Abstract: Novel sequences for calcium channel ?2?-2 and ?2?-3 subunits are provided. Also provided are cell lines that express the novel calcium channel subunits of the invention. These cells may be used for identifying compounds capable of stimulating or inhibiting the activation of the calcium channels.

Abstract: Sequences and partial sequences for three types of mammalian (human and rat sequences identified) T-type calcium channel subunits which we have labeled as the ?1G, ?1H and ?1I subunits are provided. Knowledge of the sequence of these calcium channel permits the localization and recovery of the complete sequence from human cells, and the development of cell lines which express the novel calcium channels of the invention. These cells may be used for identifying compounds capable of acting as agonists or antagonists to the calcium channels.

Abstract: Compounds of the formula and their salts, wherein Cy represents cyclohexyl; Y is CH?CH?, CH?2, ? or Cy, X is trivalent straight-chain alkylene (3–10C) or trivalent straight-chain 1-alkenylene (3–10C) optionally substituted by oxo at the C adjacent N when n is 0 and Y is ?2CH; and is otherwise trivalent straight-chain alkylene (5–10C) or trivalent straight-chain 1-alkenylene (5–10C) optionally substituted by oxo at the C adjacent N; Z is N, NCO, CHNCOR1 or CHNR1, wherein R1 is alkyl (1–6C); and n is 0–5; wherein each ? and Cy independently may optionally be substituted by alkyl (1–6C) or by halo, CF3, OCF3, NO2, NR2, OR, SR, COR, COOR, CONR2, NROCR or OOCR where R is H or alkyl (1–4C), or two substituents may form a 5–7 membered ring with the proviso that the compounds of formula (1) contain at least one aromatic moiety, are useful as calcium channel blockers.

Abstract: Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.

Abstract: Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.

Abstract: Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.

Abstract: Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.

Abstract: Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.

Abstract: Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.

Abstract: Compounds of the formula 1

Abstract: A fluorescence based assay for compounds that modulate T-type calcium ion channels and that can be adapted to high throughput screening formats. Modulators of T-type channels are useful to correct functional abnormalities. These abnormalities are associated with epilepsy, pain, schizophrenia, depression, anxiety, cardiac arrhythmia, hypertension, certain types of cancer, diabetes, infertility, sexual dysfunction and other undesirable conditions.

Abstract: Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.

Abstract: Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.

Abstract: Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.

Abstract: Compounds comprising at least one aromatic ring linked to a heterocycle are described which are useful in altering abnormal calcium channel activity.

Abstract: Compounds of the formula and their salts, wherein Cy represents cyclohexyl; Y is CH═CH&PHgr;, CH&PHgr;2, &PHgr; or Cy, X is trivalent straight-chain alkylene (3-10C) or trivalent straight-chain 1-alkenylene (3-10C) optionally substituted by oxo at the C adjacent N when n is 0 and Y is &PHgr;2CH; and is otherwise trivalent straight-chain alkylene (5-10C) or trivalent straight-chain 1-alkenylene (5-10C) optionally substituted by oxo at the C adjacent N; Z is N, NCO, CHNCOR1 or CHNR1, wherein R1 is alkyl (1-6C); and n is 0-5; wherein each &PHgr; and Cy independently may optionally be substituted by alkyl (1-6C) or by halo, CF3, OCF3, NO2, NR2, OR, SR, COR, COOR, CONR2, NROCR or OOCR where R is H or alkyl (1-4C), or two substituents may form a 5-7 membered ring with the proviso that the compounds of formula (1) contain at least one aromatic moiety, are useful as calcium channel blockers.

Abstract: A specific amino acid sequence proximal to the carboxy terminus of P/Q type ion channels has been shown to mediate, through binding to the Homer protein, the expression of the gene encoding syntaxin-1A. This region of the P/Q type calcium ion channel provides peptides that can be used in screening assays for compounds that modulate the central nervous system.

Abstract: Compounds of the formula 1

Abstract: Compounds of the formula or the salts thereof, wherein each Z is independently N or CH, but one Z must be N; wherein n1 is 1 and n2 is 0 or 1; X1 and X2 are linkers; Ar represents one or two substituted or unsubstituted aromatic or heteroaromatic rings, and Cy represents one or two substituted or unsubstituted aliphatic cyclic or heterocyclic rings, or consists of one substituted or unsubstituted aliphatic cyclic or heterocyclic ring and one substituted or unsubstituted aromatic or heteroaromatic ring; each of Ya and Yb is two substituted or unsubstituted aromatic or heteroaromatic rings, or can be two substituted or unsubstituted aliphatic cyclic or heterocyclic rings or consists of one substituted or unsubstituted aliphatic cyclic or heterocyclic ring and one substituted or unsubstituted aromatic or heteroaromatic ring; with the proviso that said rings cannot both be phenyl when both Ar includes a single phenyl ring and X1 contains less than 5C; and with the proviso that formula (1

Abstract: Compounds of the formula and their salts, wherein Cy represents cyclohexyl; Y is CH═CH&PHgr;, CH&PHgr;2, &PHgr; or Cy, X is trivalent straight-chain alkylene (3-10C) or trivalent straight-chain 1-alkenylene (3-10C) optionally substituted by oxo at the C adjacent N when n is 0 and Y is &PHgr;2CH; and is otherwise trivalent straight-chain alkylene (5-10C) or trivalent straight-chain 1-alkenylene (5-10C) optionally substituted by oxo at the C adjacent N; Z is N, NCO, CHNCOR1 or CHNR1, wherein R1 is alkyl (1-6C); and n is 0-5; wherein each &PHgr; and Cy independently may optionally be substituted by alkyl (1-6C) or by halo, CF3, OCF3, NO2, NR2, OR, SR, COR, COOR, CONR2, NROCR or OOCR where R is H or alkyl (1-4C), or two substituents may form a 5-7 membered ring with the proviso that the compounds of formula (1) contain at least one aromatic moiety, are useful as calcium channel blockers.