Published in Drug Des Discov on June 01, 1994
A recursive-partitioning model for blood-brain barrier permeation. J Comput Aided Mol Des (2005) 0.84
Prediction of blood-brain partitioning using Monte Carlo simulations of molecules in water. J Comput Aided Mol Des (2001) 0.80
Prediction of blood-brain barrier permeation using quantum chemically derived information. J Comput Aided Mol Des (2003) 0.76
Definition and antagonism of histamine H 2 -receptors. Nature (1972) 18.58
Metiamide--an orally active histamine H2-receptor antagonist. Agents Actions (1973) 6.82
Dimaprit -(S-[3-(N,N-dimethylamino)prophyl]isothiourea) - a highly specific histamine H2 -receptor agonist. Part 1. Pharmacology. Agents Actions (1977) 3.33
Chemical differentiation of histamine H1- and H2-receptor agonists. J Med Chem (1975) 3.20
Some chemical aspects of histamine H2-receptor antagonists. Fed Proc (1976) 3.07
Impromidine (SK&F 92676) is a very potent and specific agonist for histamine H2 receptors. Nature (1978) 2.91
International Union of Pharmacology. XIII. Classification of histamine receptors. Pharmacol Rev (1997) 2.71
Compounds affecting the central nervous system. I. 4-Piperidones and related compounds. J Med Chem (1965) 2.69
Calcium-activated potassium channels sustain calcium signaling in T lymphocytes. Selective blockers and manipulated channel expression levels. J Biol Chem (2001) 1.88
High constitutive activity of native H3 receptors regulates histamine neurons in brain. Nature (2000) 1.60
The pharmacology of cimetidine, a new histamine H2-receptor antagonist. Br J Pharmacol (1975) 1.51
Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist. J Pharmacol Exp Ther (1998) 1.38
Characterization and development of cimetidine as a histamine H2-receptor antagonist. Gastroenterology (1978) 1.35
S-[2-(4-imidazolyl)ethyl]isothiourea, a highly specific and potent histamine H3 receptor agonist. J Pharmacol Exp Ther (1992) 1.22
Correlation between log POCT/H2O and pKB estimates for a series of muscarinic and histamine H2-receptor antagonists. Br J Pharmacol (1988) 1.18
Development of a new physicochemical model for brain penetration and its application to the design of centrally acting H2 receptor histamine antagonists. J Med Chem (1988) 1.18
Bis-quinolinium cyclophanes: 6,10-diaza-3(1,3),8(1,4)-dibenzena-1,5(1,4)- diquinolinacyclodecaphane (UCL 1684), the first nanomolar, non-peptidic blocker of the apamin-sensitive Ca(2+)-activated K+ channel. J Med Chem (1998) 1.17
Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain. Br J Pharmacol (2000) 1.12
Cyanoguanidine-thiourea equivalence in the development of the histamine H2-receptor antagonist, cimetidine. J Med Chem (1977) 1.10
Characterization and inhibition of a cholecystokinin-inactivating serine peptidase. Nature (1996) 1.09
Synthesis, molecular modeling, and pharmacological testing of bis-quinolinium cyclophanes: potent, non-peptidic blockers of the apamin-sensitive Ca(2+)-activated K(+) channel. J Med Chem (2000) 1.07
Discrimination between subtypes of apamin-sensitive Ca(2+)-activated K+ channels by gallamine and a novel bis-quaternary quinolinium cyclophane, UCL 1530. Br J Pharmacol (1996) 1.01
BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor: Preclinical pharmacology. J Pharmacol Exp Ther (2006) 1.01
Selective impairment of atrioventricular conduction by 2-(2-pyridyl)-ethylamine and 2-(2-thiazolyl)-ethylamine, two histamine H1-receptor agonists. Eur J Pharmacol (1975) 0.99
Sedation and histamine H1-receptor antagonism: studies in man with the enantiomers of chlorpheniramine and dimethindene. Br J Pharmacol (1991) 0.97
Dimaprit, (S-[3-(N,N-dimethylamino)propyl]isothiourea). A highly specific histamine H2-receptor agonist. Part 2. Structure-activity considerations. Agents Actions (1977) 0.96
Sulphur-methylene isosterism in the development of metiamide, a new histamine H2-receptor antagonist. Nature (1974) 0.95
Binding of [3H]cimetidine to rat brain tissue. Agents Actions (1980) 0.92
Clotrimazole analogues: effective blockers of the slow afterhyperpolarization in cultured rat hippocampal pyramidal neurones. Br J Pharmacol (2001) 0.90
The pressor activity of burimamide: a relationship between chemical constitution and pressor activity of burimamide and related histamine H2-receptor antagonists. Agents Actions (1977) 0.89
Modulation of GABA(A) receptors and inhibitory synaptic currents by the endogenous CNS sleep regulator cis-9,10-octadecenoamide (cOA). Br J Pharmacol (1998) 0.88
Histamine-induced inhibition of lymphocyte proliferation and lysosomal enzyme release from polymorphs may not be mediated via H1- or H2-receptors. Agents Actions (1982) 0.88
[125I]Iodobolpyramine, a highly sensitive probe for histamine H1-receptors in guinea-pig brain. Eur J Pharmacol (1986) 0.87
Compounds that block both intermediate-conductance (IK(Ca)) and small-conductance (SK(Ca)) calcium-activated potassium channels. Br J Pharmacol (2000) 0.87
Zolantidine (SK&F 95282) is a potent selective brain-penetrating histamine H2-receptor antagonist. Br J Pharmacol (1988) 0.87
Influence of imidazole replacement in different structural classes of histamine H(3)-receptor antagonists. Eur J Pharm Sci (2001) 0.85
bis-Quinolinium cyclophanes: 8,14-diaza-1,7(1, 4)-diquinolinacyclotetradecaphane (UCL 1848), a highly potent and selective, nonpeptidic blocker of the apamin-sensitive Ca(2+)-activated K(+) channel. J Med Chem (2000) 0.85
(Partial) agonist/antagonist properties of novel diarylalkyl carbamates on histamine H3 receptors. Bioorg Med Chem (2000) 0.84
Icotidine, an antagonist of histamine at both H1 and H2 receptors. N Engl Reg Allergy Proc (1987) 0.84
The histamine H3 receptor and its ligands. Prog Med Chem (2001) 0.83
The synthesis and some pharmacological actions of the enantiomers of the K(+)-channel blocker cetiedil. J Pharm Pharmacol (1996) 0.83
The histamine H2 receptor agonist impromidine: synthesis and structure-activity considerations. J Med Chem (1985) 0.83
Proceedings: 3-(4(5)-imidazolyl) propylguanidine (SK&F 91486) - a partial agonist at histamine H2-receptors. Agents Actions (1975) 0.83
Differences in the actions of some blockers of the calcium-activated potassium permeability in mammalian red cells. Br J Pharmacol (1999) 0.81
Characterization of histamine H1-receptor binding peptides in guinea pig brain using [125I]iodoazidophenpyramine, an irreversible specific photoaffinity probe. Proc Natl Acad Sci U S A (1988) 0.81
Search for histamine H3 receptor antagonists with combined inhibitory potency at Ntau-methyltransferase: ether derivatives. Pharmazie (2005) 0.81
Synthesis and quantitative structure-activity relationship of a novel series of small conductance Ca(2+)-activated K+ channel blockers related to dequalinium. J Med Chem (1996) 0.80
Dipole moment in relation to H2 receptor histamine antagonist activity for cimetidine analogues. J Med Chem (1986) 0.80
Evidence for low brain penetration by the H1-receptor antagonist temelastine (SK&F 93944). Eur J Pharmacol (1987) 0.80
Novel partial agonists for the histamine H(3) receptor with high in vitro and in vivo activity. J Med Chem (1999) 0.79
Histamine H1-receptor in heart: unique electrophoretic mobility and autoradiographic localization. J Neurochem (1990) 0.79
Potential histamine H2-receptor antagonists. 3. Methylhistamines. J Med Chem (1976) 0.79
Synthesis and structure-activity relationships of cetiedil analogues as blockers of the Ca(2+)-activated K+ permeability of erythrocytes. J Med Chem (2001) 0.78
Conformation of histamine derivatives. 3. A relationship between conformation and pharmacological activity. J Med Chem (1973) 0.78
Therapeutic implications of constitutive activity of receptors: the example of the histamine H3 receptor. J Neural Transm Suppl (2003) 0.78
Synthesis and structure-activity relationships of dequalinium analogues as K+ channel blockers. Investigations on the role of the charged heterocycle. J Med Chem (1995) 0.78
Different antagonist binding properties of human and rat histamine H3 receptors. Bioorg Med Chem Lett (2001) 0.78
Letter: Calculation of conformational free energy of histamine. J Theor Biol (1974) 0.78
Tautomerism of 4-methylhistamine--effect of the methyl substituent [proceedings]. Agents Actions (1979) 0.78
Benzophenone derivatives and related compounds as potent histamine H3-receptor antagonists and potential PET/SPECT ligands. Arch Pharm (Weinheim) (2001) 0.77
Medicinal chemistry in the development of societies. Biodiversity and natural products. Eur J Med Chem (2000) 0.76
On the concept of a bivalent pharmacophore for SKCa channel blockers: synthesis, pharmacological testing, and radioligand binding studies on mono-, bis-, and tris-quinolinium compounds. Arch Pharm (Weinheim) (1996) 0.76
New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency. J Med Chem (2000) 0.76
Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists. Bioorg Med Chem Lett (2000) 0.76
N-Methyldimaprit (SK&F92054). A chemical control for the histamine H2-receptor agonist dimaprit. Agents Actions (1986) 0.75
Synthesis and quantitative structure-activity relationships of dequalinium analogues as K+ channel blockers: investigation into the role of the substituent at position 4 of the quinoline ring. J Med Chem (1995) 0.75
Synthesis and pharmacological testing of dequalinium analogues as blockers of the apamin-sensitive Ca(2+)-activated K+ channel: variation of the length of the alkylene chain. J Med Chem (1996) 0.75
Structures of histamine H1-receptor antagonists derived from the cimetidine group of histamine H2-receptor antagonists. Acta Crystallogr B (1994) 0.75
The pharmacology of cimetidine, a new histamine H2-receptor antagonist. 1975. Br J Pharmacol (2010) 0.75
Design of an affinity matrix for purification of the histamine H1 receptor from guinea pig cerebellum. J Neurochem (1992) 0.75
Development of chiral N-alkylcarbamates as new leads for potent and selective H3-receptor antagonists: synthesis, capillary electrophoresis, and in vitro and oral in vivo activity. J Med Chem (1999) 0.75
Compounds affecting the central nervous system. IV. Substituted 2-benzyl-3-dialkylaminoalkylindenes and related compounds. J Med Chem (1967) 0.75
Dimaprit, [S-[3-(N,N-dimethylamino)propyl]isothiourea]. A highly specific histamine H2-receptor agonist. Part 2. Structure-activity considerations. 1977. Agents Actions (1994) 0.75
Importance of the lipophilic group in carbamates having histamine H3-receptor antagonist activity. Pharmazie (2000) 0.75
Substituted N-phenylcarbamates as histamine H3 receptor antagonists with improved in vivo potency. Pharmazie (2000) 0.75
Molecule--receptor specificity. Philos Trans R Soc Lond B Biol Sci (1975) 0.75
Metiamide--an orally active histamine H2-receptor antagonist. 1973. Agents Actions (1994) 0.75
Structure-activity studies of pyridinylalkyl-isocytosine H1-receptor antihistamines and identification of an active conformation. Farmaco (1991) 0.75
Stereochemical studies of chiral H-1 antagonists of histamine: the resolution, chiral analysis, and biological evaluation of four antipodal pairs. Chirality (1992) 0.75
The synthesis of tertiary arylalkylamines from aryl Grignard reagents. J Med Chem (1966) 0.75
Polyclonal and monoclonal antibodies directed against SK & F 94461, a specific H1 histamine receptor ligand. Mol Pharmacol (1988) 0.75
Potential histamine H2-receptor antagonists. 4. Benzylhistamines. J Med Chem (1982) 0.75
Conformation of histamine derivatives. 1. Application of molecular orbital calculations and nuclear magnetic resonance spectroscopy. J Med Chem (1973) 0.75
Dimaprit--[S-[3-(N,N-dimethylamino)propyl]isothiourea]--a highly specific histamine H2-receptor agonist. Part 1. Pharmacology. 1977. Agents Actions (1994) 0.75
Novel histamine H(3)-receptor antagonists with carbonyl-substituted 4-(3-(phenoxy)propyl)-1H-imidazole structures like ciproxifan and related compounds. J Med Chem (2000) 0.75
The tautomer ratio of histamine. J Pharm Pharmacol (1973) 0.75
Synthesis, molecular modeling, and K+ channel-blocking activity of dequalinium analogues having semirigid linkers. J Med Chem (1996) 0.75
Conformation of histamine derivatives. 2. Molecular orbital calculations of preferred conformations in relation to dual receptor activity. J Med Chem (1973) 0.75
Indane and indene derivatives of biological interest. Adv Drug Res (1967) 0.75
Analogues of triprolidine: structural influences upon antihistamine activity. J Pharm Pharmacol (1992) 0.75
Compounds affecting the central nervous system. V. Substituted 3-dialkylaminoalkylindenes. J Med Chem (1969) 0.75
Zwitterionic analogues of cimetidine as H2 receptor antagonists. J Med Chem (1987) 0.75
Relative concentrations of zwitterionic and uncharged species in catecholamines and the effect of N-substituents. J Med Chem (1977) 0.75
Photolabile derivatives of 125I-apamin: defining the structural criteria required for labeling high and low molecular mass polypeptides associated with small conductance Ca(2+)-activated K+ channels. Biochemistry (1996) 0.75