugs/800004504. 
  2. ↑ 2.0 2.1 "Delving into the Latest Updates on Sch-50971 with Synapse". 13 September 2025. https://synapse.patsnap.com/drug/d68364c40248440f9c929a9831c29daa. 
  3. ↑ 3.0 3.1 3.2 3.3 3.4 "Studies on the pharmacology of the novel histamine H3 receptor agonist Sch 50971". Arzneimittel-Forschung 48 (9): 881–888. September 1998. PMID 9793613. 
  4. ↑ 4.0 4.1 "Trans-4-methyl-3-imidazoyl pyrrolidine as a potent, highly selective histamine H3 receptor agonist in vivo". Bioorganic & Medicinal Chemistry Letters 8 (3): 243–248. February 1998. doi:10.1016/s0960-894x(98)00020-1. PMID 9871662. 
  5. ↑ "Substance P is involved in the effect of histamine H3 receptor agonist, Sch 50971 on nasal allergic symptoms in mice". International Immunopharmacology 8 (8): 1083–1088. August 2008. doi:10.1016/j.intimp.2008.03.018. PMID 18550011. 
  6. ↑ "Participation of histamine H3 receptors in experimental allergic rhinitis of mice". Journal of Pharmacological Sciences 108 (2): 206–211. October 2008. doi:10.1254/jphs.08164fp. PMID 18845911. 
  7. ↑ "Sch 50971, an orally active histamine H3 receptor agonist, inhibits central neurogenic vascular inflammation and produces sedation in the guinea pig". The Journal of Pharmacology and Experimental Therapeutics 287 (1): 43–50. October 1998. doi:10.1016/S0022-3565(24)37761-4. PMID 9765320. 
  8. ↑ "4-((3R,4R)-4-methylpyrrolidin-3-yl)-1H-imidazole". https://pubchem.ncbi.nlm.nih.gov/compound/9815232. 
  9. ↑ "The medicinal chemistry and therapeutic potentials of ligands of the histamine H3 receptor". Progress in Drug Research / Fortschritte der Arzneimittelforschung / Progrès des Recherches Pharmaceutiques. 45. 1995. pp. 107–165. doi:10.1007/978-3-0348-7164-8_4. ISBN 978-3-0348-7166-2. 
  10. ↑ "Computer-Assisted Analysis of Histamine H 2 − and H 3 -Receptor Agonists". Quantitative Structure-Activity Relationships 14 (2): 121–125. 1995. doi:10.1002/qsar.19950140203. ISSN 0931-8771. https://onlinelibrary.wiley.com/doi/10.1002/qsar.19950140203. Retrieved 6 October 2025. 



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